pexidartinib (Rx)

Brand and Other Names:Turalio
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 200mg

Tenosynovial Giant Cell Tumor

Indicated for adults with tenosynovial giant cell tumor (TGCT) associated with severe morbidity or functional limitations and not amenable to improvement with surgery

400 mg PO BID on an empty stomach until disease progression or unacceptable toxicity

Dosage Modifications

Dose reduction schedule

  • First reduction: 200 mg in AM and 400 mg in PM
  • Second reduction: 200 mg BID
  • Permanently discontinue if unable to tolerate 200 mg BID
  • >3-5x ULN
    • Withhold and monitor liver tests weekly
    • If AST and ALT are ≤3x ULN within 4 weeks, resume at reduced dose
    • If AST or ALT is not ≤3x ULN in 4 weeks, permanently discontinue
  • >5-10x ULN
    • Withhold and monitor liver tests twice weekly
    • If AST and ALT are ≤3x ULN within 4 weeks, resume at reduced dose
    • If AST or ALT are not ≤3x ULN in 4 weeks, permanently discontinue
  • >10x ULN
    • Permanently discontinue
    • Monitor liver tests twice weekly until AST or ALT ≤5x ULN, then weekly until ≤3x ULN

Increase ALP and GGT

  • ALP >2x ULN with GGT >2x ULN
    • Permanently discontinue
    • Monitor liver tests twice weekly until ALP ≤5x ULN, then weekly until ≤2x ULN

Increased bilirubin

  • Total bilirubin (TB) >ULN to <2x ULN or direct bilirubin (DB) >ULN and <1.5x ULN
    • Withhold and monitor liver tests twice weekly
    • If an alternate cause for increased bilirubin confirmed and bilirubin
    • If bilirubin is not
  • TB ≥2x ULN or DB >1.5x ULN
    • Permanently discontinue
    • Monitor liver tests twice weekly until bilirubin ≤ULN

Other severe/intolerable adverse effects or laboratory abnormalities

  • Withhold until improvement or resolution
  • Resume at reduced dose upon improvement or resolution

Coadministration with moderate or strong CYP3A4 inhibitors or UGT inhibitors

  • Avoid coadministration
  • If use is unavoidable, reduce pexidartinib dose
  • Dosage reductions for coadministration with strong CYP3A or UGT inhibitors
    • Planned total daily dose (TDD) of 600 or 800 mg: Modify to 200 mg BID
    • Planned TDD of 400 mg: Modify to 200 mg qDay

Concomitant use of acid-reducing agents

  • Avoid coadministration of proton pump inhibitors (PPIs)
  • Alternatives to PPI
    • Locally acting antacid: Administer pexidartinib at least 2 hr before or after
    • H2-receptor antagonist: Administer pexidartinib at least 2 hr before or 10 hr after

Renal impairment

  • Mild-to-severe (CrCl 15-89 mL/min): 200 mg in AM and 400 mg in evening

Hepatic impairment

  • Mild (total bilirubin [TB] ≤ULN and AST >ULN or TB >1x to 1.5x ULN with any AST): No dosage adjustment required
  • Moderate (TB 1.5x to 3x ULN with any AST; not due to Gilbert’s syndrome): Reduce to 200 mg PO qDay
  • Severe (TB >3x to 10x ULN and any AST): Not studied

Dosing Considerations

Monitor liver tests before initiating and at specified intervals during treatment

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and pexidartinib

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            Contraindicated (1)

            • lonafarnib

              pexidartinib will decrease the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lonafarnib is a sensitive CYP3A4 substrate. Coadministration with strong or moderate CYP3A4 inducers is contraindicated.

            Serious - Use Alternative (171)

            • abametapir

              abametapir will increase the level or effect of pexidartinib 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.

