tofacitinib (Rx)

Brand and Other Names:Xeljanz, Xeljanz XR
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet (Xeljanz)

  • 5mg
  • 10mg

tablet, extended-release (Xeljanz XR)

  • 11mg
  • 22mg

Rheumatoid Arthritis

Xeljanz or Xeljanz XR

Indicated for moderate-to-severe active rheumatoid arthritis (RA) in adults with an inadequate response or intolerance to methotrexate; may be used as monotherapy or in combination with methotrexate or other nonbiologic DMARDs

Xeljanz: 5 mg PO BID

Xeljanz XR: 11 mg PO qDay

Psoriatic Arthritis

Xeljanz or Xeljanz XR

Indicated for active psoriatic arthritis who have had an inadequate response or intolerance to methotrexate or other DMARDs

Recommended dose in combination with nonbiologic DMARDs

  • Xeljanz: 5 mg PO BID
  • Xeljanz XR: 11 mg PO qDay

Ulcerative Colitis

Xeljanz or Xeljanz XR

Indicated for adults with moderately to severely active ulcerative colitis (UC)

Xeljanz

  • Induction
    • 10 mg PO BID for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response
    • If needed, continue 10 mg BID for maximum of 16 weeks; discontinue after 16 weeks if adequate therapeutic benefit not achieved
  • Maintenance
    • 5 mg PO BID; may consider 10 mg BID (limited to shorter duration) in patients with loss of response during maintenance treatment
    • Use the lowest effective dose needed to maintain response

Xeljanz XR

  • Induction
    • 22 mg PO qDay for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response
    • If needed, continue 22 mg qDay for maximum of 16 weeks; discontinue after 16 weeks if adequate therapeutic benefit not achieved
  • Maintenance
    • 11 mg PO qDay; may consider 22 mg qDay (limited to shorter duration) in patients with loss of response during maintenance treatment
    • Use the lowest effective dose needed to maintain response

Dosage Modifications

Strong CYP3A4 inhibitors OR moderate CYP3A4 inhibitors with strong CYP2C19 inhibitors

  • RA or PsA
    • Xeljanz: Not to exceed 5 mg qDay
    • Xeljanz XR: Switch to Xeljanz 5 mg qDay
  • UC
    • Xeljanz: If taking 10 mg BID, reduce to 5 mg BID; if taking 5 mg BID, reduce to 5 mg qDay
    • Xeljanz XR: If taking 22 mg qDay, reduce to 11 mg qDay; if taking 11 mg qDay, switch to Xeljanz 5 mg qDay

Renal impairment

  • RA or PsA
    • Mild: No dosage adjustment required
    • Moderate-to-severe (Xeljanz): Not to exceed 5 mg qDay
    • Moderate-to-severe (Xeljanz XR): Switch to Xeljanz 5 mg qDay
  • UC
    • Mild (Xeljanz and Xeljanz XR): No dosage adjustment required
    • Moderate-to-severe (Xeljanz): If taking 10 mg BID, reduce to 5 mg BID; if taking 5 mg BID, reduce to 5 mg qDay
    • Moderate-to-severe (Xeljanz XR): If taking 22 mg qDay, reduce to 11 mg qDay; if taking 11 mg qDay, switch to Xeljanz 5 mg qDay
    • For patients undergoing hemodialysis, administer dose after session on dialysis days

Hepatic impairment

  • Safety and efficacy have not been studied in patients with positive hepatitis B virus or hepatitis C virus serology (Add to adult)
  • RA or PsA
    • Mild (Xeljanz and Xeljanz XR): No dosage adjustment required
    • Moderate (Xeljanz): Not to exceed 5 mg qDay
    • Moderate (Xeljanz XR): Switch to Xeljanz 5 mg qDay
    • Severe (Xeljanz and Xeljanz XR): Not recommended
  • UC
    • Mild (Xeljanz and Xeljanz XR): No dosage adjustment required
    • Moderate (Xeljanz): If taking 10 mg BID, reduce to 5 mg BID; if taking 5 mg BID, reduce to 5 mg qDay
    • Moderate (Xeljanz XR): If taking 22 mg qDay, reduce to 11 mg qDay; if taking 11 mg qDay, switch to Xeljanz 5 mg qDay
    • Severe (Xeljanz and Xeljanz XR): Not recommended

Lymphopenia

  • RA, PsA, or UC
    • Lymphocytes ≥500 cells/mm3: Maintain dose
    • Lymphocytes <500 cells/mm3: Confirmed by repeat testing; discontinue until infection controlled

