Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 40mg

Colorectal Cancer

Indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild type, an anti-EGFR therapy

160 mg (four 40-mg tablets) PO qDay for the first 21 days of each 28-day cycle

Continue treatment until disease progression or unacceptable toxicity

Also see Administration

Gastrointestinal Stromal Tumors

Indicated for the treatment of locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) in patients who have been previously treated with imatinib mesylate and sunitinib

160 mg (four 40-mg tablets) PO qDay for the first 21 days of each 28-day cycle

Continue treatment until disease progression or unacceptable toxicity

Also see Administration

Hepatocellular Carcinoma

Indicated for patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib

160 mg (four 40-mg tablets) PO qDay for the first 21 days of each 28-day cycle

Continue treatment until disease progression or unacceptable toxicity

Also see Administration

Dosage Modifications

Interrupt dose

  • Grade 2 hand-foot skin reaction (HFSR)/palmar-plantar erythrodysesthesia (PPES) that is recurrent or does not improve within 7 days despite dose reduction; interrupt therapy for a minimum of 7 days for Grade 3 HFSR
  • Symptomatic Grade 2 hypertension
  • Any Grade 3 or 4 adverse reaction

Reduce dose to 120 mg/day

  • For the first occurrence of Grade 2 HFSR of any duration
  • After recovery of any Grade 3 or 4 adverse reaction except infection
  • For Grade 3 aspartate aminotransferase (AST)/alanine aminotransferase (ALT) elevation; only resume if the potential benefit outweighs the risk of hepatotoxicity

Reduce dose to 80 mg/day

  • For reoccurrence of Grade 2 HFSR at the 120 mg dose
  • After recovery of any Grade 3 or 4 adverse reactions at the 120 mg dose (except hepatotoxicity or infection)

Discontinue permanently

  • Failure to tolerate 80 mg dose
  • Any occurrence of AST/ALT >20x ULN
  • Any occurrence of AST/ALT >3x ULN with concurrent bilirubin >2x ULN
  • Reoccurrence of AST/ALT >5x ULN despite dose reduction to 120 mg
  • For any Grade 4 adverse reaction; only resume if the potential benefit outweighs the risks

Renal Impairment

  • Mild-to-severe: No dosage adjustment necessary
  • Patients on dialysis: Not studied

Hepatic Impairment

  • Mild (total bilirubin ≤ULN and AST>ULN, or total bilirubin >ULN to ≤1.5x ULN) or moderate (total bilirubin >1.5 to ≤3x ULN and any AST): No dosage adjustment necessary
  • Severe (total bilirubin >3x ULN): Not recommended; not studied

Glioblastoma Multiforme (Orphan)

Orphan designation for glioblastoma multiforme

Orphan sponsor

Bayer HealthCare Pharmaceuticals, Inc; 100 Bayer Boulevard; P.O. Box 915; Whippany, New Jersey 07981

Safety and efficacy not established

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Interactions

Interaction Checker

and regorafenib

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            Contraindicated (41)

            • abametapir

              abametapir will increase the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5

            • atazanavir

              atazanavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • bosentan

              bosentan, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • carbamazepine

              carbamazepine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • clarithromycin

              clarithromycin, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • conivaptan

              conivaptan, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • dabrafenib

              dabrafenib, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • darunavir

              darunavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • dexamethasone

              dexamethasone, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • enzalutamide

              enzalutamide, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • eslicarbazepine acetate

              eslicarbazepine acetate, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • etravirine

              etravirine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • fosamprenavir

              fosamprenavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • fosphenytoin

              fosphenytoin, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • grapefruit

              grapefruit, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • imatinib

              imatinib, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • indinavir

              indinavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • isoniazid

              isoniazid, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • ketoconazole

              ketoconazole, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • lopinavir

              lopinavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • nafcillin

              nafcillin, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • nefazodone

              nefazodone, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • nelfinavir

              nelfinavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • nevirapine

              nevirapine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • nicardipine

              nicardipine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • oxcarbazepine

              oxcarbazepine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • pentobarbital

              pentobarbital, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • phenobarbital

              phenobarbital, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • phenytoin

              phenytoin, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • posaconazole

              posaconazole, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • primidone

              primidone, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • quinidine

              quinidine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • rifabutin

              rifabutin, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • rifampin

              rifampin, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • rifapentine

              rifapentine, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • ritonavir

              ritonavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • saquinavir

              saquinavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • St John's Wort

              St John's Wort, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5.

