mobocertinib (Rx)

Brand and Other Names:Exkivity
  • Print

Dosing & Uses

AdultPediatric

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

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

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and mobocertinib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (212)

              • abametapir

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

              • 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

              • 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

              • apalutamide

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

              • apomorphine

                mobocertinib will decrease the level or effect of apomorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently

              • 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.

              • 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

                clozapine 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 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.

              • 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

                desipramine 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 desipramine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

              • deutetrabenazine

                mobocertinib and deutetrabenazine 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.

              • elagolix

                elagolix will decrease the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • mitotane

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

              • modafinil

                modafinil 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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 (4)

              • 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.

              • doxepin

                doxepin 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.

              Minor (0)

                Previous
                Next:

                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%)
                Previous
                Next:

                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
                Previous
                Next:

                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.

                Previous
                Next:

                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
                Previous
                Next:

                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)

                Previous
                Next:

                Images

                No images available for this drug.
                Previous
                Next:

                Patient Handout

                A Patient Handout is not currently available for this monograph.
                Previous
                Next:

                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
                Additional Offers
                Email to Patient

                From:

                To:

                The recipient will receive more details and instructions to access this offer.

                By clicking send, you acknowledge that you have permission to email the recipient with this information.

                Email Forms to Patient

                From:

                To:

                The recipient will receive more details and instructions to access this offer.

                By clicking send, you acknowledge that you have permission to email the recipient with this information.

                Previous
                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.