Dosing & Uses
Dosage Forms & Strengths
tablet
- 4.5mg
- 9mg
- 13.5mg
Cholangiocarcinoma
Indicated for unresectable locally advanced or metastatic cholangiocarcinoma in previously treated patients with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement
Each cycle is 21 days
13.5 mg PO qDay for 14 consecutive days followed by 7 days off therapy
Continue until disease progression or unacceptable toxicity occurs
Myeloid or Lymphoid Neoplasms
Indicated for relapsed or refractory myeloid/lymphoid neoplasms (MLNs) in adults with fibroblast growth factor receptor 1 (FGFR1) rearrangement
13.5 mg PO qDay
Continue until disease progression or unacceptable toxicity occur
Dosage Modifications
Dose reductions for adverse reactions
-
Cholangiocarcinoma
- First dose reduction: 9 mg qDay for first 14 days of each 21-day cycle
- Second dose reduction: 4.5 mg qDay for first 14 days of each 21-day cycle
- Patients unable to tolerate 4.5 mg qDay: Permanently discontinue
-
MLNs
- First dose reduction: 9 mg qDay
- Second dose reduction: 4.5 mg qDay
- Third dose reduction: 4.5 mg PO qDay for first 14 days of each 21-day cycle
- Permanently discontinue if unable to tolerate 4.5 mg PO qDay for first 14 days of each 21-day cycle
Retinal pigment epithelial detachment (RPED)
- Asymptomatic and stable on serial examination: Continue treatment
-
Symptomatic OR worsening on serial examination
- Withhold; resume at a lower dose if asymptomatic and improved on subsequent examination
- Symptoms persist or examination does not improve: Consider permanent discontinuation based on clinical status
Hyperphosphatemia
- Initiate phosphate lowering therapy and monitor serum phosphate weekly
-
Serum phosphate >7 to ≤10 mg/dL
- Withhold if levels are still ≥7 mg/dL within 2 weeks of starting phosphate lowering therapy
- Resume at the same dose when phosphate levels are <7 mg/dL for first occurrence; resume at a lower dose level for subsequent recurrences
-
Serum phosphate >10 mg/dL
- Withhold if levels are still >10 mg/dL within 1 week of starting phosphate lowering therapy
- Resume at the next lower dose level when phosphate levels are <7 mg/dL
- Permanently discontinue for recurrence of serum phosphate >10 mg/dL following 2 dose reductions
Other adverse reactions
-
Grade 3
- Withhold until resolves to Grade ≤1; resume at next lower dose if resolves within 2 weeks
- Permanently discontinue if unresolved within 2 weeks OR for recurrent Grade 3 after 2 dose reductions
-
Grade 4
- Permanently discontinue
Coadministration with CYP3A inhibitors
- Avoid coadministration
- If use cannot be avoided, reduce dose (ie, 13.5 mg to 9 mg, 9 mg to 4.5 mg)
- If strong or moderate CYP3A inhibitor is discontinued, increase pemigatinib dose (after 3 plasma half-lives of the CYP3A inhibitor) to dose taken before initiating inhibitor
Renal impairment
- Mild or moderate (GFR ≥30 to <89 mL/min/1.73 m2): No dosage adjustment necessary
- End-stage renal disease (eGFR <15 mL/min/1.73 m2) who are receiving intermittent hemodialysis: No dosage adjustment necessary
-
Severe (GFR <30 mL/min/1.73 m2)
- Cholangiocarcinoma: Reduce to 9 mg PO qDay for 14 consecutive days followed by 7 days off therapy for each 21-day cycle
- MLNs: Reduce to 9 mg PO qDay
Hepatic impairment
- Mild or moderate (total bilirubin ≤3x ULN with any AST): No dosage adjustment necessary
-
Severe (total bilirubin >3x ULN with any AST)
- Cholangiocarcinoma: Reduce to 9 mg PO qDay for 14 consecutive days followed by 7 days off therapy for each 21-day cycle
- MLNs: Reduce to 9 mg PO qDay
Dosing Considerations
Verify pregnancy status of females of reproductive potential before initiation
Patient selection
-
Cholangiocarcinoma
- Select based on detection of an FGFR2 fusion or rearrangement
- Information on such FDA-approved test(s) is available at http://www.fda.gov/CompanionDiagnostics
-
MLNs
- Select relapsed or refractory myeloid/lymphoid neoplasms with FGFR1 rearrangement
- No FDA-approved test for detecting FGFR1 rearrangement is availabl
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (91)
- amiodarone
amiodarone will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- amobarbital
amobarbital will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- aprepitant
aprepitant will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- armodafinil
armodafinil will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- atazanavir
atazanavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- bexarotene
bexarotene will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bicalutamide
bicalutamide will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- bosentan
bosentan will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- brigatinib
brigatinib will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butabarbital
butabarbital will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butalbital
butalbital will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ceritinib
ceritinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- chloramphenicol
chloramphenicol will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- clarithromycin
clarithromycin will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- clobazam
clobazam will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cobicistat
cobicistat will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- conivaptan
conivaptan will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- crizotinib
crizotinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- cyclosporine
cyclosporine will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- dabrafenib
dabrafenib will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- darunavir
darunavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- diltiazem
diltiazem will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- doxycycline
doxycycline will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- dronedarone
dronedarone will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- efavirenz
efavirenz will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- elagolix
elagolix will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- encorafenib
encorafenib, pemigatinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pemigatinib (a CYP3A4 substrate) with encorafenib (a CYP3A4 inducer and inhibitor) may increase or decrease plasma levels or effects of pemigatinib.
