hydroxydaunorubicin

Hydroxydaunorubicin, commonly referred to as doxorubicin, is an anthracycline antibiotic used in cancer chemotherapy. It is produced by Streptomyces species and is one of the most widely employed anticancer drugs. In clinical practice it is typically given intravenously and is not effective when taken orally due to poor bioavailability.

Mechanism of action centers on DNA damage and cell death. The drug intercalates between DNA base pairs, inhibiting DNA replication and transcription. It also inhibits topoisomerase II, an enzyme essential for DNA unwinding, and generates reactive oxygen species through iron-mediated redox cycling, contributing to cytotoxic effects in rapidly dividing tumor cells.

Hydroxydaunorubicin has a broad spectrum of activity against many solid tumors and hematologic malignancies. It is used in various combination regimens for breast cancer, lymphomas, leukemias, sarcomas, and ovarian cancer, among others. Treatment regimens often combine doxorubicin with other chemotherapeutic agents to enhance efficacy while balancing toxicity. Cardiac function is routinely monitored due to potential cardiotoxicity.

Pharmacokinetics and metabolism involve extensive tissue distribution and hepatic metabolism to active and inactive metabolites, including doxorubicinol. Excretion is predominantly biliary, with limited renal elimination. The drug’s pharmacokinetics are influenced by liver function and age, and cumulative exposure is an important consideration in dosing.

Adverse effects include myelosuppression, mucositis, alopecia, and nausea. The most serious risk is dose-related cardiotoxicity, which can lead to congestive heart failure, often after high cumulative doses. Other risks include local tissue injury if extravasation occurs and an increased risk of secondary malignancies with long-term use. Monitoring and dose planning are essential to mitigate these risks.