ANC 500-1000cells/mm³

  • RA or PsA
    • Interrupt dosing for persistent decreases; when ANC >1000/mm3, resume dose at Xeljanz 5 mg BID or Xeljanz XR 11 mg qDay
    • ANC <500 cells/mm3: Confirmed by repeat testing; discontinue
  • UC
    • Xeljanz: If taking 10 mg BID, reduce to 5 mg BID; when ANC >1000, increase to 10 mg BID based on clinical response; if taking 5 mg BID, interrupt dosing; when ANC >1000, resume 5 mg BID
    • Xeljanz XR: If taking 22 mg qDay, reduce to 11 mg qDay when ANC >1000, increase to 22 mg qDay based on clinical response; if taking 11 mg qDay, interrupt dosing; when ANC >1000, resume 11 mg qDay

Anemia

  • RA, PsA, or UC
    • Hgb ≤2 g/dL decrease and level ≥9.0 g/dL: Maintain dose
    • Hgb >2 g/dL decrease or level <8.0 g/dL: Confirmed by repeat testing; interrupt treatment until Hgb levels have normalized

Dosing Considerations

Should not be used in combination with biologic DMARDs or potent immunosuppressive agents (eg, azathioprine, cyclosporine)

Interrupt dose for management of lymphopenia, neutropenia, and anemia

Interrupt use if patient develops a serious infection until the infection is controlled

There is a higher incidence of infections in geriatric patients; use with caution

Do not initiate if

  • Absolute lymphocyte count <500 cells/mm³ OR
  • ANC <1000 cells/mm³ OR
  • Hgb <9 g/dL

Dosage Forms & Strengths

oral solution (Xeljanz)

  • 1mg/mL

tablet (Xeljanz)

  • 5mg
  • 10mg

Polyarticular Course Juvenile Idiopathic Arthritis

Indicated for active polyarticular course juvenile idiopathic arthritis (pcJIA) in patients aged ≥2 years

≥2 years

  • Oral solution
    • 10 to <20 kg: 3.2 mg PO BID
    • 20 to <40 kg: 4 mg PO BID
  • Oral solution or tablet
    • ≥40 kg: 5 mg PO BID

Dosage Modifications

Coadministration with strong CYP3A4 inhibitors, OR a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s)

  • pcJIA
    • If taking 3.2 mg BID, reduce to 3.2 mg qDay
    • If taking 4 mg BID, reduce to 4 mg qDay
    • If taking 5 mg BID, reduce to 5 mg qDay

Hematologic abnormalities

  • Do not initiate in patients with an absolute lymphocyte count <500 cells/mm3, ANC <1000 cells/mm3 or Hgb <9 g/dL
  • Lymphocyte count <500 cells/mm3: Confirmed by repeat testing; discontinue dosing
  • ANC 500-1000 cells/mm3: Interrupt dosing until ANC >1000 cells/mm3
  • ANC <500 cells/mm3: Discontinue dosing
  • Hgb <8 g/dL or a decrease of >2 g/dL: Interrupt dosing until Hgb normalized

Renal impairment

  • pcJIA
    • Mild: No dosage adjustment required
    • Moderate-to-severe: Reduce dosing frequency to qDay (eg, 3.2 mg BID to 3.2 mg qDay)
    • Hemodialysis: Administer after dialysis session on dialysis days; if dose taken before dialysis, supplemental doses are not recommended after dialysis

Hepatic impairment

  • pcJIA
    • Mild: No dosage adjustment required
    • Moderate: Reduce dosing frequency to qDay (eg, 3.2 mg BID to 3.2 mg qDay)
    • Severe: Not studied; not recommended
    • Safety and efficacy have not been studied in patients with positive hepatitis B virus or hepatitis C virus serology (Add to adult)

Dosing Considerations

Limitation of use: Use in combination with biologic DMARDs or potent immunosuppressants (eg, azathioprine, cyclosporine) is not recommended

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Interactions

Interaction Checker

and tofacitinib

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              Serious - Use Alternative (109)

              • abametapir

                abametapir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

              • abatacept

                abatacept, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • antithymocyte globulin equine

                antithymocyte globulin equine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • antithymocyte globulin rabbit

                antithymocyte globulin rabbit, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • apalutamide

                apalutamide will decrease the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP2C19 inducer, with drugs that are CYP2C19 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered.

                apalutamide will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

              • atazanavir

                atazanavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • auranofin

                auranofin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • azathioprine

                azathioprine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • baricitinib

                baricitinib, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Baricitinib is not recommended in combination with other JAK inhibitors, biologic DMARDs, or potent immunosuppressives.