- enzalutamide
enzalutamide will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin base
erythromycin base will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- erythromycin stearate
erythromycin stearate will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- etravirine
etravirine will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fedratinib
fedratinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- fexinidazole
fexinidazole will increase the level or effect of pemigatinib 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.
- fluconazole
fluconazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors cannot be avoided, reduce selumetinib dosage (refer to selumetinib monograph for further information). After discontinuation of the strong or moderate CYP3A4 inhibitor for 3 elimination half-lives, resume selumetinib dose that was taken before initiating the inhibitor.
- fosamprenavir
fosamprenavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors cannot be avoided, reduce selumetinib dosage (refer to selumetinib monograph for further information). After discontinuation of the strong or moderate CYP3A4 inhibitor for 3 elimination half-lives, resume selumetinib dose that was taken before initiating the inhibitor.
- fosaprepitant
fosaprepitant will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- fosphenytoin
fosphenytoin will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fostamatinib
fostamatinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- grapefruit
grapefruit will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- haloperidol
haloperidol will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- idelalisib
idelalisib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- iloperidone
iloperidone will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- imatinib
imatinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- indinavir
indinavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- isoniazid
isoniazid will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- itraconazole
itraconazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- ivacaftor
ivacaftor will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- ivosidenib
ivosidenib will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ketoconazole
ketoconazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- lapatinib
lapatinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- larotrectinib
larotrectinib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- letermovir
letermovir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- levoketoconazole
levoketoconazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- lorlatinib
lorlatinib will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- metronidazole
metronidazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- mifepristone
mifepristone will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- mitotane
mitotane will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nafcillin
nafcillin will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nefazodone
nefazodone will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- nelfinavir
nelfinavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- netupitant/palonosetron
netupitant/palonosetron will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- pentobarbital
pentobarbital will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenobarbital
phenobarbital will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenytoin
phenytoin will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- posaconazole
posaconazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- primidone
primidone will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- ribociclib
ribociclib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- rifabutin
rifabutin will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifapentine
rifapentine will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ritonavir
ritonavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- saquinavir
saquinavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- schisandra
schisandra will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- secobarbital
secobarbital will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sertraline
sertraline will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- St John's Wort
St John's Wort will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- stiripentol
stiripentol, pemigatinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of pemigatinib (a CYP3A4 substrate) with stiripentol (a CYP3A4 inducer and inhibitor) may increase or decrease plasma levels or effects of pemigatinib.
- telotristat ethyl
telotristat ethyl will decrease the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tetracycline
tetracycline will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- tipranavir
tipranavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- tucatinib
tucatinib will increase the level or effect of pemigatinib 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.
- verapamil
verapamil will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- voriconazole
voriconazole will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- voxelotor
voxelotor will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
Monitor Closely (2)
- lenacapavir
lenacapavir will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of pemigatinib with moderate CYP3A4 inhibitors. If unavoiable, reduce pemigatinib dose as the following: for 13.5 mg /day-dose for the first 14 days of each cycle--decrease pemigatinib dose to 9 mg; 9-mg/day-dose for the first 14 days of each cycle--decrease the pemigatinib dose to 4.5 mg. After discontinuing the inhibitor for 3-5 half-lives, resume the pemigatinib dose used before starting the inhibitor.