            • acetaminophen

              acetaminophen and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • alfentanil

              pexidartinib will decrease the level or effect of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • allopurinol

              allopurinol and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • amiodarone

              amiodarone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              amiodarone will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • amobarbital

              amobarbital will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • amoxicillin

              amoxicillin and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • apalutamide

              apalutamide will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • aprepitant

              aprepitant will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • atazanavir

              atazanavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              atazanavir will increase the level or effect of pexidartinib by Other (see comment). Avoid or Use Alternate Drug. Pexdartinib is a UGTA4 substrate. Reduce pexdartinib dose if concomitant use of UGT inhibitors cannot be avoided (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • auranofin

              auranofin and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • azathioprine

              azathioprine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • bicalutamide

              bicalutamide will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • bosentan

              bosentan will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • busulfan

              busulfan and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • butabarbital

              butabarbital will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • butalbital

              butalbital will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • carbamazepine

              carbamazepine will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              carbamazepine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              pexidartinib will decrease the level or effect of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • ceritinib

              ceritinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • chloramphenicol

              chloramphenicol will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • chlorpromazine

              chlorpromazine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • cimetidine

              cimetidine will increase the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Separate pexidartinib by 2 hr before or 10 hr after taking an H2-antagonist.

            • clarithromycin

              clarithromycin will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • clavulanate

              clavulanate and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • clozapine

              clozapine will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • cobicistat

              cobicistat will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • conivaptan

              conivaptan will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • crizotinib

              crizotinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • cyclosporine

              cyclosporine will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              pexidartinib will decrease the level or effect of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • dabrafenib

              dabrafenib will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • danazol

              danazol and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • dantrolene

              dantrolene and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • darunavir

              darunavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • desipramine

              desipramine will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • dexlansoprazole

              dexlansoprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • diclofenac

              diclofenac and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • didanosine

              didanosine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • dienogest/estradiol valerate

              dienogest/estradiol valerate and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • dihydroergotamine

              pexidartinib will decrease the level or effect of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • diltiazem

              diltiazem will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • disopyramide

              pexidartinib will decrease the level or effect of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • disulfiram

              disulfiram and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • doxycycline

              doxycycline will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • dronedarone

              dronedarone will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • efavirenz

              efavirenz will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              efavirenz and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • encorafenib

              encorafenib, pexidartinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 substrate) with encorafenib (a CYP3A4 inducer and inhibitor) may increase or decrease plasma levels or effects of pexidartinib.

            • enzalutamide

              enzalutamide will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ergotamine

              pexidartinib will decrease the level or effect of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • erythromycin base

              erythromycin base and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              erythromycin base will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              erythromycin ethylsuccinate will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • erythromycin lactobionate

              erythromycin lactobionate and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              erythromycin lactobionate will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • erythromycin stearate

              erythromycin stearate and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              erythromycin stearate will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • esomeprazole

              esomeprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • ethosuximide

              pexidartinib will decrease the level or effect of ethosuximide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • etravirine

              etravirine will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • everolimus

              pexidartinib will decrease the level or effect of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • famotidine

              famotidine will increase the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Separate pexidartinib by 2 hr before or 10 hr after taking an H2-antagonist.

            • fedratinib

              fedratinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • fentanyl

              pexidartinib will decrease the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • fexinidazole

              fexinidazole will increase the level or effect of pexidartinib 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.

            • finerenone

              pexidartinib will decrease the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • floxuridine

              floxuridine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • fluconazole

              fluconazole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • fluoxymesterone

              fluoxymesterone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • flutamide

              flutamide and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • fluvoxamine

              fluvoxamine will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • fosamprenavir

              fosamprenavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • fostamatinib

              fostamatinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • gemfibrozil

              gemfibrozil will increase the level or effect of pexidartinib by Other (see comment). Avoid or Use Alternate Drug. Pexdartinib is a UGTA4 substrate. Reduce pexdartinib dose if concomitant use of UGT inhibitors cannot be avoided (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • grapefruit

