Dosing & Uses
Dosage Forms & Strengths
capsule
- 40mg
Non-Small Cell Lung Cancer
Indicated for locally advanced or metastatic non–small cell lung cancer (NSCLC) in adults with epidermal growth factor receptor (EGFR) exon 20 insertion mutations and whose disease has progressed on or after platinum-based chemotherapy
160 mg PO qDay
Continue until disease progression or unacceptable toxicity
Dosage Modifications
Dose reductions for adverse reactions
- First dose reduction: 120 mg PO qDay
- Second dose reduction: 80 mg PO qDay
QT (QTc) prolongations and torsades de pointes
-
Grade 2 (QTc interval 481-500 msec)
- First occurrence: Withhold until Grade ≤1 or baseline; upon recovery, resume at same dose
- Recurrence: Withhold until Grade ≤1 or baseline; upon recovery, resume at next lower dose or permanently discontinue
-
Grade 3 (QTc interval ≥501 msec or QTc interval increases >60 msec from baseline)
- First occurrence: Withhold until Grade ≤1 or baseline; upon recovery, resume at next lower dose or permanently discontinue
- Recurrence: Permanently discontinue
- Grade 4 (torsades de pointes; polymorphic ventricular tachycardia; signs/symptoms of serious arrhythmia): Permanently discontinue
Interstitial lung disease (ILD)/pneumonitis
- Any grade: Withhold if ILD/pneumonitis is suspected
- Permanently discontinue if ILD/pneumonitis confirmed
Decreased ejection fraction (EF) or heart failure (HF)
-
Grade 2 decreased EF
- Withhold until Grade ≤1 or baseline
- If recovered to baseline within 2 weeks, resume at same dose or next lower dose
- If not recovered to baseline within 2 weeks, permanently discontinue
- Grade 2 HF or Grade ≥3 EF: Permanently discontinue
Diarrhea
- Intolerable or recurrent Grade 2 or Grade 3: Withhold until Grade ≤1 or baseline; resume at same dose or next lower dose
-
Grade 4
- First occurrence: Withhold until Grade ≤1 or baseline; resume at next lower dose
- Recurrence: Permanently discontinue
Increased amylase or lipase
-
Grade 3
- Withhold until Grade ≤1
- Grade 3 without signs or symptoms: Resume at same dose or next lower dose
- Grade 3 with signs or symptoms: Resume at next lower dose
- If not recovered to Grade ≤1 within 2 weeks, permanently discontinue
-
Grade 4 (1st occurrence)
- Withhold until Grade ≤1
- Resume at next lower dose if recovery occurs within 2 weeks
- Permanently discontinue if not recovered within 2 weeks
-
Grade 4 (recurrence)
- Permanently discontinue
Other adverse reactions
- Intolerable or recurrent Grade 2 or Grade 3: Withhold until Grade ≤1 or baseline; resume at same dose or next lower dose
-
Grade 4
- First occurrence: Withhold until Grade ≤1 or baseline; resume at the next lower dose if recovery occurs within 2 weeks
- Permanently discontinue if no recovery occurs within 2 weeks
- Recurrence: Permanently discontinue
Coadministration of moderate or strong CYP3A4 inhibitors
- Avoid coadministration
- If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80mg, 120 to 60 mg, or 80 to 40 mg); closely monitor QTc interval
- Once moderate CYP3A4 inhibitor has been discontinued for 3-5 half-lives, resume at dose taken before initiating moderate CYP3A4 inhibitor
Renal impairment
- Mild-to-moderate (eGFR 30-89 mL/min/1.73 m2): No dosage adjustment necessary
- Severe (eGFR <30 mL/min/1.73 m2): No recommended dosage established
Hepatic impairment
- Mild-to-moderate (total bilirubin [TB] <3x ULN and any AST): No dosage adjustment necessary
- Severe (TB >3x ULN and any AST): No recommended dosage established
Dosing Considerations
Verify pregnancy status in females of reproductive potential
Patient selection
- Select patients based on presence of EGFR exon 20 insertion mutations
- Information on FDA approved tests is available at: http://www.fda.gov/CompanionDiagnostic
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- mavacamten
mobocertinib will decrease the level or effect of mavacamten by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
Serious - Use Alternative (240)
- abametapir
abametapir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- adagrasib
adagrasib, mobocertinib. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.
