Idarubicin — Drug Monograph

Brand names: Idamycin PFS

Drug class: Anthracycline

Mechanism of Action

Idarubicin is a DNA-intercalating analog of daunorubicin that inhibits the enzyme topoisomerase II, leading to the formation of DNA-protein complexes and DNA strand breaks. Its high lipophilicity compared to daunorubicin facilitates faster cellular uptake and improved penetration into the nucleus. The active metabolite, idarubicinol, contributes significantly to its prolonged duration of action and cytotoxic effect. These processes collectively inhibit nucleic acid synthesis and induce apoptosis in hematopoietic malignancies.

FDA Indications

Common Side Effects

Clinical Pearl

Idarubicin is generally considered more potent than daunorubicin on a milligram-for-milligram basis due to its lipophilicity and active metabolite. Like other anthracyclines, it carries a lifetime cumulative dose limit, usually recommended to not exceed 150 mg/m². Patients should be warned about the transient red discoloration of urine to avoid unnecessary alarm.

Related Therapies & Mechanisms