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

            • haloperidol

              haloperidol will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • hydralazine

              hydralazine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • ibuprofen

              ibuprofen and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • idelalisib

              idelalisib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • iloperidone

              iloperidone will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • imatinib

              imatinib and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              imatinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • indinavir

              indinavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              indinavir will increase the level or effect of pexidartinib by Other (see comment). Avoid or Use Alternate Drug. Pexdartinib is a UGTA4 substrate. Reduce pexdartinib dose if concomitant use of UGT inhibitors cannot be avoided (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • infigratinib

              pexidartinib will decrease the level or effect of infigratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • infliximab

              infliximab and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • interferon alfa 2b

              interferon alfa 2b and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • interferon beta 1a

              interferon beta 1a and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • interferon beta 1b

              interferon beta 1b and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • isoniazid

              isoniazid will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              isoniazid and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • itraconazole

              itraconazole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • ivacaftor

              ivacaftor will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • ivosidenib

              ivosidenib will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ketoconazole

              ketoconazole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              ketoconazole will increase the level or effect of pexidartinib by Other (see comment). Avoid or Use Alternate Drug. Pexdartinib is a UGTA4 substrate. Reduce pexdartinib dose if concomitant use of UGT inhibitors cannot be avoided (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              ketoconazole and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • lansoprazole

              lansoprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • lapatinib

              lapatinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • larotrectinib

              larotrectinib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • lefamulin

              pexidartinib will decrease the level or effect of lefamulin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of lefamulin with strong or moderate CYP3A inducers unless the benefit outweighs risks. Monitor for reduced efficacy.

            • letermovir

              letermovir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • levonorgestrel oral

              levonorgestrel oral and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • levonorgestrel oral/ethinylestradiol/ferrous bisglycinate

              levonorgestrel oral/ethinylestradiol/ferrous bisglycinate and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • lopinavir

              lopinavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • lorlatinib

              lorlatinib will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • lumacaftor/ivacaftor

              lumacaftor/ivacaftor will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • methotrexate

              methotrexate and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • methyldopa

              methyldopa and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • methyltestosterone

              methyltestosterone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • metronidazole

              metronidazole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • midazolam

              pexidartinib will decrease the level or effect of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • mifepristone

              mifepristone will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • milk thistle

              milk thistle will increase the level or effect of pexidartinib by Other (see comment). Avoid or Use Alternate Drug. Pexdartinib is a UGTA4 substrate. Reduce pexdartinib dose if concomitant use of UGT inhibitors cannot be avoided (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • minocycline

              minocycline and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • mitotane

              mitotane will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nafcillin

              nafcillin will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nefazodone

              nefazodone will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • nelfinavir

              nelfinavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • netupitant/palonosetron

              netupitant/palonosetron will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • nevirapine

              nevirapine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • nitrofurantoin

              nitrofurantoin and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • nizatidine

              nizatidine will increase the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Separate pexidartinib by 2 hr before or 10 hr after taking an H2-antagonist.

            • omeprazole

              omeprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • oxandrolone

              oxandrolone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • oxymetholone

              oxymetholone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • pantoprazole

              pantoprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • peginterferon alfa 2a

              peginterferon alfa 2a and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • peginterferon alfa 2b

              peginterferon alfa 2b and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • peginterferon beta-1a

              peginterferon beta-1a and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • pentobarbital

              pentobarbital will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • phenobarbital

              phenobarbital will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • phenytoin

              phenytoin will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              phenytoin and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • pimozide

              pexidartinib will decrease the level or effect of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • posaconazole

              posaconazole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • primidone

              primidone will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • propylthiouracil

              propylthiouracil and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • pyrazinamide

              pyrazinamide and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • quinidine

              quinidine and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

              pexidartinib will decrease the level or effect of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • quinine

              pexidartinib will decrease the level or effect of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • quinupristin/dalfopristin

              quinupristin/dalfopristin will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • rabeprazole

              rabeprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • ribociclib

              ribociclib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • rifabutin

              rifabutin will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifampin

              rifampin will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

              rifampin and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • rifapentine

              rifapentine will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ritonavir

              ritonavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • saquinavir

              saquinavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • schisandra

              schisandra will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • secobarbital

              secobarbital will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • sertraline

              sertraline will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • simvastatin

              simvastatin and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • sirolimus

              pexidartinib will decrease the level or effect of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • St John's Wort

              St John's Wort will decrease the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • stiripentol

              stiripentol, pexidartinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 substrate) with stiripentol (a CYP3A4 inducer and inhibitor) may increase or decrease plasma levels or effects of pexidartinib.

