Idarubicin: an anthracycline antineoplastic agent

The mechanism of action, pharmacokinetics, activity, adverse effects, and administration of idarubicin are reviewed. Idarubicin is currently approved for use with other agents in the management of acute nonlymphocytic leukemia in adults. This drug is a structural analogue of daunorubicin and has the same mechanism of action as daunorubicin and doxorubicin. Unlike the other currently available anthracyclines, idarubicin has significant oral bioavailability (average 28%), and an oral dosage form is currently under investigation. Idarubicin is at least as effective as daunorubicin for acute nonlymphocytic leukemia, and two studies indicate greater activity and longer survival with an idarubicin-cytarabine regimen than with a daunorubicin-cytarabine regimen. Additional data indicate activity in acute lymphocytic leukemia, lymphomas, and breast cancer. Adverse effects are similar to those seen with other anthracyclines, although idarubicin may be associated with less cardiotoxicity than doxorubicin or daunorubicin. A maximum cumulative dose to prevent chronic cardiomyopathy has not yet been defined. Idarubicin is an effective agent for the management of acute nonlymphocytic leukemia and is reportedly more potent and less cardiotoxic than daunorubicin or doxorubicin.