mobocertinib (Rx)

Brand and Other Names:Exkivity

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

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

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 (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)

              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.