- rucaparib
rucaparib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
Minor (0)
Adverse Effects
>10% (Cholangiocarcinoma)
All grades
- Increased phosphate (94%)
- Decreased phosphate (68%)
- Hyperphosphatemia (60%)
- Alopecia (49%)
- Diarrhea (47%)
- Nail toxicity (43%)
- Increased AST/ALT (43%)
- Increased calcium (43%)
- Decreased hemoglobin (43%)
- Fatigue (42%)
- Increased alkaline phosphatase (41%)
- Increased creatinine (41%)
- Nausea (40%)
- Dysgeusia (40%)
- Decreased sodium (39%)
- Increased glucose (36%)
- Decreased lymphocytes (36%)
- Constipation (35%)
- Stomatitis (35%)
- Dry eye (35%)
- Dry mouth (34%)
- Decreased albumin (34%)
- Decreased appetite (33%)
- Increased urate (30%)
- Decreased platelets (28%)
- Increased leukocytes (27%)
- Vomiting (27%)
- Increased bilirubin (26%)
- Decreased potassium (26%)
- Arthralgia (25%)
- Hypophosphatemia (23%)
- Abdominal pain (23%)
- Dry skin (20%)
- Back pain (20%)
- Pain in extremity (19%)
- Decreased leukocytes (18%)
- Peripheral edema (18%)
- Decreased calcium (17%)
- Headache (16%)
- Urinary tract infection (16%)
- Weight loss (16%)
- Dehydration (15%)
- Palmoplantar erythrodysesthesia syndrome (15%)
- Increased potassium (12%)
- Decreased glucose (11%)
Grade ≥3
- Decreased phosphate (38%)
- Hypophosphatemia (12%)
- Decreased sodium (12%)
- Increased alkaline phosphatase (11%)
>10% (MLNs)
Increased phosphate (97%)
Hyperphosphatemia (74%)
Decreased lymphocytes (65%)
Decreased leukocytes (65%)
Nail toxicity (62%)
Increased alkaline phosphatase (62%)
Alopecia (59%)
Stomatitis (53%)
Decreased hemoglobin (53%)
Diarrhea (50%)
Dry eye (50%)
Increased ALT (50%)
Increased AST (47%)
Decreased neutrophils (45%)
Fatigue (44%)
Increased creatinine (44%)
Decreased phosphate (41%)
Decreased sodium (41%)
Rash (35%)
Abdominal pain (35%)
Anemia (35%)
Increased glucose (33%)
Constipation (32%)
Dry mouth (32%)
Epistaxis (29%)
Retinal pigment epithelial detachment (26%)
Pain in extremity (26%)
Decreased calcium (26%)
Increased calcium (26%)
Decreased phosphate, Grade 3 or 4 (26%)
Decreased appetite (24%)
Dyspepsia (24%)
Dry skin (24%)
Back pain (24%)
Decreased potassium (24%)
Increased bilirubin (21%)
Nail toxicity, Grade 3 or 4 (21%)
Nausea (21%)
Vision blued (21%)
Peripheral edema (21%)
Dizziness (21%)
Palmoplantar erythrodysesthesia (18%)
Trichiasis (18%)
Pyrexia (18%)
Anemia, Grade 3 or 4 (18%)
Decreased lymphocyte, Grade 3 or 4 (16%)
Stomatitis, Grade 3 or 4 (15%)
Decreased leukocytes, Grade 3 or 4 (15%)
Decreased platelets, Grade 3 or 4 (15%)
Pain in extremity, Grade 3 or 4 (12%)
Decreased neutrophils, Grade 3 or 4 (12%)
Increased ALT, Grade 3 or 4 (12%)
1-10% (Cholangiocarcinoma)
Grade ≥3
- Increased urate (10%)
- Decreased lymphocytes (8%)
- Decreased hemoglobin (6%)
- Increased bilirubin (6%)
- Increased AST (6%)
- Arthralgia (6%)
- Decreased potassium (5%)
- Stomatitis (5%)
- Abdominal pain (4.8%)
- Fatigue (4.8%)
- Increased calcium (4.1%)
- Increased ALT (4.1%)
- Palmoplantar erythrodysesthesia syndrome (4.1%)
- Decreased platelets (3.4%)
- Dehydration (3.4%)
- Decreased calcium (2.7%)
- Diarrhea (2.7%)
- Back pain (2.7%)
- Urinary tract infection (2.7%)
- Increased potassium (2.1%)
- Nail toxicity (2.1%)
- Pain in extremity (2.1%)
- Weight loss (2.1%)
- Decreased leukocytes (1.4%)
- Increased creatinine (1.4%)
- Decreased glucose (1.4%)
- Decreased appetite (1.4%)
- Vomiting (1.4%)
1-10% (MLNs)
Palmoplantar erythrodysesthesia, Grade 3 or 4 (9%)
Fatigue, Grade 3 or 4 (9%)
Dizziness, Grade 3 or 4 (9%)
Decreased hemoglobin, Grade 3 or 4 (9%)
Decreased sodium, Grade 3 or 4 (9%)
Increased AST, Grade 3 or 4 (9%)
Increased alkaline phosphate, Grade 3 or 4 (9%)
Decreased appetite, Grade 3 or 4 (6%)
Rash, Grade 3 or 4 (6%)
Dry eye, Grade 3 or 4 (6%)
Increased glucose, Grade 3 or 4 (3%)
Hyperphosphatemia, Grade 3 or 4 (2.9%)
