Dosing & Uses
Dosage Forms & Strengths
capsule
- 125mg
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
250 mg PO BID with low-fat meal (~11-14 g total fat); continue until disease progression or unacceptable toxicity
Taking with high-fat meal (~55-65 g total fat) increases pexidartinib concentrations and may increase risk of adverse reactions, including hepatotoxicity
Dosage Modifications
Dose reduction schedule
- First reduction: 125 mg in AM and 250 mg in PM
- Second reduction: 125 mg BID
- Permanently discontinue if unable to tolerate 125 mg BID
Increased ALT and/or AST
-
>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
- 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 unavoidable, reduce pexidartinib dose
-
Dosage reductions for coadministration with strong CYP3A or UGT inhibitors
- Taking 500 mg/day (250 mg BID): Reduce to 125 mg BID
- Taking 375 mg/day (125 mg qAM and 250 mg qPM): Reduce to 125 mg BID
- Taking 250 mg/day (125 mg BID): Reduce to 125 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): 125 mg in AM and 250 mg in evening
Hepatic impairment
- Mild (total bilirubin [TB] ≤ULN and AST ≥ULN or TB 1-1.5x ULN): No dosage adjustment required
- Moderate (TB 1.5-3x ULN with any AST; not due to Gilbert’s syndrome): Reduce to 125 mg PO qDay
- Severe (TB 3-10x ULN and any AST): Not studied
Dosing Considerations
Monitor liver tests before initiating and at specified intervals during treatment
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (3)
- 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.
- mavacamten
pexidartinib will decrease the level or effect of mavacamten by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- pacritinib
pexidartinib will decrease the level or effect of pacritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
Serious - Use Alternative (180)
- 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.
- 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.
- daridorexant
pexidartinib will decrease the level or effect of daridorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- 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.
- 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. - elacestrant
pexidartinib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- 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.
- fosaprepitant
fosaprepitant 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.
- ganaxolone
pexidartinib will decrease the level or effect of ganaxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of ganaxolone with moderate or strong CYP3A4 inducers. If coadministration unavoidable, consider increasing ganaxolone dose; however, do not exceed maximum daily dose for weight.
- 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
pexidartinib will decrease the level or effect of larotrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- 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.
- lenacapavir
pexidartinib will decrease the level or effect of lenacapavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of lenacapavir with moderate CYP3A4 inducers.
lenacapavir will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - leniolisib
pexidartinib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- 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.
- levoketoconazole
levoketoconazole 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.
levoketoconazole 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.
levoketoconazole 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. - 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.
- lumateperone
pexidartinib will decrease the level or effect of lumateperone 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.
- olutasidenib
pexidartinib will decrease the level or effect of olutasidenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong or moderate CYP3A inducers decrease olutasidenib (a CYP3A4 substrate) plasma concentrations and efficacy.
- omaveloxolone
pexidartinib will decrease the level or effect of omaveloxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- 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.
- vonoprazan
pexidartinib will decrease the level or effect of vonoprazan 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 (21)
- 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.
- warfarin
pexidartinib will decrease the level or effect of warfarin by Other (see comment). Use Caution/Monitor. Warfarin's less potent R-enantiomer is metabolized in part by CYP3A4 (and also CYP1A2 and CYP2C19). Monitor INR more frequently if coadministered with inducers of these isoenzymes and adjust warfarin dose if needed.
- zanubrutinib
pexidartinib will decrease the level or effect of zanubrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of zanubrutinib (a CYP3A4 substrate) with moderate CYP3A4 inhibitors. If unavoidable, increase zanubrutinib dose to 320 mg PO BID. After discontinuing the CYP3A4 inhibitor, resume previous dose of zanubrutinib.
Minor (3)
- acetazolamide
acetazolamide will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
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%)
Postmarketing Reports
Blood creatine phosphokinase increased
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
-
Risks associated with high-fat meal
- Taking with high-fat meal increases pexidartinib concentrations, which may increase incidence and severity of adverse reactions, including hepatotoxicity
- Instruct patients to take drug with a low-fat meal
- Consider referring patients to a dietician as deemed necessary
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
- Substrate of CYP3A4 and UGT1A4; also known to cause hepatoxicity
- 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
- Strong CYP3A inhibitors increase pexidartinib plasma concentrations and potentially increases the incidence and severity of adverse reactions
- Reduce pexidartinib dose according to recommendations
-
Strong CYP3A inducers
- Avoid coadministration
- Strong CYP3A inducers decrease pexidartinib plasma levels, which may decrease pexidartinib efficacy
-
CYP3A substrates
- 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)
- PPIs decrease pexidartinib plasma concentrations, which may decrease pexidartinib efficacy
- Alternatively, may use locally-acting antacid or H2-receptor antagonist
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.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)
Administration
Oral Administration
Administer on empty stomach, at least 1 hr before or 2 hr after a meal or snack
Administer with low-fat meal (~11-14 g total fat); high-fat meal (~55-65 g total fat) increases pexidartinib concentrations and risk for adverse effects
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
Images
Formulary
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