- alfentanil
mobocertinib will decrease the level or effect of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- alfuzosin
mobocertinib will decrease the level or effect of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently
- amiodarone
amiodarone will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib will decrease the level or effect of amiodarone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently - amisulpride
amisulpride and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug. ECG monitoring is recommended if coadministered.
- amitriptyline
mobocertinib will decrease the level or effect of amitriptyline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently
- amobarbital
amobarbital will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- amoxapine
mobocertinib will decrease the level or effect of amoxapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently
- anagrelide
anagrelide and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- aprepitant
aprepitant will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- arformoterol
mobocertinib and arformoterol both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- armodafinil
armodafinil will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- arsenic trioxide
mobocertinib and arsenic trioxide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- artemether/lumefantrine
mobocertinib and artemether/lumefantrine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- asenapine
mobocertinib and asenapine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- asenapine transdermal
mobocertinib and asenapine transdermal both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- atazanavir
atazanavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- azithromycin
mobocertinib and azithromycin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- bedaquiline
mobocertinib and bedaquiline both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- belzutifan
belzutifan will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bexarotene
bexarotene will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bicalutamide
bicalutamide will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- bosentan
bosentan will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- brigatinib
brigatinib will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- buprenorphine
buprenorphine and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine buccal
buprenorphine buccal and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine subdermal implant
buprenorphine subdermal implant and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine transdermal
buprenorphine transdermal and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine, long-acting injection
buprenorphine, long-acting injection and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- butabarbital
butabarbital will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butalbital
butalbital will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib will decrease the level or effect of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information. - ceritinib
ceritinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- chloramphenicol
chloramphenicol will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- chlorpromazine
mobocertinib and chlorpromazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ciprofloxacin
mobocertinib and ciprofloxacin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- citalopram
mobocertinib and citalopram both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- clarithromycin
clarithromycin will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib and clarithromycin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - clobazam
clobazam will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- clofazimine
mobocertinib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- clomipramine
mobocertinib and clomipramine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- clonidine
mobocertinib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- clotrimazole
clotrimazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- clozapine
mobocertinib and clozapine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- cobicistat
cobicistat will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- colchicine
mobocertinib will decrease the level or effect of colchicine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- conivaptan
conivaptan will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- crizotinib
crizotinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and crizotinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - cyclosporine
cyclosporine will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- dabrafenib
dabrafenib will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- daridorexant
mobocertinib 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 mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dasatinib
mobocertinib and dasatinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- degarelix
mobocertinib and degarelix both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- desflurane
desflurane and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- desipramine
mobocertinib and desipramine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- dienogest/estradiol valerate
mobocertinib will decrease the level or effect of dienogest/estradiol valerate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of mobocertinib with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective non-hormonal contraception.
- dihydroergotamine
mobocertinib will decrease the level or effect of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- diltiazem
diltiazem will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- disopyramide
mobocertinib will decrease the level or effect of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
mobocertinib and disopyramide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - dofetilide
mobocertinib and dofetilide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- dolasetron
mobocertinib and dolasetron both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- donepezil
donepezil and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- doxycycline
doxycycline will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- dronedarone
dronedarone will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and dronedarone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - droperidol
mobocertinib and droperidol both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- drospirenone
mobocertinib will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of mobocertinib with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective non-hormonal contraception.
- efavirenz
efavirenz will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
efavirenz and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug. - elacestrant
mobocertinib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- elagolix
elagolix will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eliglustat
eliglustat and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- encorafenib
encorafenib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and encorafenib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - entrectinib
mobocertinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- enzalutamide
enzalutamide will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ergotamine
mobocertinib will decrease the level or effect of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- eribulin
mobocertinib and eribulin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- erythromycin base
erythromycin base will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and erythromycin base both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and erythromycin ethylsuccinate both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and erythromycin lactobionate both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - erythromycin stearate
erythromycin stearate will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and erythromycin stearate both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - escitalopram
mobocertinib and escitalopram both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ethinylestradiol
mobocertinib will decrease the level or effect of ethinylestradiol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of mobocertinib with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective non-hormonal contraception.