            • tipranavir

              tipranavir, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            • voriconazole

              voriconazole, regorafenib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5.

            Serious - Use Alternative (16)

            • alpelisib

              regorafenib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

            • apalutamide

              apalutamide will decrease the level or effect of regorafenib 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.

            • chloramphenicol

              chloramphenicol will increase the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • efavirenz

              efavirenz will decrease the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inducers decrease regorafenib levels and increase exposure of the active metabolite M-5

            • fexinidazole

              fexinidazole will increase the level or effect of regorafenib 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.

            • idelalisib

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

            • itraconazole

              itraconazole will increase the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong CYP3A4 inhibitors increase regorafenib levels and decrease exposure of the active metabolites M-2 and M-5. Not recommended during and 2 weeks after itraconazole treatment.

            • ivosidenib

              ivosidenib will decrease the level or effect of regorafenib 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.

            • lonafarnib

              lonafarnib will increase the level or effect of regorafenib 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.

            • mifepristone

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

            • ozanimod

              regorafenib increases toxicity of ozanimod by Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of ozanimod (a BCRP substrate) with BCRP inhibitors increases the exposure of the minor (RP101988, RP101075) and major active metabolites (CC112273, CC1084037) of ozanimod, which may increase the risk of ozanimod adverse reactions. .

            • palifermin

              palifermin increases toxicity of regorafenib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

            • rimegepant

              regorafenib will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of rimegepant (a BCRP substrate) with inhibitors of BCRP.

            • talazoparib

              regorafenib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.

            • tucatinib

              tucatinib will increase the level or effect of regorafenib 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.

            • voxelotor

              voxelotor will increase the level or effect of regorafenib 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 (53)

            • artesunate

              regorafenib will increase the level or effect of artesunate by decreasing metabolism. Use Caution/Monitor. Coadministration may increase active artesunate metabolite (DHA) by inhibiting UGT. Monitor for increased adverse effects.

            • atorvastatin

              regorafenib will increase the level or effect of atorvastatin by Other (see comment). Use Caution/Monitor. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity

            • berotralstat

              regorafenib increases levels of berotralstat by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reduced dose of berotralstat (a BCRP substrate) to 110 mg/day when coadministered with BCRP inhibitors.

            • cenobamate

              cenobamate will decrease the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • chlorothiazide

              regorafenib will increase the level or effect of chlorothiazide by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • cimetidine

              regorafenib will increase the level or effect of cimetidine by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • daunorubicin

              regorafenib will increase the level or effect of daunorubicin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • dichlorphenamide

              dichlorphenamide and regorafenib both decrease serum potassium. Use Caution/Monitor.

            • digoxin

              regorafenib will decrease the level or effect of digoxin by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Chemotherapy may decrease absorption of digoxin; monitor levels and adjust digoxin dose accordingly

            • dipyridamole

              regorafenib will increase the level or effect of dipyridamole by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • doxorubicin

              regorafenib will increase the level or effect of doxorubicin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • doxorubicin liposomal

              regorafenib will increase the level or effect of doxorubicin liposomal by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • duvelisib

              duvelisib will increase the level or effect of regorafenib 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.

              regorafenib will increase the level or effect of duvelisib by Other (see comment). Use Caution/Monitor. Coadministration of duvelisib (a BCRP substrate) with a BCRP transport inhibitor may increase levels or effects of duvelisib.

            • elagolix

              elagolix decreases levels of regorafenib 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, regorafenib. 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.

            • fedratinib

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

            • fluvastatin

              regorafenib will increase the level or effect of fluvastatin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • glecaprevir/pibrentasvir

              regorafenib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.

