Idarubicin

Idarubicin is an anthracycline antibiotic used in cancer chemotherapy. It is primarily employed to treat acute myeloid leukemia (AML), typically as part of induction regimens such as idarubicin with cytarabine, and is used in some regimens for other hematologic malignancies. It is a semi-synthetic derivative of daunorubicin with greater lipophilicity, which enhances cellular uptake and tissue penetration.

Mechanism of action centers on DNA intercalation and inhibition of topoisomerase II, leading to disruption of DNA replication and repair. Idarubicin also generates reactive free radicals that contribute to cytotoxicity. It is a cell cycle-nonspecific agent. The drug is administered intravenously, and dosing varies by regimen and patient factors. The major circulating metabolite is idarubicinol, formed in the liver and retaining pharmacologic activity.

Pharmacokinetics and metabolism involve extensive hepatic processing, with elimination occurring through hepatic and, to a lesser extent, renal routes. Dosing and duration are determined by the specific AML or other cancer regimen and regional practice patterns.

Safety and adverse effects are dominated by hematologic toxicity, notably myelosuppression. Other common effects include mucositis, nausea, vomiting, fatigue, and alopecia. Cardiotoxicity is a key concern with anthracyclines; cumulative dose limits and regular cardiac monitoring (such as echocardiography) are recommended to mitigate risk of cardiomyopathy or heart failure. Infusion-related reactions and extravasation risk are also considerations.

Regulatory status: idarubicin is approved in many countries for AML as part of combination regimens and is used as an alternative to daunorubicin or doxorubicin in some protocols. See also doxorubicin and daunorubicin for related compounds.