              • basiliximab

                basiliximab, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • belatacept

                belatacept, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • bendamustine

                bendamustine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • betamethasone

                betamethasone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • busulfan

                busulfan, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • capecitabine

                capecitabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • carboplatin

                carboplatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • carmustine

                carmustine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • certolizumab pegol

                certolizumab pegol, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • chlorambucil

                chlorambucil, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • chloramphenicol

                chloramphenicol will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • cimetidine

                cimetidine increases levels of tofacitinib by decreasing metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with 1 or more concomitant medications that result in both moderate CYP3A4 inhibition and potent CYP2C19 inhibition.

              • cisplatin

                cisplatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • cladribine

                cladribine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • clarithromycin

                clarithromycin increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • clofarabine

                clofarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • cobicistat

                cobicistat increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • conivaptan

                conivaptan increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • corticotropin

                corticotropin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • cortisone

                cortisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • cyclophosphamide

                cyclophosphamide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • cyclosporine

                cyclosporine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • cytarabine

                cytarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • dacarbazine

                dacarbazine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • darunavir

                darunavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • daunorubicin

                daunorubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • deferiprone

                deferiprone, tofacitinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.

              • dexamethasone

                dexamethasone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • doxorubicin

                doxorubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • doxorubicin liposomal

                doxorubicin liposomal, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • epirubicin

                epirubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • etanercept

                etanercept, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • everolimus

                everolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • fexinidazole

                fexinidazole will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

              • floxuridine

                floxuridine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • fluconazole

                fluconazole increases levels of tofacitinib by decreasing metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with 1 or more concomitant medications that result in both moderate CYP3A4 inhibition and potent CYP2C19 inhibition.

              • fludarabine

                fludarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • fludrocortisone

                fludrocortisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • fluorouracil

                fluorouracil, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • fosamprenavir

                fosamprenavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • gemcitabine

                gemcitabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • gold sodium thiomalate

                gold sodium thiomalate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • hydrocortisone

                hydrocortisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • hydroxychloroquine sulfate

                hydroxychloroquine sulfate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • hydroxyurea

                hydroxyurea, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • idelalisib

                idelalisib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

              • ifosfamide

                ifosfamide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.

                ifosfamide will increase the level or effect of tofacitinib by Other (see comment). Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.

              • imatinib

                imatinib increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • indinavir

                indinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • infliximab

                infliximab, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • isoniazid

                isoniazid increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • itraconazole

                itraconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • ivosidenib

                ivosidenib will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

              • ketoconazole

                ketoconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • leflunomide

                leflunomide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • lomustine

                lomustine will increase the level or effect of tofacitinib by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.

              • lonafarnib

                lonafarnib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

                lonafarnib will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Lonafarnib may increase the AUC and peak concentration of CYP2C19 substrates. If coadministration unavoidable, monitor for adverse reactions and reduce the CYP2C19 substrate dose in accordance with its approved product labeling.

              • lopinavir

                lopinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • mechlorethamine

                mechlorethamine will increase the level or effect of tofacitinib by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.

              • mechlorethamine topical

                mechlorethamine topical, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • melphalan

                melphalan will increase the level or effect of tofacitinib by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.

              • mercaptopurine

                mercaptopurine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • methotrexate

                methotrexate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • methylprednisolone

                methylprednisolone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • mitoxantrone

                mitoxantrone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • muromonab CD3

                muromonab CD3, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • mycophenolate

                mycophenolate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • nefazodone

                nefazodone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • nelarabine

                nelarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • nelfinavir

                nelfinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • nicardipine

                nicardipine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • oxaliplatin

                oxaliplatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • pemetrexed

                pemetrexed, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • pentostatin

                pentostatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • posaconazole

                posaconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • pralatrexate

                pralatrexate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • prednisolone

                prednisolone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • prednisone

                prednisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • procarbazine

                procarbazine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.

              • quinidine

                quinidine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • ribociclib

                ribociclib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • ritonavir

                ritonavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • saquinavir

                saquinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • sirolimus

                sirolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • streptozocin

                streptozocin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • tacrolimus

                tacrolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • temozolomide

                temozolomide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • temsirolimus

                temsirolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • thioguanine

                thioguanine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • thiotepa

                thiotepa, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • tipranavir

                tipranavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • triamcinolone acetonide injectable suspension

                triamcinolone acetonide injectable suspension, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • tucatinib

                tucatinib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

              • valrubicin

                valrubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • vinblastine

                vinblastine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • vincristine

                vincristine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • vincristine liposomal

                vincristine liposomal, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • vinorelbine

                vinorelbine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • voriconazole

                voriconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.