            • glyburide

              regorafenib will increase the level or effect of glyburide by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • imatinib

              regorafenib will increase the level or effect of imatinib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • irinotecan

              regorafenib will increase the level or effect of irinotecan by decreasing metabolism. Use Caution/Monitor. Regorafenib may inhibit UGT1A1-mediated metabolism of irinotican and its metabolite

              regorafenib will increase the level or effect of irinotecan by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • irinotecan liposomal

              regorafenib will increase the level or effect of irinotecan liposomal by decreasing metabolism. Use Caution/Monitor. Regorafenib may inhibit UGT1A1-mediated metabolism of irinotican and its metabolite

              regorafenib will increase the level or effect of irinotecan liposomal by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • istradefylline

              istradefylline will increase the level or effect of regorafenib 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

              regorafenib will increase the level or effect of lapatinib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • ledipasvir/sofosbuvir

              regorafenib will increase the level or effect of ledipasvir/sofosbuvir by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • leflunomide

              regorafenib will increase the level or effect of leflunomide by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • lenvatinib

              regorafenib will increase the level or effect of lenvatinib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • lorlatinib

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

            • methotrexate

              regorafenib will increase the level or effect of methotrexate by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • mitotane

              mitotane decreases levels of regorafenib 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.

            • mitoxantrone

              regorafenib will increase the level or effect of mitoxantrone by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • nitrofurantoin

              regorafenib will increase the level or effect of nitrofurantoin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • osimertinib

              regorafenib will increase the level or effect of osimertinib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • pantoprazole

              regorafenib will increase the level or effect of pantoprazole by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • pazopanib

              regorafenib will increase the level or effect of pazopanib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • pitavastatin

              regorafenib will increase the level or effect of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • ribociclib

              ribociclib will increase the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • riociguat

              regorafenib will increase the level or effect of riociguat by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • rosuvastatin

              regorafenib will increase the level or effect of rosuvastatin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • rucaparib

              rucaparib will increase the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • selexipag

              regorafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • siponimod

              siponimod and regorafenib 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.

            • sofosbuvir

              regorafenib will increase the level or effect of sofosbuvir by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • sofosbuvir/velpatasvir

              regorafenib will increase the level or effect of sofosbuvir/velpatasvir by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • stiripentol

              stiripentol, regorafenib. 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.

            • sulfasalazine

              regorafenib will increase the level or effect of sulfasalazine by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • tazemetostat

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

            • tecovirimat

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

            • tenofovir AF

              regorafenib will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • tenofovir DF

              regorafenib will increase the level or effect of tenofovir DF by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • topotecan

              regorafenib will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • vemurafenib

              regorafenib will increase the level or effect of vemurafenib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • warfarin

              regorafenib will increase the level or effect of warfarin by anticoagulation. Use Caution/Monitor. Monitor INR more frequently

            Minor (0)

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              Adverse Effects

              All grades of severity are listed unless otherwise indicated

              >10% (Colorectal Cancer)

              Anemia (79%)

              Increased AST (65%)

              Asthenia (64%)

              Proteinuria (60%)

              Hypocalcemia (59%)

              Hypophosphatemia (57%)

              Lymphopenia (54%)

              Decreased appetite and food intake (47%)

              Increased lipase (46%)

              HFSR/PPES (45%)

              Hyperbilirubinemia (45%)

              Increased ALT (45%)

              Diarrhea (43%)

              Thrombocytopenia (41%)

              Mucositis (33%)

              Weight loss (32%)

              Infection (31%)

              Hypophosphatemia, Grade 3 or 4 (31%)

              Hypertension (30%)

              Dysphonia (30%)

              Hyponatremia (30%)

              Pain (29%)

              Fever (28%)

              Rash (26%)

              Hypokalemia (26%)

              Increased amylase (26%)

              Increased INR (24%)

              Hemorrhage (21%)

              Nausea (20%)

              HFSR/PPES, Grade 3 or 4 (17%)

              Asthenia/fatigue, Grade 3 or 4 (15%)

              >10% (GIST)

              HFSR/PPES (67%)

              Pain (60%)

              Hypertension (59%)

              Proteinuria (59%)

              Increased AST (58%)

              Hypophosphatemia (55%)

              Asthenia (52%)

              Diarrhea (47%)

              Mucositis (40%)

              Dysphonia (39%)

              Increased ALT (39%)

              Hyperbilirubinemia (33%)

              Infection (32%)

              Decreased appetite and food intake (31%)

              Rash (30%)

              Lymphopenia (30%)

              Alopecia (24%)

              ever (21%)

              HFSR/PPES, Grade 3 or 4 (22%)

              Hypokalemia (21%)

              Nausea (20%)

              Hypophosphatemia, Grade 3 or 4 (20%)