- ethosuximide
mobocertinib will decrease the level or effect of ethosuximide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- etravirine
etravirine will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- everolimus
mobocertinib will decrease the level or effect of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- ezogabine
mobocertinib and ezogabine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- fedratinib
fedratinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- fentanyl
mobocertinib will decrease the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- fentanyl intranasal
mobocertinib will decrease the level or effect of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- fentanyl iontophoretic transdermal system
mobocertinib will decrease the level or effect of fentanyl iontophoretic transdermal system by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- fentanyl transdermal
mobocertinib will decrease the level or effect of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- fentanyl transmucosal
mobocertinib will decrease the level or effect of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- fexinidazole
fexinidazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- fingolimod
fingolimod and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- flecainide
mobocertinib and flecainide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- fluconazole
fluconazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and fluconazole both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - fluoxetine
mobocertinib and fluoxetine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- fluphenazine
mobocertinib and fluphenazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- fluvoxamine
fluvoxamine will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- formoterol
mobocertinib and formoterol both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- fosamprenavir
fosamprenavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- fosaprepitant
fosaprepitant will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- foscarnet
mobocertinib and foscarnet both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- fosphenytoin
fosphenytoin will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fostamatinib
fostamatinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- fostemsavir
mobocertinib and fostemsavir both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ganaxolone
mobocertinib 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.
- gemifloxacin
mobocertinib and gemifloxacin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- gemtuzumab
mobocertinib and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- gilteritinib
gilteritinib and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- granisetron
granisetron and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- grapefruit
grapefruit will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- haloperidol
haloperidol will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and haloperidol both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - hydroxychloroquine sulfate
mobocertinib and hydroxychloroquine sulfate both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- hydroxyzine
hydroxyzine and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- ibrexafungerp
ibrexafungerp will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- ibutilide
mobocertinib and ibutilide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- idelalisib
idelalisib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- iloperidone
iloperidone will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and iloperidone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - imatinib
imatinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- indacaterol, inhaled
mobocertinib and indacaterol, inhaled both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- indapamide
mobocertinib and indapamide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- indinavir
indinavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- inotuzumab
mobocertinib and inotuzumab both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- isoflurane
isoflurane and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- isoniazid
isoniazid will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- isradipine
mobocertinib and isradipine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- itraconazole
itraconazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
itraconazole and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug. - ivacaftor
ivacaftor will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- ivosidenib
ivosidenib will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ketoconazole
ketoconazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lapatinib
lapatinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and lapatinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - larotrectinib
larotrectinib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- lefamulin
lefamulin will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and lefamulin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - lenacapavir
mobocertinib 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 mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with mobocertinib (CYP3A4 substrate) when possible. If unavoiable, reduce mobocertinib by approximately 50% and monitor QTc interval more frequently. After moderate CYP3A inhibitor has been discontinued for 3-5 elimination half-lives, resume mobocertinib at dose taken before initiating moderate CYP3A inhibitor. - leniolisib
mobocertinib 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 mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- levofloxacin
mobocertinib and levofloxacin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- levoketoconazole
levoketoconazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- levonorgestrel oral
mobocertinib will decrease the level or effect of levonorgestrel oral by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of mobocertinib with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective non-hormonal contraception.
- levonorgestrel oral/ethinylestradiol/ferrous bisglycinate
mobocertinib will decrease the level or effect of levonorgestrel oral/ethinylestradiol/ferrous bisglycinate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of mobocertinib with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective non-hormonal contraception.