            • sulfadiazine

              sulfadiazine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • sulfamethoxazole

              sulfamethoxazole and pexidartinib both increase inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • sulfasalazine

              sulfasalazine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • sulfisoxazole

              sulfisoxazole and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • sulindac

              sulindac and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • tacrolimus

              pexidartinib will decrease the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • tegaserod

              tegaserod and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • testosterone

              testosterone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • testosterone buccal system

              testosterone buccal system and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • testosterone intranasal

              testosterone intranasal and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • testosterone topical

              testosterone topical and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • tetracycline

              tetracycline will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • thioguanine

              thioguanine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • ticlopidine

              ticlopidine and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • tipranavir

              tipranavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • triazolam

              pexidartinib will decrease the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pexidartinib (a CYP3A4 inducer) with sensitive CYP3A substrates may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling.

            • tucatinib

              tucatinib will increase the level or effect of pexidartinib 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.

            • valerian

              valerian will increase the level or effect of pexidartinib by Other (see comment). Avoid or Use Alternate Drug. Pexdartinib is a UGTA4 substrate. Reduce pexdartinib dose if concomitant use of UGT inhibitors cannot be avoided (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • valproic acid

              valproic acid and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • verapamil

              verapamil will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • vitamin A

              vitamin A and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • vitamin D

              vitamin D and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • voclosporin

              pexidartinib will decrease the level or effect of voclosporin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • voriconazole

              voriconazole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            • voxelotor

              voxelotor will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.

            Monitor Closely (19)

            • aluminum hydroxide

              aluminum hydroxide will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • aluminum hydroxide/magnesium carbonate

              aluminum hydroxide/magnesium carbonate will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • aluminum hydroxide/magnesium trisilicate

              aluminum hydroxide/magnesium trisilicate will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • aspirin/citric acid/sodium bicarbonate

              aspirin/citric acid/sodium bicarbonate will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • atogepant

              pexidartinib will decrease the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Recommended atogepant dosage with concomitant use of strong or moderate CYP3A4 inducers is 30 mg or 60 mg qDay.

            • belumosudil

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

            • calcium carbonate

              calcium carbonate will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • cenobamate

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

            • citric acid/sodium bicarbonate

              citric acid/sodium bicarbonate will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • elagolix

              elagolix decreases levels of pexidartinib 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.

            • isavuconazonium sulfate

              pexidartinib will decrease the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of pexidartinib 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.

            • magnesium hydroxide

              magnesium hydroxide will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • magnesium oxide

              magnesium oxide will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • rucaparib

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

            • simethicone

              simethicone will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Separate pexidartinib by 2 hr before or after taking a locally-acting antacid.

            • siponimod

              siponimod and pexidartinib 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.

            • tazemetostat

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

            • tivozanib

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

            Minor (0)

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              Adverse Effects

              All grades of severity listed unless otherwise indicated

              >10%

              Increased LDH (92%)

              Hair color changes (67%)

              Fatigue (64%)

              Increased AST, Grade 1 (61%)

              Increased cholesterol (44%)

              Decreased neutrophils (44%)

              Decreased lymphocytes (38%)

              Increased ALT (31%)

              Increased ALP (31%)

              Eye edema (30%)

              Decreased hemoglobin (30%)

              Rash (28%)

              Dysgeusia (26%)

              Peripheral edema (20%)

              Vomiting (20%)