              Hypothyroidism (18%)

              Vomiting (17%)

              Hypocalcemia (17%)

              Headache (16%)

              Neutropenia (16%)

              Weight loss (14%)

              Increased lipase (14%)

              Muscle spasms (14%)

              Thrombocytopenia (13%)

              Hemorrhage (11%)

              >10% (HCC)

              Increased AST (93%)

              Hyperbilirubinemia (78%)

              Hypophosphatemia (70%)

              Increased ALT (70%)

              Lymphopenia (68%)

              Thrombocytopenia (63%)

              Pain (55%)

              Proteinuria (51%)

              HFSR/PPES (51%)

              Increased INR (44%)

              Asthenia/fatigue (42%)

              Diarrhea (41%)

              Increased lipase (41%)

              Hypophosphatemia, Grade 3 or 4 (31%)

              Hypertension (31%)

              Infection (31%)

              Hypokalemia (31%)

              Decreased appetite and food intake (31%)

              Hypocalcemia (23%)

              Increased amylase (23%)

              Fever (20%)

              Hypothyroidism (18%)

              Hemorrhage (18%)

              Dysphonia (18%)

              Nausea (17%)

              Hypocalcemia (17%)

              Proteinuria, Grade 3 or 4 (17%)

              Headache (16%)

              Hypertension, Grade 3 or 4 (15%)

              Neutropenia (14%)

              Mucositis (13%)

              Vomiting (13%)

              Weight loss (13%)

              Hyperbilirubinemia, Grade 3 or 4 (13%)

              HFSR/PPES, Grade 3 or 4 (12%)

              Increased lipase, Grade 3 or 4 (11%)

              1-10% (Colorectal Cancer)

              Headache (10%)

              Hyperbilirubinemia, Grade 3 or 4 (10%)

              Pain, Grade 3 or 4 (9%)

              Infection, Grade 3 or 4 (9%)

              Increased lipase, Grade 3 or 4 (9%)

              Lymphopenia, Grade 3 or 4 (9%)

              Hypertension, Grade 3 or 4 (8%)

              Diarrhea, Grade 3 or 4 (8%)

              Hypokalemia, Grade 3 or 4 (7%)

              Musculoskeletal stiffness (6%)

              Rash, Grade 3 or 4 (6%)

              Decreased appetite and food intake, Grade 3 or 4 (5%)

              Anemia, Grade 3 or 4 (5%)

              Increased AST/ALT, Grade 3 or 4 (6%)

              Mucositis, Grade 3 or 4 (4%)

              Hypokalemia, Grade 3 or 4 (4%)

              Neutropenia (3%)

              Tremor (2%)

              Hemorrhage, Grade 3 or 4 (2%)

              Fever, Grade 3 or 4 (2%)

              Proteinuria, Grade 3 or 4 (2%)

              Increased amylase, Grade 3 or 4 (2%)

              Neutropenia, Grade 3 or 4 (1%)

              Hypocalcemia, Grade 3 or 4 (1%)

              1-10% (GIST)

              Lymphopenia, Grade 3 or 4 (8%)

              Pain, Grade 3 or 4 (8%)

              Diarrhea, Grade 3 or 4 (8%)

              Rash, Grade 3 or 4 (8%)

              Infection, Grade 3 or 4 (5%)

              Asthenia/fatigue, Grade 3 or 4 (4%)

              Hemorrhage, Grade 3 or 4 (4%)

              Increased AST/ALT, Grade 3 or 4 (3-4%)

              Hyperbilirubinemia, Grade 3 or 4 (3%)

              Proteinuria, Grade 3 or 4 (3%)

              Hypokalemia, Grade 3 or 4 (3%)

              Neutropenia, Grade 3 or 4 (2%)

              Mucositis, Grade 3 or 4 (2%)

              Nausea, Grade 3 or 4 (2%)

              Hypocalcemia, Grade 3 or 4 (2%)

              Thrombocytopenia, Grade 3 or 4 (1%)

              1-10% (HCC)

              Muscle spasms (10%)

              Asthenia/fatigue, Grade 3 or 4 (10%)

              Infection, Grade 3 or 4 (8%)

              Increased ALT, Grade 3 or 4 (6%)

              Hemorrhage, Grade 3 or 4 (5%)