- lithium
lithium and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- lofexidine
mobocertinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- lonafarnib
lonafarnib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lopinavir
lopinavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib and lopinavir both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - lorlatinib
lorlatinib will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lumateperone
mobocertinib will decrease the level or effect of lumateperone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- maprotiline
mobocertinib and maprotiline both increase QTc interval. Avoid or Use Alternate Drug. ]If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- mefloquine
mobocertinib and mefloquine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- methadone
mobocertinib and methadone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- metronidazole
metronidazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- midazolam
mobocertinib will decrease the level or effect of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- mirtazapine
mirtazapine and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- moxifloxacin
mobocertinib and moxifloxacin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- nafcillin
nafcillin will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nefazodone
nefazodone will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nelfinavir
nelfinavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- netupitant/palonosetron
netupitant/palonosetron will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- nilotinib
mobocertinib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- nortriptyline
mobocertinib and nortriptyline both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- octreotide
mobocertinib and octreotide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ofloxacin
mobocertinib and ofloxacin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- olanzapine
mobocertinib and olanzapine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- olutasidenib
mobocertinib 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
mobocertinib will increase the level or effect of omaveloxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ondansetron
mobocertinib and ondansetron both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- osilodrostat
mobocertinib and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- osimertinib
mobocertinib and osimertinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- oxaliplatin
oxaliplatin and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- ozanimod
mobocertinib and ozanimod both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- paliperidone
mobocertinib and paliperidone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- panobinostat
mobocertinib and panobinostat both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- pasireotide
mobocertinib and pasireotide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- pazopanib
mobocertinib and pazopanib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- pentamidine
mobocertinib and pentamidine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- pentobarbital
pentobarbital will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- perphenazine
mobocertinib and perphenazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- phenobarbital
phenobarbital will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenytoin
phenytoin will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pimavanserin
mobocertinib and pimavanserin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- pimozide
mobocertinib will decrease the level or effect of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
mobocertinib and pimozide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - pitolisant
mobocertinib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ponesimod
mobocertinib and ponesimod both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- posaconazole
posaconazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib and posaconazole both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - primaquine
primaquine and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- primidone
primidone will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- procainamide
mobocertinib and procainamide both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- propafenone
mobocertinib and propafenone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- protriptyline
mobocertinib and protriptyline both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- quetiapine
mobocertinib and quetiapine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- quinidine
mobocertinib will decrease the level or effect of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
mobocertinib and quinidine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - quinine
mobocertinib will decrease the level or effect of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
mobocertinib and quinine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- ranolazine
mobocertinib and ranolazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ribociclib
ribociclib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - rifabutin
rifabutin will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifapentine
rifapentine will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rilpivirine
mobocertinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- risperidone
mobocertinib and risperidone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ritonavir
ritonavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib and ritonavir both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - romidepsin
mobocertinib and romidepsin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- rucaparib
rucaparib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- saquinavir
saquinavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib and saquinavir both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - schisandra
schisandra will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- secobarbital
secobarbital will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sertraline
sertraline will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and sertraline both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - sevoflurane
sevoflurane and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- siponimod
siponimod and mobocertinib both increase QTc interval. Avoid or Use Alternate Drug.
- sirolimus
mobocertinib will decrease the level or effect of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- solifenacin
mobocertinib and solifenacin both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- sorafenib
mobocertinib and sorafenib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- sotalol
mobocertinib and sotalol both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- St John's Wort
St John's Wort will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- stiripentol
stiripentol will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sunitinib
mobocertinib and sunitinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- tacrolimus
mobocertinib will decrease the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
mobocertinib and tacrolimus both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - tetrabenazine
mobocertinib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- tetracycline
tetracycline will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- thioridazine
mobocertinib and thioridazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- thiothixene
mobocertinib and thiothixene both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- tipranavir
tipranavir will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- toremifene
mobocertinib and toremifene both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- triazolam
mobocertinib will decrease the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- trimipramine
mobocertinib and trimipramine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- vandetanib
mobocertinib and vandetanib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- vardenafil
mobocertinib and vardenafil both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- vemurafenib
mobocertinib and vemurafenib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- verapamil
verapamil will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- vilanterol/fluticasone furoate inhaled
mobocertinib and vilanterol/fluticasone furoate inhaled both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- voriconazole
voriconazole will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
mobocertinib and voriconazole both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - vorinostat
mobocertinib and vorinostat both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- voxelotor
voxelotor will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
- zanubrutinib
mobocertinib will decrease the level or effect of zanubrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. 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.
