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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Isocitrate dehydrogenase (IDH) inhibitors
ivosidenib
L01XM02
Adult Dosing
- AML with IDH1 mutation: 500 mg orally once daily until disease progression or unacceptable toxicity
- Cholangiocarcinoma with IDH1 mutation: 500 mg orally once daily until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy not established in pediatric patients
Indications
- Newly diagnosed acute myeloid leukemia (AML) with an isocitrate dehydrogenase-1 (IDH1) mutation in adults unable to receive intensive induction chemotherapy
- Relapsed or refractory AML with an IDH1 mutation in adults
- Locally advanced or metastatic cholangiocarcinoma with an IDH1 mutation previously treated with at least one prior therapy
Mechanism of Action
- Small-molecule inhibitor of mutant isocitrate dehydrogenase 1 (IDH1)
- Inhibits mutant IDH1 enzymes (R132H, R132C, R132L, R132S, R132G), reducing 2-hydroxyglutarate (2-HG) levels
- Restores normal cellular differentiation and induces apoptosis in leukemic cells
Contraindications
- History of severe hypersensitivity to ivosidenib
Adverse Reactions
- Differentiation syndrome
- QT interval prolongation
- Leukocytosis
- Arthralgia and myalgia
- Diarrhea, nausea, and vomiting
- Fatigue
- Edema
Drug Interactions
- Strong or moderate CYP3A4 inhibitors increase ivosidenib exposure and risk of QT prolongation; monitor closely and reduce dose if needed
- Strong or moderate CYP3A4 inducers decrease ivosidenib concentrations; avoid coadministration
- Coadministration with other drugs known to prolong the QT interval (e.g., antiarrhythmics, fluoroquinolones, azole antifungals) increases risk of ventricular arrhythmias
Curated Content: Needs Vetting Before Put to Clinical Use