Idarubicin (DB01177): A Comprehensive Clinical and Pharmacological Monograph

Section 1: Drug Identification and Physicochemical Properties

1.1 Overview and Classification

Idarubicin is a potent, semi-synthetic antineoplastic agent belonging to the anthracycline class of antibiotics.[1] It is classified as a small molecule and a derivative of a natural product, primarily utilized in the chemotherapeutic treatment of specific hematological malignancies.[3] As a member of the antitumor antibiotic family, Idarubicin is a cornerstone of induction therapy for certain types of leukemia, distinguished from its parent compounds by its high lipophilicity and enhanced potency.[2]

1.2 Nomenclature and Identifiers

Idarubicin is the International Nonproprietary Name (INN) for the active substance, which is also available for clinical use as Idarubicin Hydrochloride.[1] The drug is known by several synonyms, with the most chemically descriptive being 4-demethoxydaunorubicin, which highlights its structural relationship to the parent compound, daunorubicin.[1] Other historical and research identifiers include IMI-30 and NSC-256439.[1] A comprehensive list of its key identifiers is provided in Table 1.1.

1.3 Chemical and Physical Characteristics

Idarubicin has the molecular formula C26​H27​NO9​ and a molecular weight of approximately 497.49 g/mol.[8] It exists as a solid that is formulated for clinical use as a sterile, red-orange, isotonic parenteral solution.[4] The increased lipophilicity imparted by the removal of the methoxy group is a defining physicochemical characteristic that profoundly influences its pharmacological behavior.[2] For storage, the compound requires protection from light and is kept in dry, sealed conditions at 2-8°C for short-term stability or -20°C for long-term storage.[4]