- ziprasidone
mobocertinib and ziprasidone both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
Monitor Closely (8)
- atogepant
mobocertinib 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
mobocertinib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- deutetrabenazine
mobocertinib and deutetrabenazine both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).
- doxepin
doxepin and mobocertinib both increase QTc interval. Use Caution/Monitor.
- floxuridine
floxuridine and mobocertinib both increase QTc interval. Use Caution/Monitor.
- isavuconazonium sulfate
mobocertinib will decrease the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- valbenazine
valbenazine and mobocertinib both increase QTc interval. Use Caution/Monitor.
- warfarin
mobocertinib 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.
Minor (0)
Adverse Effects
>10%
All grades
- Diarrhea (92%)
- Rash (78%)
- Decreased red blood cells (59%)
- Increased creatinine (52%)
- Decreased lymphocytes (52%)
- Stomatitis (46%)
- Increased amylase (40%)
- Vomiting (40%)
- Decreased appetite (39%)
- Paronychia (39%)
- Nausea (37%)
- Increased lipase (35%)
- Musculoskeletal pain (34%)
- Dry skin (32%)
- Fatigue (29%)
- Decreased potassium (29%)
- Decreased platelets (26%)
- Decreased leukocytes (25%)
- Increased alkaline phosphatase (25%)
- Pruritus (24%)
- Cough (24%)
- Decreased albumin (23%)
- Decreased magnesium (23%)
- Increased ALT (22%)
- Decreased weight (21%)
- Increased AST (21%)
- Decreased sodium (20%)
- Alopecia (19%)
- Abdominal pain (18%)
- Upper respiratory tract infection (16%)
- Gastroesophageal reflux disease (15%)
- Dyspnea (15%)
- Rhinorrhea (13%)
- Dyspepsia (11%)
- Ocular toxicity (11%)
Grade 3 or 4
- Diarrhea (22%)
- Decreased lymphocytes (15%)
- Increased amylase (13%)
1-10%
All grades
- QTc prolongation (10%)
- Hypertension (10%)
- Headache (10%)
Grade 3 or 4
- Increased lipase (10%)
- Decreased potassium (5.3%)
- Nausea (4.4%)
- Stomatitis (4.4%)
- Hypertension (4.4%)
- Dyspnea (4.4%)
- QTc prolongation (3.5%)
- Fatigue (3.5%)
- Decreased red blood cells (3.5%)
- Decreased magnesium (2.7%)
- Increased ALT (2.7%)
- Increased creatinine (2.7%)
- Vomiting (2.6%)
- Musculoskeletal pain (2.6%)
- Abdominal pain (1.8%)
- Rash (1.8%)
- Increased alkaline phosphatase (1.8%)
- Decreased albumin (1.8%)
- Increased AST (1.8%)
<1%
Grade 3 or 4
- Decreased appetite (0.9%)
- Paronychia (0.9%)
- Pruritus (0.9%)
- Decreased platelets (0.9%)
- Decreased sodium (0.9%)
Warnings
Black Box Warnings
QTc prolongation and torsades de pointes
- Life-threatening heart rate–corrected QTc prolongation, including torsades de pointes, may occur
- Monitor QTc and electrolytes periodically during treatment
- Increase monitoring frequency in patients with risk factors for QTc prolongation (eg, congenital long QT syndrome, heart disease, electrolyte abnormalities)
- Avoid coadministration with drugs that may further prolong the QTc interval (eg, drugs known to prolong QTc interval, strong or moderate CYP3A inhibitors)
- Withhold, reduce dose, or permanently discontinue treatment based on the severity of QTc prolongation
Contraindications
None
Cautions
ILD/pneumonitis, which can be fatal, reported; monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis
Cardiac toxicity (including decreased EF, cardiomyopathy, and congestive HF) resulting in HF, may occur; monitor cardiac function (eg, assessment of left ventricular EF at baseline and during treatment)
May cause fetal harm
QTc prolongation and torsades de pointes
- Life-threatening QTc prolongation, including torsades de pointes, reported
- Assess QTc and electrolytes at baseline and correct abnormalities in sodium, potassium, calcium, and magnesium before initiating therapy
Diarrhea
- Severe diarrhea reported
- Median time to first onset of diarrhea was 5 days; diarrhea occurred within 24 hr after administration
- Diarrhea may lead to dehydration or electrolyte imbalance, with or without renal impairment; treat diarrhea promptly
- Advise patients to start an antidiarrheal agent (eg, loperamide) at first sign of diarrhea or increased bowel movement frequency and to increase fluid and electrolyte intake