              Thrombocytopenia, Grade 3 or 4 (5%)

              Neutropenia, Grade 3 or 4 (4%)

              Diarrhea, Grade 3 or 4 (3%)

              Diarrhea, Grade 3 or 4 (3%)

              Decreased appetite or food intake (3%)

              Weight loss (2%)

              Mucositis, Grade 3 or 4 (1%)

              <1%

              GIST

              • Decreased appetite and food intake, Grade 3 or 4
              • Vomiting, Grade 3 or 4

              HCC

              • Nausea
              • Vomiting
              • Increased INR

              Colorectal cancer

              • Headache, Grade 3 or 4

              Postmarketing Reports

              Hypersensitivity reactions

              Nephrotic syndrome

              Cardiac failure

              Arterial (including aortic) aneurysms, dissections, and rupture

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              Warnings

              Black Box Warnings

              Hepatotoxicity

              • Severe and sometimes fatal hepatotoxicity observed in clinical trials
              • Monitor hepatic function prior to and during treatment
              • Interrupt and then reduce or discontinue for hepatotoxicity as manifested by elevated liver function tests or hepatocellular necrosis, depending upon severity and persistence
              • Also see Dosage Modifications and Cautions

              Contraindications

              None

              Cautions

              Also see Dosage Modifications

              May cause severe drug-induced liver injury with fatal outcome (see Black Box Warnings); obtain liver function tests (ALT, AST, and bilirubin) before initiation of therapy and monitor at least every 2 weeks during first 2 months of treatment; thereafter, monitor monthly or more frequently as clinically indicated; monitor liver function tests weekly in patients experiencing elevated liver function tests until improvement to less than 3 times the ULN or baseline; temporarily hold and then reduce or permanently discontinue therapy depending on severity and persistence of hepatotoxicity as manifested by elevated liver function tests or hepatocellular necrosis

              Increases risk for hemorrhage; discontinue therapy for severe or life-threatening hemorrhage

              Increased risk of infections reported; most common infections include urinary tract infections, nasopharyngitis, mucocutaneous and systemic fungal infections and pneumonia

              Increases risk for HFSR/PPES and rash; a higher incidence of HFSR reported in Asian patients; interrupt and then reduce or discontinue regorafenib depending on severity and persistence of dermatologic toxicity

              Hypertension may occur, typically during the first treatment cycle; do not initiate therapy unless blood pressure is adequately controlled; monitor blood pressure weekly for first 6 weeks of treatment and then every cycle, or more frequently, as clinically indicated; temporarily or permanently withhold therapy for severe or uncontrolled hypertension

              Myocardial ischemia and infarction observed in clinical trials; withhold regorafenib for new or acute cardiac ischemia/infarction and resume only after resolution of acute ischemic events

              One case report of reversible posterior leukoencephalopathy syndrome (RPLS) reported (1 of 1100 treated patients); discontinue therapy if RPLS occurs

              Discontinue therapy if gastrointestinal perforation or fistula occur

              May impair wound healing (class effect of VEGFR inhibitors); complications can occur in patients who receive drugs that inhibit the VEGF signaling pathway; discontinue at least 2 weeks before scheduled surgery; do not administer for at least 2 weeks following major surgery and until adequate wound healing; safety of resumption of drug after resolution of wound healing complications not established; discontinue therapy in patients with wound dehiscence

              Embryo-fetal toxicity likely if taken while pregnant (see Pregnancy & Lactation)

              Drug interactions overview

              • Strong CYP3A4 inhibitors
                • Coadministration with strong CYP3A4 inhibitors increases regorafenib plasma concentrations, decreased active metabolite (M-2 and M-5) plasma concentrations, and may increase toxicity
                • Avoid concomitant use of regorafenib with strong CYP3A4 inhibitors (eg, clarithromycin, grapefruit juice, itraconazole, ketoconazole, nefazodone, posaconazole, telithromycin, and voriconazole)
              • Breast cancer resistance protein (BCRP) substrates
                • Coadministration with a BCRP substrate increases the BCRP substrate plasma concentrations
                • Closely monitor for signs and symptoms of exposure-related toxicity of the BCRP substrate (eg, methotrexate, fluvastatin, atorvastatin)
                • Consult the concomitant BCRP substrate product information when considering administration of regorafenib
              • UGT substrates
                • Regorafenib competitively inhibits UGT1A9 and UGT1A1 substrates
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              Pregnancy & Lactation

