olutasidenib (Rx)

Brand and Other Names:Rezlidhia
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 150mg

Acute Myeloid Leukemia

Indicated for relapsed and/or refractory acute myeloid leukemia with a confirmed IDH1 mutation (mIDH1+ R/R AML)

150 mg PO BID until disease progression or unacceptable toxicity

For patients without disease progression or toxicity, treat for a minimum of 6 months to allow time for clinical response

Dosage Modifications

Differentiation syndrome

  • Withhold if differentiation syndrome is suspected until signs and symptoms improve
  • Administer systemic corticosteroids and initiate hemodynamic monitoring until symptom resolution for a minimum of 3 days
  • After resolution, resume at 150 mg BID
  • Recurrence
    • If recurrence suspected, withhold and institute treatment per above guidance
    • After symptom resolution, may resume at reduced dose of 150 mg qDay for minimum of 7 days; may then increase to 150 mg BID

Noninfectious leukocytosis

  • Initiate treatment with hydroxyurea, as per standard practices
  • Taper hydroxyurea only after leukocytosis improves or resolves

Hepatotoxicity

  • Grade 3
    • Withhold and monitor liver function tests, twice per week, until laboratory values return to baseline or Grade 1 toxicity
    • Resume at reduced dose of 150 mg qDay and continue monitoring
    • May increase to 150 mg BID if hepatotoxicity resolves to baseline for at least 28 days
    • Discontinue if hepatotoxicity (Grade 3) recurs at 150 mg qDay
  • Grade 4
    • Grade 4 hepatotoxicity OR AST/ALT >3x ULN and total bilirubin (TB) >2x ULN and alkaline phosphatase <2x ULN in absence of a clear alternative explanation: Permanently discontinue

Other adverse effects Grade ≥3

  • Interrupt dosing until toxicity resolves to Grade ≤2
  • Resume at 150 mg qDay; may increase to 150 mg BID if toxicities resolve to Grade ≤1 for at least 1 week
  • Discontinue if Grade ≥3 recurs at 150 mg qDay

Renal impairment

  • Mild-to-moderate (CrCl 30 to <90 mL/min): No dosage modification recommended
  • Severe (CrCl 15-29 mL/min), kidney failure (CrCl <15 mL/min), or dialysis: Recommended dose not established

Hepatic impairment

  • Mild-to-moderate (TB <3x ULN with any AST): No dosage modification recommended; closely monitor for increased probability of differentiation syndrome
  • Severe (TB >3 x ULN with any AST): Recommended dose not established

Dosing Considerations

Patient selection

  • Treatment based on presence of IDH1 mutations in blood or bone marrow as detected by FDA-approved tests

Monitoring

  • Assess blood counts, and blood chemistries including liver function tests H5
  • Before initiating drug
  • First 2 months: At least once weekly
  • Third month: q2weeks
  • Fourth month: Once
  • Month 5 and for duration of therapy: Once every other month

Safety and efficacy not established

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Interactions

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              Serious - Use Alternative (66)

              • alfentanil

                olutasidenib will decrease the level or effect of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • amobarbital

                amobarbital 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.

              • apalutamide

                apalutamide 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.

              • armodafinil

                armodafinil 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.

              • belzutifan

                belzutifan 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.

              • bexarotene

                bexarotene 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.

              • bosentan

                bosentan 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.

              • butabarbital

                butabarbital 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.

              • butalbital

                butalbital 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.

              • carbamazepine

                carbamazepine 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.

                olutasidenib will decrease the level or effect of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • cenobamate

                cenobamate 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.

              • clonidine

                olutasidenib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • colchicine

                olutasidenib will decrease the level or effect of colchicine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • cyclosporine

                olutasidenib will decrease the level or effect of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • dabrafenib

                dabrafenib 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.

              • dihydroergotamine

                olutasidenib will decrease the level or effect of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • disopyramide

                olutasidenib will decrease the level or effect of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • efavirenz

                efavirenz 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.

              • elacestrant

                olutasidenib 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 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.

              • encorafenib

                encorafenib 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.

              • enzalutamide

                enzalutamide 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.

              • ergotamine

                olutasidenib will decrease the level or effect of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • eslicarbazepine acetate

                eslicarbazepine acetate 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.

              • ethosuximide

                olutasidenib will decrease the level or effect of ethosuximide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • etravirine

                etravirine 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.