- Monitor electrolytes
Drug interaction overview
- CYP3A4 substrate
- Moderate CYP3A4 inducer
- Inhibitor of breast cancer resistance protein (BCRP); clinical significance of changes in pharmacokinetics of sulfasalazine (a BCRP substrate) when coadministered with multiple doses of mobocertinib is unknown
-
Strong or moderate CYP3A4 inhibitors
- Avoid coadministration
- If use of moderate CYP3A4 inhibitors is unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently
- Strong or moderate CYP3A4 inhibitors may increase mobocertinib plasma concentrations and toxicities, including QTc interval
-
Strong or moderate CYP3A4 inducers
- Avoid coadministration
- Strong or moderate CYP3A4 inducers may decrease mobocertinib plasma concentrations and antitumor activity
-
Sensitive CYP3A4 substrates
- Avoid coadministration with hormonal contraceptives OR other CYP3A4 substrates where minimal concentration changes may lead to serious therapeutic failures
- If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information
- Mobocertinib may decrease plasma concentrations of CYP3A4 substrates
-
Drugs that prolong QTc interval
- Avoid coadministration
- If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently
Pregnancy & Lactation
Pregnancy
Based on findings from animal studies and its mechanism of action, may cause fetal harm when administered to pregnant females
No data are available on use in pregnant females
Verify pregnancy status in females of reproductive potential
Contraception
- Females of reproductive potential: Use effective nonhormonal contraception during treatment and for 1 month after last dose; mobocertinib may render hormonal contraceptives ineffective
- Males with female partners of reproductive potential: Use effective contraception during treatment and for 1 week after the last dose
Infertility
- Based on animal studies, fertility in males and females of reproductive potential may be impaired
Animal data
- Oral administration to pregnant rats during organogenesis resulted in embryolethality and maternal toxicity at plasma exposures approximately 1.7x the human exposure based on AUC at the 160-mg once-daily clinical dose
- Advise pregnant females of potential risk to a fetus
Lactation
There are no data on presence of mobocertinib or its metabolites in human milk, its effects on breastfed children, or its effects on milk production
Advise women not to breastfeed during treatment and for 1 week after last 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
Kinase inhibitor of EGFR; irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild-type (WT) EGFR
In cultured cell models, mobocertinib inhibited cell proliferation driven by different EGFR exon 20 insertion mutation variants
In animal tumor implantation models, mobocertinib exhibited antitumor activity against xenografts with the EGFR exon 20 insertions NPH or ASV
Absorption
Peak plasma time: 4 hr
Absolute bioavailability: 37%
Distribution
Plasma bound: 99.3%
Vd (steady-state): 3509 L
Plasma-to-blood ratio
- Mobocertinib: 0.76
- AP32960: 1.2
- AP32914: 0.71
Metabolism
Primarily metabolized by CYP3A4
Active metabolites: AP32960 and AP32914 are equipotent to mobocertinib and account for 36% and 4% of the combined molar AUC, respectively
Elimination
Half-life (steady-state)
- Mobocertinib: 18 hr
- AP32960: 24 hr
- AP32914: 18 hr
Clearance (steady-state)
- Mobocertinib: 138 L/hr
- AP32960: 149 L/hr
- AP32914: 159 L/hr
Excretion
- Mobocertinib: Feces (76% [6% unchanged]); urine (4% [1% unchanged])
- AP32960: Feces (12%); urine (1%)
- AP32914: Below detection limit in both urine and feces
Administration
Oral Administration
Take with or without food at same time each day
Swallow capsules whole; do not open, chew, or dissolve contents
Missed or vomited dose
- Missed dose >6 hr: Skip dose and take next dose the following day at its regularly scheduled time
- Vomited dose: Do not take an additional dose; take next dose as prescribed the following day
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Images
Formulary
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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.