              Pregnancy

              Based on animal studies and mechanism of action, fetal harm may occur when administered to a pregnant woman

              There are no available data on use in pregnant women

              Advise pregnant women of the potential hazard to a fetus

              Animal data

              • Administration of regorafenib was embryolethal and teratogenic in rats and rabbits at exposures lower than human exposures at the recommended dose, with increased incidences of cardiovascular, genitourinary, and skeletal malformations

              Contraception

              • Females: Use effective contraception during treatment and for 2 months following the final dose
              • Males: Advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 2 months following final dose

              Infertility

              • There are no data on the effect on human fertility
              • Results from animal studies indicate that regorafenib can impair male and female fertility

              Lactation

              There are no data on the presence of regorafenib or its metabolites in human milk, the effects of regorafenib on the breastfed infant, or on milk production In rats, regorafenib and its metabolites are excreted in milk

              Because of the potential for serious adverse reactions in breastfed infants from regorafenib, do not breastfeed during treatment and for 2 weeks after the final dose

              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

              Tyrosine kinase inhibitor; shown to inhibit activity of membrane-bound and intracellular kinases involved in normal cellular functions and in pathological processes (eg, oncogenesis, tumor angiogenesis) RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, Trk2A, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl

              Absorption

              Bioavailability: 69-83% (with low fat meal)

              Peak Plasma Time: 4 hr

              Peak Plasma Concentration: 2.5 mcg/mL (single dose); 3.9 mcg/mL (steady-state)

              AUC: 70.4 mcg•h/mL (single dose); 58.3 mcg•h/mL (steady-state)

              Distribution

              Protein Bound: 99.5% (regorafenib); 99.8% (M-2 active metabolite); 99.95% (M-5 active metabolite)

              Undergoes enterohepatic circulation with multiple plasma concentration peaks observed during 24-hr interval

              Metabolism

              Metabolized by CYP3A4 and UGT1A9

              Metabolites (active): M-2 (N-oxide) and M-5 (N-oxide and N-desmethyl), both of them having similar in vitro pharmacological activity and steady-state concentrations as regorafenib

              Elimination

              Half-life: 28 hr (regorafenib); 25 hr (M-2 active metabolite); 51 hr (M-5 active metabolite)

              Excretion: 71% feces; 19% urine (within 12 days of single dose)

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              Administration

              Oral Administration

              Administer orally same time each day

              Swallow table whole with water, do not split, chew, or crush

              Take after a low-fat meal that contains <600 calories and <30% fat

              Do not take 2 doses on the same day to make up for a missed dose from the previous day

              Storage

              Tablets: Store at 25°C (77°F); excursions are permitted from 15-30°C (59-86°F)

              Store tablets in the original bottle and do not remove the desiccant

              Keep the bottle tightly closed after first opening

              Discard any unused tablets 7 weeks after opening the bottle; dispose of unused tablets in accordance with local requirements

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Stivarga oral
              -
              40 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              regorafenib oral

              REGORAFENIB - ORAL

              (RE-goe-RAF-e-nib)

              COMMON BRAND NAME(S): Stivarga

              WARNING: Regorafenib has rarely caused very serious (possibly fatal) liver disease, especially in the first 2 months of treatment. People of Asian descent are at greater risk. Your doctor will monitor your liver function before and during treatment with this medication. Tell your doctor right away if you develop new or worsening symptoms of liver disease, such as nausea/vomiting that doesn't stop, severe stomach/abdominal pain, dark urine, yellowing eyes/skin.

              USES: Regorafenib is used to treat cancer of the colon and rectum. It is also used to treat liver cancer and a certain cancer of the digestive system (gastrointestinal stromal tumor). It works by slowing or stopping the growth of cancer cells.

              HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking regorafenib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with a low-fat meal as directed by your doctor, usually once daily for 21 days, then stopping the medication for 7 days. This is one cycle of treatment. Continue taking the medication this way as directed by your doctor. Swallow the medication whole. Do not crush, chew, or split the tablets.The dosage is based on your medical condition and response to treatment. 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.Take this medication regularly to get the most benefit from it. Remember to take it at the same time each day that you are scheduled to take it.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

              SIDE EFFECTS: See also Warning section.Diarrhea, pain/sores in the mouth/throat, changes in taste, dry mouth, loss of appetite, hair loss, voice changes, weight loss, or muscle stiffness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.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.Treatment with this drug may sometimes cause your hands/feet to develop a skin reaction called hand-foot skin reaction (palmar-plantar erythrodysesthesia). People of Asian descent are at greater risk. Tell your doctor right away if you experience swelling, pain, redness, peeling, blisters, or tingling/burning of the hands/feet. The symptoms can be made worse by heat/pressure on your hands/feet. Avoid prolonged sun exposure, tanning booths, and sunlamps, as well as unnecessary exposure to heat (for example, hot dishwater, long hot baths). Use a sunscreen and wear protective clothing when outdoors. Avoid pressure on elbows, knees, and soles of feet (such as leaning on elbows, kneeling, taking long walks). Wear loose clothing and comfortable shoes. Depending on how severe your hand-foot reaction is, your doctor may give you an additional medication to reduce the symptoms, or stop or delay your regorafenib treatment.This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high. Your doctor may control your blood pressure with medication.Tell your doctor right away if you have any serious side effects, including: slow wound healing, signs of dehydration (such as extreme thirst, dizziness, decreased urination), signs of mineral imbalance (such as muscle cramps/weakness, irregular heartbeat, mental/mood changes), signs of infection (such as fever, chills, persistent sore throat), signs of underactive thyroid (weight gain, cold intolerance, unusual tiredness, slow heartbeat).This medication can cause serious bleeding. Tell your doctor right away if you have any signs of serious bleeding, including: easy bleeding/bruising, severe stomach/abdominal pain, vomit that is bloody or looks like coffee grounds, black/tarry stool, unusual vaginal bleeding, pink/bloody urine, coughing up blood.Get medical help right away if you have any very serious side effects, including: signs of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), sudden/severe back pain, seizure, severe headache, confusion, sudden vision changes, weakness on one side of the body, trouble speaking.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, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.Regorafenib can commonly cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Get medical help right away if you develop any rash.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: Before taking regorafenib, 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: liver problems, high blood pressure, heart disease (such as heart attack, chest pain), bleeding problems (such as bleeding of the stomach/intestines), blood vessel problems (such as an aneurysm or a tear/break in the aorta or other blood vessels), recent major surgery/injury.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Your doctor or dentist may tell you to stop taking regorafenib at least 2 weeks before surgery. This medication may cause wounds to heal more slowly. Follow all instructions about when to stop or restart this medication.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).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Older adults may be at greater risk for high blood pressure while using this drug.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using regorafenib. Regorafenib may harm an unborn baby. Both women and men should ask about reliable forms of birth control while using this medication and for 2 months after stopping treatment. If you or your partner becomes pregnant, talk to your doctor right away about the risks and benefits of this medication.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug and for 2 weeks after stopping treatment is not recommended. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: See also How to Use 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.Some products that may interact with this drug include: irinotecan, other drugs that can cause bleeding/bruising (including antiplatelet drugs such as clopidogrel, NSAIDs such as ibuprofen, "blood thinners" such as warfarin).Aspirin can increase the risk of bleeding when used with this medication. However, if your doctor has directed you to take low-dose aspirin for heart attack or stroke prevention (usually 81-162 milligrams a day), you should continue taking it unless your doctor instructs you otherwise. Ask your doctor or pharmacist for more details.Other medications can affect the removal of regorafenib from your body, which may affect how regorafenib works. Examples include boceprevir, nefazodone, telaprevir, telithromycin, azole antifungals (such as ketoconazole, itraconazole), macrolide antibiotics (such as clarithromycin), HIV protease inhibitors (such as ritonavir, nelfinavir), rifamycins (such as rifabutin, rifampin), St. John's wort, drugs used to treat seizures (such as phenytoin), 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.Laboratory and/or medical tests (such as liver function, complete blood count, blood mineral levels, blood pressure, urine protein test) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

              MISSED DOSE: If you miss a dose and remember on the same day, take it as soon as you remember. If you remember on the next day, 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. Keep the medication in the original bottle with the desiccant to protect against moisture. Do not store in the bathroom. Discard any remaining tablets 7 weeks after opening the bottle. 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.

              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.