              • voxelotor

                voxelotor will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

              Monitor Closely (74)

              • amiodarone

                amiodarone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • aprepitant

                aprepitant increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • bicalutamide

                bicalutamide increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • bosentan

                bosentan will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • cannabidiol

                cannabidiol will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of sensitive CYP2C19 substrates, as clinically appropriate, when coadministered with cannabidiol.

              • carbamazepine

                carbamazepine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • cenobamate

                cenobamate will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider a dose reduction of CYP2C19 substrates, as clinically appropriate, when used concomitantly with cenobamate.

              • cimetidine

                cimetidine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

                cimetidine increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • clozapine

                clozapine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • crizotinib

                crizotinib increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • cyclosporine

                cyclosporine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • dabrafenib

                dabrafenib will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • desipramine

                desipramine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • dexamethasone

                dexamethasone will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • diltiazem

                diltiazem increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • doxycycline

                doxycycline increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • dronedarone

                dronedarone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • duvelisib

                duvelisib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.

              • efavirenz

                efavirenz increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers.

              • elagolix

                elagolix will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak CYP2C19 inhibitor. Caution with sensitive CYP2C19 substrates.

                elagolix decreases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

              • encorafenib

                encorafenib, tofacitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

              • enzalutamide

                enzalutamide will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • erythromycin base

                erythromycin base increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • erythromycin ethylsuccinate

                erythromycin ethylsuccinate increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • erythromycin lactobionate

                erythromycin lactobionate increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • erythromycin stearate

                erythromycin stearate increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • eslicarbazepine acetate

                eslicarbazepine acetate will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

                eslicarbazepine acetate will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              • etravirine

                etravirine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • fedratinib

                fedratinib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

                fedratinib will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP2C19 substrates as necessary.

              • fexinidazole

                fexinidazole will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              • fluconazole

                fluconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

                fluconazole increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • fluvoxamine

                fluvoxamine increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Decrease tofacitinib dose is coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • gemfibrozil

                gemfibrozil increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • grapefruit

                grapefruit increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • haloperidol

                haloperidol increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • iloperidone

                iloperidone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • isoniazid

                isoniazid increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • istradefylline

                istradefylline will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

              • lapatinib

                lapatinib increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • lidocaine

                lidocaine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • lorlatinib

                lorlatinib will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • lumacaftor/ivacaftor

                lumacaftor/ivacaftor, tofacitinib. affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2C19 substrates. .

              • metronidazole

                metronidazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • mifepristone

                mifepristone will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If coadministration necessary, reduce dose of tofacitinib if chronic mifepristone therapy used; reduce to 5 mg twice daily in patients receiving 10 mg twice daily; reduce to 5 mg once daily in patients receiving 5 mg twice daily; change to 11 mg XR once daily in patients receiving 22 mg once daily of XR formulation; change to immediate-release formulation at dose of 5 mg once daily in patients receiving 11 mg XR once daily

              • mitotane

                mitotane decreases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

              • modafinil

                modafinil increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • nafcillin

                nafcillin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • nevirapine

                nevirapine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • ocrelizumab

                tofacitinib and ocrelizumab both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Coadministration of ocrelizumab with immunosuppressants may increase the risk of immunosuppression.

              • ofatumumab SC

                ofatumumab SC, tofacitinib. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.

              • omeprazole

                omeprazole increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • oxcarbazepine

                oxcarbazepine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • pentobarbital

                pentobarbital will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • phenobarbital

                phenobarbital will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • phenytoin

                phenytoin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • primidone

                primidone will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • rifabutin

                rifabutin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • rifampin

                rifampin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • rifapentine

                rifapentine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • rucaparib

                rucaparib will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP2C19 substrates, if clinically indicated.

              • sertraline

                sertraline increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.

              • siponimod

                siponimod and tofacitinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • St John's Wort

                St John's Wort will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers

              • stiripentol

                stiripentol, tofacitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

                stiripentol will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of CYP2C19 substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.