              Pruritus (18%)

              Decreased appetite (16%)

              Decreased platelets (15%)

              Increased AST, Grade 2 (15%)

              Hypertension (15%)

              Increased ALT, Grade 2 (13%)

              Constipation (12%)

              Blurred vision (>10%)

              >10% (Grade ≥3)

              Increased ALT (20%)

              Increased AST (12%)

              1-10%

              Neuropathy (10%)

              Photophobia (<10%)

              Diplopia (<10%)

              Reduced visual acuity (<10%)

              Dry mouth (<10%)

              Stomatitis (<10%)

              Mouth ulceration (<10%)

              Pyrexia (<10%)

              Cholangitis (<10%)

              Hepatotoxicity (<10%)

              Liver disorder (<10%)

              Cognitive disorders (eg, memory impairment, amnesia, confusional state, disturbance in attention, attention-deficit/hyperactivity disorder) (<10%)

              Alopecia (<10%)

              Skin pigment changes (hypopigmentation, depigmentation, discoloration, hyperpigmentation) (<10%)

              Increased cholesterol (4.9%)

              Decreased phosphate (3.3%)

              Increased ALP, Grade 2 (3.3%)

              Increased bilirubin, Grade 1-2 (3.3%)

              1-10% (Grade ≥3)

              Hypertension (4.9%)

              Increased ALP (4.9%)

              Decreased neutrophils (3.3%)

              Increased bilirubin (3.3%)

              Rash (1.6%)

              Eye edema (1.6%)

              Vomiting (1.6%)

              Decreased lymphocytes (1.6%)

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              Warnings

              Black Box Warnings

              Hepatotoxicity

              • Serious and potentially fatal liver injury may occur
              • Monitor liver tests before initiating treatment and periodically during treatment
              • Withhold and dose reduce or permanently discontinue based on severity of hepatotoxicity
              • Available only through a restricted program called the Turalio Risk Evaluation and Mitigation Strategy (REMS)

              Contraindications

              None

              Cautions

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

              Hepatoxicity

              • Hepatotoxicity with ductopenia and cholestasis occurred; mechanism of cholestatic hepatotoxicity is unknown and its occurrence cannot be predicted
              • It is unknown whether liver injury occurs in the absence of increased transaminases
              • Administration with food increases drug exposure by 100% and may increase risk of hepatotoxicity
              • Monitor liver tests before initiating treatment, weekly for the first 8 weeks, every 2 weeks for the next month, and every 3 months thereafter

              REMS program

              • Available only through a restricted program under a REMS, owing to the risk of hepatoxicity
              • Requirements of the program include the following:
              • Prescribers must be certified with the program by enrolling and completing training
              • Patients must complete and sign an enrollment form for inclusion in a patient registry
              • Pharmacies must be certified with the program and must only dispense to patients who are authorized to receive pexidartinib
              • Further information is available at www.turalioREMS.com or 1-833-887-2546

              Drug interaction overview

              • Pexidartinib is CYP3A4 and UGT1A4 substrate; also known to cause hepatoxicity
              • Pexidartinib is a moderate CYP3A inducer
              • Hepatotoxic agents
                • Avoid coadministration of pexidartinib with other products known to cause hepatoxicity in patients with increased serum transaminases, total bilirubin, or direct bilirubin (>ULN) or active liver or biliary tract disease, owning to increased risk of hepatoxicity
              • Strong or moderate CYP3A inhibitors or UGT inhibitors
                • Avoid coadministration
                • Coadministration with a strong CYP3A inhibitor increases pexidartinib plasma concentrations and potentially increases the incidence and severity of adverse reactions
                • Reduce pexidartinib dose according to recommendations
              • Strong CYP3A inducers
                • Avoid coadministration
                • Concomitant use of a strong CYP3A inducer with pexidartinib decreases pexidartinib plasma, which may decrease pexidartinib efficacy
              • CYP3A substrates
                • Concomitant use of CYP3A4 substrates with pexidartinib decreases the concentration of CYP3A substrates, which may reduce the efficacy of these substrates
                • Avoid coadministration with hormonal contraceptives
                • Avoid coadministration with CYP3A substrates where minimal concentration changes may lead to serious therapeutic failures; if coadministration unavoidable, increase the CYP3A substrate dosage in accordance with prescribing information
              • Acid-reducing agents
                • Avoid coadministration with proton pump inhibitors (PPIs)
                • Concomitant PPI decreases pexidartinib plasma concentrations, which may decrease pexidartinib efficacy
                • Alternatively, may use locally acting antacid or H2-receptor antagonist
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              Pregnancy & Lactation