              • everolimus

                olutasidenib will decrease the level or effect of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • fentanyl

                olutasidenib will decrease the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • fentanyl intranasal

                olutasidenib will decrease the level or effect of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • fentanyl iontophoretic transdermal system

                olutasidenib will decrease the level or effect of fentanyl iontophoretic transdermal system by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • fentanyl transdermal

                olutasidenib will decrease the level or effect of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • fentanyl transmucosal

                olutasidenib will decrease the level or effect of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • fosphenytoin

                fosphenytoin 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.

              • ivosidenib

                ivosidenib 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.

              • lenacapavir

                olutasidenib 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.

              • lorlatinib

                lorlatinib 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.

              • lumacaftor/ivacaftor

                lumacaftor/ivacaftor 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.

              • mavacamten

                mavacamten 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.

              • midazolam

                olutasidenib will decrease the level or effect of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • mitapivat

                mitapivat 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.

              • mitotane

                mitotane 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.

              • mobocertinib

                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.

              • modafinil

                modafinil 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.

              • nafcillin

                nafcillin 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

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

              • pacritinib

                olutasidenib will decrease the level or effect of pacritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • pentobarbital

                pentobarbital 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.

              • pexidartinib

                pexidartinib will decrease the level or effect of olutasidenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Strong or moderate CYP3A inducers decrease olutasidenib (a CYP3A4 substrate) plasma concentrations and efficacy.

              • phenobarbital

                phenobarbital 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.

              • phenytoin

                phenytoin 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.

              • pimozide

                olutasidenib will decrease the level or effect of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • primidone

                primidone 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.

              • quinidine

                olutasidenib will decrease the level or effect of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • quinine

                olutasidenib will decrease the level or effect of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • rifabutin

                rifabutin 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.

              • rifampin

                rifampin 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.

              • rifapentine

                rifapentine 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.

              • secobarbital

                secobarbital 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.

              • sirolimus

                olutasidenib will decrease the level or effect of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • sotorasib

                sotorasib 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.

              • St John's Wort

                St John's Wort 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.

              • tacrolimus

                olutasidenib will decrease the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • telotristat ethyl

                telotristat ethyl 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.

              • triazolam

                olutasidenib will decrease the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • warfarin

                olutasidenib will decrease the level or effect of warfarin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.

              • zanubrutinib

                olutasidenib 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.

              Monitor Closely (1)

              • lenacapavir

                lenacapavir will increase the level or effect of olutasidenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

              Minor (0)

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                Adverse Effects

                >10%

                All grades

                • AST increased (47%)
                • ALT increased (46%)
                • Potassium decreased (46%)
                • Sodium decreased (42%)
                • Alkaline phosphatase increased (42%)
                • Creatinine increased (38%)
                • Fatigue/malaise (36%)
                • Arthralgia (28%)
                • Lymphocytes increased (26%)
                • Bilirubin increased (26%)
                • Uric acid increased (25%)
                • Leukocytosis (25%)
                • Lipase increased (24%)
                • Pyrexia (24%)
                • Dyspnea (24%)
                • Rash (24%)
                • Mucositis (23%)
                • Diarrhea (20%)
                • Transaminitis (20%)
                • Edema (18%)
                • Abdominal pain (18%)
                • Vomiting (17%)
                • Cough (17%)
                • Differentiation syndrome (16%)
                • Decreased appetite (16%)
                • Headache (13%)

                Grades 3 or 4

                • ALT increased (13%)
                • Transaminitis (12%)

                1-10%

                All grades

                • Hypertension (10%)

                Grades 3 or 4

                • AST increased (10%)
                • Potassium decreased (9%)
                • Leukocytosis (9%)
                • Differentiation syndrome (8%)
                • Lipase increased (8%)
                • Sodium decreased (7%)
                • Alkaline phosphatase increased (7%)
                • Dyspnea (5%)
                • Hypertension (5%)
                • Mucositis (3%)
                • Fatigue/malaise (3%)
                • Edema (3%)
                • Arthralgia (3%)
                • Lymphocytes increased (3%)
                • Uric acid increased (3%)
                • Creatinine increased (2%)
                • Bilirubin increased (2%)
                • Decreased appetite (2%)
                • Diarrhea (1%)
                • Abdominal pain (1%)
                • Vomiting (1%)
                • Pyrexia (1%)
                • Cough (1%)
                • Rash (1%)
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                Warnings