              • tecovirimat

                tecovirimat will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Tecovirimat is a weak inhibitor of CYP2C8 and CYP2C19. Monitor for adverse effects if coadministered with sensitive substrates of these enzymes.

                tecovirimat will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

              • tetracycline

                tetracycline increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • ticagrelor

                ticagrelor increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • ticlopidine

                ticlopidine increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • trastuzumab

                trastuzumab, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              • trastuzumab deruxtecan

                trastuzumab deruxtecan, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              • triclabendazole

                triclabendazole will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. If plasma concentrations of the CYP2C19 substrates are elevated during triclabendazole, recheck plasma concentration of the CYP2C19 substrates after discontinuation of triclabendazole.

              • verapamil

                verapamil increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              • zileuton

                zileuton increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .

              Minor (0)

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                Adverse Effects

                >10%

                UC

                • Nasopharyngitis (10-14%)

                1-10%

                RA

                • Upper respiratory tract infection (4%)
                • Nasopharyngitis (3-4%)
                • Diarrhea (3-4%)
                • Headache (3-4%)
                • Hypertension (2%)

                UC

                • Elevated cholesterol levels (5-9%)
                • Headache (3-9%)
                • Upper respiratory tract infection (6-7%)
                • Increased blood creatine phosphokinase (3-7%)
                • Rash (3-6%)
                • Diarrhea (2-5%)
                • Herpes zoster (1-5%)
                • Gastroenteritis (3-4%)
                • Anemia (2-4%)
                • Nausea (1-4%)

                Frequency Not Defined

                RA

                • Blood and lymphatic system disorders: Anemia
                • Infections and infestations: Diverticulitis
                • Metabolism and nutrition disorders: Dehydration
                • Psychiatric disorders: Insomnia
                • Nervous system disorders: Paresthesia
                • Respiratory, thoracic and mediastinal disorders: Dyspnea, cough, sinus congestion, interstitial lung disease (cases were limited to patients with rheumatoid arthritis and some were fatal)
                • Gastrointestinal disorders: Abdominal pain, dyspepsia, vomiting, gastritis, nausea
                • Hepatobiliary disorders: Hepatic steatosis
                • Skin and subcutaneous tissue disorders: Rash, erythema, pruritus
                • Musculoskeletal, connective tissue and bone disorders: Musculoskeletal pain, arthralgia, tendonitis, joint swelling
                • Neoplasms benign, malignant and unspecified (including cysts and polyps): Non-melanoma skin cancers
                • General disorders and administration site conditions: Pyrexia, fatigue, peripheral edema

                Postmarketing Reports

                Immune system disorders: Drug hypersensitivity

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                Warnings

                Serious infections

                • Increased risk for developing serious infections that may lead to hospitalization or death; most patients who developed these infections were taking concomitant immunosuppressants (eg, methotrexate, corticosteroid)
                • If serious infection develops, interrupt until infection controlled
                • Reported infections include active TB, invasive fungal infections, and bacterial, viral, or other opportunistic pathogens
                • Test for latent TB before and during tofacitinib treatment; treatment for latent TB infection should be initiated prior to tofacitinib treatment

                Malignancies

                • Lymphoma and other malignancies reported
                • Epstein Barr virus-associated post-transplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with tofacitinib and concomitant immunosuppressive medications

                Mortality

                • A higher rate of all-cause mortality, including sudden cardiovascular death, reported in rheumatoid arthritis patients ≥50 years with at least 1 cardiovascular risk factor treated with 10 mg BID compared to those treated with 5 mg BID or TNF blockers

                Increased risk of blood clots

                • Thrombosis, including pulmonary embolism, deep venous thrombosis, and arterial thrombosis have occurred in patients treated with Janus kinase inhibitors used to treat inflammatory conditions
                • Patients with rheumatoid arthritis aged ≥50 years with at least 1 CV risk factor treated with 10 mg BID showed an increased incidence of thrombosis compared with 5 mg BID or TNF blockers in a large, ongoing postmarketing safety study
                • Avoid in patients at risk
                • Discontinue therapy and promptly evaluate patients with thrombosis symptoms
                • For patients with ulcerative colitis, use lowest effective dose and for shortest duration needed to achieve/maintain therapeutic response

                Contraindications

                None

                Cautions

                Malignancy and lymphoproliferative disorders reported (see Black Box Warnings); malignancies were observed in clinical studies and the postmarketing setting, including, but not limited to, lung cancer, breast cancer, melanoma, prostate cancer, and pancreatic cancer