Diarrhea, Grade 3 or 4 (2.9%)
Abdominal pain, Grade 3 or 4 (2.9%)
Constipation, Grade 3 or 4 (2.9%)
Vision blurred, Grade 3 or 4 (2.9%)
Trichiasis, Grade 3 or 4 (2.9%)
Pyrexia, Grade 3 or 4 (2.9%)
Decreased calcium, Grade 3 or 4 (2.9%)
Increased calcium, Grade 3 or 4 (2.9%)
Decreased potassium, Grade 3 or 4 (2.9%)
Increased phosphate, Grade 3 or 4 (2.9%)
<1% (Cholangiocarcinoma)
Grade ≥3
- Increased leukocytes (0.7%)
- Increased glucose (0.7%)
- Dry skin (0.7%)
- Constipation (0.7%)
- Peripheral edema (0.7%)
- Dry eye (0.7%)
Warnings
Contraindications
None
Cautions
May cause RPED; symptoms include blurred vision, visual floaters, or photopsia; perform ophthalmological examination including optical coherence tomography before initiation, every 2 months for the first 6 months of therapy, and every 3 months thereafter, and, urgently at any time for visual symptoms
Hyperphosphatemia reported; can cause hyperphosphatemia leading to soft tissue mineralization, cutaneous calcification, calcinosis, and nonuremic calciphylaxis; monitor for hyperphosphatemia and initiate a low phosphate diet when serum phosphate level is >5.5 mg/dL
Can cause fetal harm
Drug interaction overview
CYP3A4 substrate
Also inhibits P-glycoprotein (P-gp), OCT2, and MATE1 in vitro; no clinically significant difference in glucose levels were observed when coadministered with metformin (OCT2/MATE1 substrate)
Strong or moderate CYP3A inducers
- Avoid coadministration
- Strong or moderate CYP3A inducers decrease pemigatinib plasma concentrations, which may reduce the efficacy of pemigatinib
Strong and moderate CYP3A4 inhibitors
- Avoid coadministration; reduce pemigatinib dose, if concomitant use cannot be avoided
- Strong or moderate CYP3A inhibitors increase pemigatinib plasma concentrations, which may increase the risk and severity of adverse reactions
Pregnancy & Lactation
Pregnancy
Based on animal data and its mechanism of action, fetal harm or loss of pregnancy may occur when administered to a pregnant females
No data available on use in pregnant females
Verify pregnancy status of females of reproductive potential before initiation
Contraception
- Females of reproductive potential or males with female partners of reproductive potential: Use effective contraception during treatment and for at least 1 week after final dose
Animal data
- Oral administration to pregnant rats during organogenesis at maternal plasma exposures below the human exposure at the 13.5-mg dose resulted in fetal malformations, fetal growth retardation, and embryofetal death
- Advise pregnant women of the potential risk to a fetus
Lactation
No data available on the presence of pemigatinib or its metabolites in human milk or their effects on either the breastfed child or on milk production
Advise females not to breastfeed during treatment and for 1 week after the final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Orally bioavailable inhibitor of the FGFR types 1, 2, and 3 (FGFR1/2/3)
Pemigatinib inhibits FGFR 1/2/3 phosphorylation and signaling, and decreases cell viability in cancer cell lines with activating FGFR amplifications and fusions
Absorption
Steady-state reached within 4 days following repeated once-daily dosing
Peak plasma time: 1.13 hr
Distribution
Protein bound: 90.6%
Vd: 235 L
Metabolism
Primarily metabolized by CYP3A4
Elimination
Half-life: 15.4 hr
Clearance: 10.6 L/hr
Excretion: Feces (82.4% [1.4% unchanged]); urine (12.6% [1% unchanged])
Administration
Oral Administration
Take with or without food at around the same time every day
Swallow tablet whole; do not crush, chew, split, or dissolve tablet
Missed dose by ≥4 hr or vomited dose: Resume dosing at next scheduled dose
Storage
Store at room temperature, 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Images
Formulary
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.