                Black Box Warnings

                Differentiation syndrome

                • Associated with rapid proliferation and differentiation of myeloid cells; may be life-threatening or fatal
                • Some patients may recover after treatment or after dosage interruption
                • May occur as early as 1 day and up to 18 months after treatment initiation; has been observed with or without concomitant leukocytosis
                • Symptoms may include dyspnea, pulmonary infiltrates/pleuropericardial effusion, kidney injury, hypotension, fever, and weight gain
                • If differentiation syndrome suspected, withhold olutasidenib and initiate treatment with corticosteroids and hemodynamic monitoring until symptom resolution
                • May recur with premature discontinuation of corticosteroids and/or hydroxyurea treatment after treating for concomitant leukocytosis

                Contraindications

                None

                Cautions

                Differentiation syndrome

                • Can cause differentiation syndrome
                • If suspected, withhold dose and initiate corticosteroids (eg, dexamethasone 10 mg IV q12hr for at least 3 days)
                • See dosage modifications further information

                Hepatotoxicity

                • Can cause hepatotoxicity, presenting as increased ALT, increased AST, increased blood alkaline phosphatase, and/or elevated bilirubin
                • Monitor frequently for clinical symptoms of hepatic dysfunction such as fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice
                • If hepatic dysfunction occurs, withhold, reduce, or permanently discontinue based on recurrence/severity

                Drug interaction overview

                • CYP3A substrate and inducer
                • Strong or moderate CYP3A inducers
                  • Avoid coadministration
                  • Coadministration with strong or moderate CYP3A inducers decreases olutasidenib Cmax and AUC, which may reduce efficacy
                • Sensitive CYP3A substrates
                  • Avoid coadministration, unless otherwise instructed in the substrates’ prescribing information
                  • If concomitant use is unavoidable, monitor for loss of therapeutic effect of these drugs
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                Pregnancy & Lactation

                Pregnancy

                Based on animal embryofetal toxicity studies, may cause fetal harm when administered to pregnant females

                Animal studies

                • Resulted in embryofetal death and altered fetal growth when administered to pregnant rats and rabbits during organogenesis at exposures up to 10 times and 0.7 times, respectively, the human exposure at the recommended daily dose

                Lactation

                Data are not available on presence in human milk, effects on breastfed children, or effects on milk production

                Advise females not to breastfeed during treatment and for 2 weeks 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.

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                Pharmacology

                Mechanism of Action

                Inhibits mutated isocitrate dehydrogenase-1 (IDH1), an enzyme that turns isocitrate into 2-ketoglutarate, an oncometabolite

                Inhibition of IDH1 induces cellular differentiation and prevents cellular proliferation in IDH1 expressing cells

                Absorption

                Peak plasma time: ~4 hr

                Steady-state reached: 14 days

                Peak plasma concentration (steady-state): 3473 ng/mL

                AUC (0-12 hr at steady-state): 43,050 ng⋅h/mL

                Effect of food

                • High-fat meal: Peak plasma concentration increased by 191% (20.6%) and AUC increased by 83% (18.3%) following administration of a single 150 mg dose

                Distribution

                Protein bound: 93%

                Vd: 319 L

                Metabolism

                N-dealkylation, demethylation, oxidative deamination followed by oxidation, monooxidation with subsequent glucuronidation

                Primarily (90%) metabolized by CYP3A4, with minor contributions from CYP2C8, CYP2C9, CYP1A2, and CYP2C19

                Elimination

                Half-life: ~67 hr

                Oral clearance: 4 L/hr

                Excretion: Feces 75% (35% unchanged); urine 17% (1% unchanged)

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                Administration

                Oral Administration

                Take on empty stomach at least 1 hr before or 2 hr after a meal

                Administer at about the same time each day

                Do not administer 2 doses within 8 hr

                Swallow capsule whole; do not break, open, or chew

                Vomited dose

                • Do not administer a replacement dose
                • Wait until next scheduled dose is due

                Missed dose

                • If dose is missed or not taken at the usual time, administer dose as soon as possible and at least 8 hr before next scheduled dose
                • Return to normal schedule the following day

                Storage

                Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                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
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.