                GI perforation reported, although role of JAK inhibition in these events is unknown; caution in patients at increased risk for gastrointestinal perforation (eg, diverticulitis)

                Associated with gradual decrease in lymphocyte and neutrophils counts, and hemoglobin levels that may require treatment interruption

                Associated with increased LFTs

                Associated with increase lipid parameters including total cholesterol, LDL, and HDL

                Viral reactivation, including cases of herpes virus reactivation (e.g., herpes zoster), reported; hepatitis B reactivation reported; impact on chronic viral hepatitis reactivation unknown; perform screening for viral hepatitis in accordance with clinical guidelines before starting therapy

                Non-melanoma skin cancers (NMSCs) reported; periodic skin examination recommended for patients at increased risk for skin cancer

                Use caution when treating patients with diabetes; higher incidence of infection in diabetic population in general reported

                Diverticulitis reported

                Twice daily dosing of tofacitinib 10 mg or 11 mg tofacitinib XR not recommended in patients with rheumatoid arthritis or psoriatic arthritis

                Rheumatoid arthritis patients ≥50 years of age with at least 1 cardiovascular (CV) risk factor treated with tofacitinib 10 mg BID had a higher rate of all-cause mortality

                Thrombosis, including pulmonary embolism, deep venous thrombosis, and arterial thrombosis, have occurred

                Structural joint damage progression

                • Radiographic response data from the ORAL Scan and ORAL Start studies evaluated the efficacy of tofacitinib on structural joint damage progression as measured by mean change from baseline in van der Heijde modified Total Sharp Score (mTSS) and its components, erosion score, and joint space narrowing (JSN) score

                Serious infections

                • Serious and sometimes fatal infections reported due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens; the most common serious infections reported have included pneumonia, cellulitis, herpes zoster, urinary tract infection, diverticulitis, and appendicitis
                • In the UC population, treatment with 10 mg BID was associated with greater risk of serious infections compared with 5 mg BID; additionally, opportunistic herpes zoster infections (including meningoencephalitis, ophthalmologic, and disseminated cutaneous) were seen in patients who were treated with 10 mg twice daily
                • Use caution in patients with a history of chronic lung disease, or in those who develop interstitial lung disease, as they may be more prone to infections
                • Risk of infection may be higher with increasing degrees of lymphopenia; consideration should be given to lymphocyte counts when assessing individual patient risk of infection
                • Avoid use in patients with an active, serious infection, including localized infections
                • Consider the risks and benefits of tofacitinib prior to initiating treatment
                  • Patients with chronic or recurrent infection
                  • Patients who have been exposed to tuberculosis
                  • Patients with a history of a serious or an opportunistic infection
                  • Patients who have resided or traveled in areas of endemic tuberculosis or endemic mycoses
                  • Patients with underlying conditions that may predispose them to infection

                Extended-release tablet

                • Patients may notice an inert tablet shell passing in the stool or via colostomy
                • Caution when administering the extended-release tablet to patients with pre-existing severe gastrointestinal narrowing (pathologic or iatrogenic); rare reports of obstructive symptoms with strictures in association with the ingestion of other drugs utilizing a non-deformable extended release formulation

                Increased risk of serious heart-related problems and cancer

                • On September 1st, 2021, FDA is requiring revisions to the Boxed Warning for tofacitinib to include information about the risks of serious heart-related events, cancer, blood clots, and death
                • Revisions are based on results from completed trial show a higher occurrence of serious heart-related events and cancer in tofacitinib-treated group (both doses) compared to TNF inhibitor-treated group; results also showed an increased risk of blood clots and death with lower doses of tofacitinib
                • Consider the benefits and risks for the individual patient before initiating or continuing treatment, especially the following patients:
                  • Who are current or past smokers
                  • Who have other cardiovascular risk factors
                  • Who have developed a malignancy
                  • Who have a known malignancy other than a successfully treated nonmelanoma skin cancer
                • Reserve JAK inhibitors (eg, tofacitinib) if patients have an inadequate response or intolerance to ≥1 TNF blockers
                • Counsel patients about the benefits and risks of these medicines and advise them to seek emergency medical attention if they experience signs and symptoms of a heart attack, stroke, or blood clot