              Pregnancy

              Based on findings from animal studies and its mechanism of action, embryofetal harm may occur when administered to a pregnant woman

              Available human data do not establish the presence or absence of major birth defects or miscarriage related to use in pregnant women

              Animal data

              • Oral administration of pexidartinib to pregnant animals during organogenesis resulted in malformations, postimplantation loss, and abortion at maternal exposures that were approximately equal to the human exposure at the 800 mg-dose
              • Advise pregnant women of the potential risk to a fetus

              Pregnancy testing

              • Verify pregnancy status in females of reproductive potential before initiating treatment

              Contraception

              • Females of reproductive potential: Use effective nonhormonal contraception during treatment and for 1 month after final dose; therapy can render hormonal contraceptives ineffective
              • Males with female partners of reproductive potential: Use effective contraception during treatment and for 1 week after final dose

              Infertility

              • Based on findings from animal studies, treatment may impair both male and female fertility

              Lactation

              No data available on presence of pexidartinib or its metabolites in either human or animal milk or its effects on a breastfed child or on milk production

              Advise females not to breastfeed during treatment and for at least 1 week after 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

              Orally bioavailable inhibitor of colony-stimulator factor 1 receptor (CSF1R), a tyrosine kinase receptor; also elicits potential antineoplastic, macrophage checkpoint-inhibitory, and immunomodulating activities

              Targets and binds to CSF1R expressed on monocytes, macrophages, and osteoclasts, and inhibits the binding of the CSF1R ligands colony-stimulating factor-1 and interleukin-34, to CSF1R; this prevents CSF1R activation and CSF1R-mediated signaling in these cells

              The described actions block production of inflammatory mediators by macrophages and monocytes and reduce inflammation, thereby inhibiting immunomodulating activity by macrophages and enhancing T-cell infiltration and antitumor T-cell immune responses, which inhibits tumor cell proliferation

              Absorption

              Peak plasma time: 2.5 hr

              Peak plasma concentration: 8625 ng/mL

              AUC: 77,465 ng h/mL

              Time to steady-state: ~7 days

              Administration with food

              • High-fat meal
                • Increases peak plasma concentration and AUC by 100%
                • Delays peak plasma time by 2.5 hr

              Distribution

              Vd: 187 L

              Protein binding

              • >99%
              • Human serum albumin: 99.9%
              • Alpha-1 acid glycoprotein: 89.9%

              Metabolism

              Primary pathway

              • Oxidation: CYP3A4
              • Glucuronidation: UGT1A4

              N-glucuronide metabolite

              • Major inactive metabolite formed by UGT1A4
              • ~10% higher exposure than pexidartinib after single dose

              Elimination

              Half-life: 26.6 hr

              Clearance: 5.1 L/hr

              Excretion

              • Feces: 65% (44% unchanged)
              • Urine: 27% as metabolites (>/=10% as N-glucuronide)
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              Administration

              Oral Administration

              Administer on empty stomach, at least 1 hr before or 2 hr after a meal or snack

              Swallow capsule whole; do not open, break, or chew

              Missed or vomited dose: Instruct patient to take the next dose at its scheduled time

              Storage

              Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

              Keep containers closed and do not remove desiccant from bottles

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              Images

              No images available for this drug.
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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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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.