Idarubicin is an anthracycline antineoplastic active pharmaceutical ingredient used in oncology. It is a semisynthetic derivative of daunorubicin and exerts its anticancer activity primarily through DNA intercalation and inhibition of topoisomerase II.
Idarubicin has the molecular formula C26H27NO9 and a molecular weight of 493.51 g/mol. Its CAS Number is 58957-92-9.
Idarubicin is an anthracycline antibiotic with potent cytotoxic activity. Compared with some earlier anthracyclines, its structural characteristics provide high lipophilicity and facilitate cellular uptake.
Idarubicin is primarily associated with oncology formulations, particularly pharmaceutical products used in the treatment of acute myeloid leukemia (AML).
Idarubicin acts through multiple mechanisms. It intercalates between DNA base pairs and inhibits topoisomerase II, interfering with DNA replication and transcription.
It can also generate reactive oxygen species, contributing to cellular damage and ultimately promoting cancer-cell death.
Idarubicin API is used in the development and manufacture of:
Idarubicin is produced through controlled pharmaceutical manufacturing processes involving synthesis or semisynthetic preparation, purification and isolation of the active compound.
Quality control may include identification, assay, related substances, water content, residue on ignition, optical properties and residual solvents according to the applicable approved specification.
Idarubicin is generally supplied as an orange-red to reddish crystalline powder. It has limited solubility in water and is generally handled as a pharmaceutical-grade oncology API.
Idarubicin should be stored in a tightly closed container, protected from excessive moisture, heat and direct light. Storage and handling should follow the manufacturer's current CoA, SDS and validated stability requirements.
As an antineoplastic API, appropriate occupational handling controls should be followed during manufacturing and formulation.
Depending on the intended pharmaceutical application, documentation may include:
Idarubicin is an anthracycline antineoplastic API with established cytotoxic activity through DNA intercalation and topoisomerase II inhibition. It is an important pharmaceutical ingredient for oncology drug development and formulations, particularly those associated with acute myeloid leukemia.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 3.0% |
| Residue on Ignition | NMT 0.5% |
| pH (1% Solution) | 4.0 – 6.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 3.0% |
| Melting Point | Approximately 180–185°C (decomposition) |