                Drug interactions overview

                • Tofacitinib is a CYP3A4 substrate and a minor CYP2C19 substrate
                • Strong CYP3A4 inducers may decrease clinical response
                • Decreased dose required if coadministered with strong CYP3A4 inhibitors, or moderate CYP3A4 inhibitors plus CYP2C19 inhibitors (see Dosage Modifications)
                • Avoid coadministration with live virus vaccines
                • Risk of added immunosuppression when tofacitinib is concomitantly used with potent immunosuppressive drugs (eg, azathioprine, tacrolimus, cyclosporine); combined use of multiple dose tofacitinib with potent immunosuppressants has not been studied in rheumatoid arthritis and psoriatic arthritis
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                Pregnancy & Lactation

                Pregnancy

                There is a pregnancy exposure registry that monitors pregnancy outcomes in women during pregnancy; patients can call the toll free number 1-877-311-8972

                There are no adequate and well-controlled studies therapy in pregnant women

                In the tofacitinib clinical development programs, birth defects and miscarriages were reported

                Animal data

                • Based on animal studies, tofacitinib has the potential to affect a developing fetus
                • Feticidal and teratogenic effects were noted when pregnant rats and rabbits received tofacitinib during the period of organogenesis at exposures multiples of 146 times and 13 times the human dose of 5 mg BID, respectively
                • In a peri and post-natal study in rats, tofacitinib resulted in reductions in live litter size, postnatal survival, and pup body weights at exposure multiples of approximately 73 times the human dose of 5 mg BID
                • Based on findings in rats, females of reproductive potential taking tofacitinib may result in reduced fertility

                Contraception

                • Advise females of reproductive potential to use effective contraception during treatment and for >4 weeks after the last dose
                • Advise females to inform their healthcare provider if they become pregnant, or if pregnancy is suspected, during treatment

                Lactation

                It is not known whether the drug is excreted in human milk

                There are no data to assess effects of drug on breastfed child; drug is excreted in rat milk at concentrations higher than in maternal serum

                Women should not breastfeed while treated; a decision should be made whether to discontinue breastfeeding or to discontinue therapy

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Janus kinases (JAKs) pathways inhibitor; JAK consists of a group of intracellular tyrosine kinases that transmit signals from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoieses and immune cell function

                Within the signaling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs) which modulate intracellular activity including gene expression; tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs

                These signals are essential in maintaining the inflammatory condition in rheumatoid arthritis (RA); inhibition of JAKs reduces production of and modulates proinflammatory cytokines central to RA

                Absorption

                Bioavailability

                • Xeljanz: 74%

                Minimum plasma concentration

                • Xeljanz: 1.41-3.1 ng/mL
                • Xeljanz XR: 1.07-3.11 ng/mL

                Peak plasma concentration

                • Xeljanz: 42.7-84.7 ng/mL
                • Xeljanz XR: 38.2-83.8 ng/mL

                Peak plasma time

                • Xeljanz or oral solution: 0.5-1 hr
                • Xeljanz XR: 4 hr

                AUC

                • Xeljanz: 263.4-539.6 ng⋅hr/mL
                • Xeljanz XR: 269-596.6 ng⋅hr/mL

                Steady-state reached

                • Xeljanz or oral solution: 24-48 hr
                • Xeljanz XR: 48 hr

                Distribution

                Protein Bound: ~40% (predominately to albumin)

                Vd: 87 L (following IV administration)

                Distributes equally between RBCs and plasma

                Metabolism

                Clearance mechanisms: ~70% hepatic metabolism and 30% renal excretion

                Primarily metabolized by CYP3A4 (accounting for ~53% of total clearance) and by CYP2C19 (accounting for ~17% of total clearance)

                Metabolites: Potency <10% of parent compound

                Elimination

                Renal clearance: 30%

                Excretion: 30% urine

                Half-life

                • Xeljanz or oral solution: 0.8-1 hr
                • Xeljanz XR: 4 hr
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                Administration

                Oral Administration

                May take with or without food

                Extended-release tablets: Swallow whole; do not crush, split, or chew

                Switching from regular tablets to extended-release tablets

                • Patients treated with tofacitinib 5 mg BID may switch to tofacitinib ER 11 mg qDay the day following the last dose of tofacitinib 5 mg

                • Patients treated with tofacitinib 10 mg BID may switch to tofacitinib 22 mg qDay the day following the last dose of tofacitinib 10 mg

                Storage

                Xeljanz or Xeljanz ER: Store at 20-25ºC (68-77ºF)

                Oral solution

                • Store at room temperature 20-25ºC (68-77ºF) in the original bottle and carton to protect from light
                • Safely throw away solution that is out of date or no longer needed
                • Use within 60 days of opening bottle; discard remaining oral solution after 60 days
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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Xeljanz oral
                -
                10 mg tablet
                Xeljanz oral
                -
                5 mg tablet
                Xeljanz XR oral
                -
                11 mg tablet

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                Patient Education
                tofacitinib oral

                TOFACITINIB EXTENDED-RELEASE - ORAL

                (TOE-fa-SYE-ti-nib)

                COMMON BRAND NAME(S): Xeljanz XR

                WARNING: Tofacitinib may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. The most common serious infections include pneumonia, skin infections, shingles, a certain bowel disease (diverticulitis), swelling of the appendix (appendicitis), and urinary tract infections. The risk for infections may be higher if you also take other drugs that suppress the immune system (such as cyclosporine, tacrolimus). Tell your doctor right away if you have any signs of infection (such as a sore throat that doesn't go away, fever, chills, cough, trouble breathing, painful/frequent urination, non-healing skin sores).You should have a tuberculosis (TB) skin test before and during treatment with this medication. Tell your doctor if you have been near someone with tuberculosis or have lived or traveled in areas where certain fungal infections (such as coccidioidomycosis, histoplasmosis) are common. These areas include the Ohio and Mississippi River valleys and the southwestern United States.Though it is very unlikely to occur, there may be a risk of developing cancer (such as lymphoma, skin cancer, lung cancer) with this medication. Tell your doctor right away if you develop symptoms such as fever or cough that doesn't go away, wheezing, unusual lumps/growths, unexplained weight loss, night sweats, change in appearance or size of moles, or unusual skin changes.Tofacitinib may cause serious (possibly fatal) side effects, including heart problems and blood clots. These side effects occurred more often in people who were 50 years of age or older and who had at least one risk factor for heart disease (such as high blood pressure, diabetes, previous blood clots, high cholesterol, smoking or history of smoking). Before using this medication, tell your doctor or pharmacist if you have any of these conditions or if you have a history of heart disease or stroke. Discuss the risks and benefits of treatment with your doctor. Get medical help right away if you have symptoms such as shortness of breath/rapid breathing, chest/jaw/left arm pain, unusual sweating, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, sudden/severe headaches, trouble speaking, weakness on one side of the body, or sudden vision changes.People with a kidney transplant who are also taking other drugs that suppress the immune system may be at greater risk for developing a certain white blood cell disorder (Epstein Barr Virus-associated post-transplant lymphoproliferative disorder) with this medication. Discuss the risks and benefits of treatment with your doctor.

                USES: Tofacitinib is used to treat psoriatic arthritis and rheumatoid arthritis. It helps to decrease pain/tenderness/swelling in the joints. Tofacitinib is also used to treat a certain bowel disease (ulcerative colitis). It helps to reduce symptoms of ulcerative colitis such as diarrhea, rectal bleeding, and stomach pain.

                HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking tofacitinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily. Swallow the tablets whole. Do not crush, split, or chew the tablets. Doing so can release all of the drug at once, increasing the risk of side effects.The dosage is based on your medical condition, response to treatment, lab tests, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Tell your doctor if your condition does not get better or if it gets worse.

                SIDE EFFECTS: See also Warning section.Headache or diarrhea may occur. If either of these effects lasts or gets worse, tell your doctor or pharmacist promptly.An empty tablet shell may appear in your stool. This effect is harmless because your body has already absorbed the medication.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, such as: unusual tiredness, fast heartbeat, signs of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, such as: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                PRECAUTIONS: See also Warning section.Before taking tofacitinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood/bone marrow problems (such as anemia), cancer, kidney disease, liver disease (such as hepatitis B or C), past/recent/current infections (such as tuberculosis, herpes zoster, HIV infection), other stomach/intestinal/esophagus problems (such as ulcers, diverticulitis, narrowing, difficult/painful swallowing), lung disease.Tofacitinib can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be at greater risk for infections while using this drug.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. Tell your doctor if you are planning pregnancy or become pregnant.It is unknown if this medication passes into breast milk. However, because of the possible risk to the infant, breast-feeding while using this drug and for at least 36 hours after the last dose is not recommended. Consult your doctor before breast-feeding.

                DRUG INTERACTIONS: See also Warning section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Other medications can affect the removal of tofacitinib from your body, which may affect how tofacitinib works. Examples include rifampin, among others.

                OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

                NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver/kidney function, complete blood count, cholesterol levels, skin exams) should be done while you are taking this medication. Keep all medical and lab appointments.

                MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

                STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

                MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

                Information last revised September 2021. Copyright(c) 2021 First Databank, Inc.

                IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.