Products
Doxorubicin is commercially available as an injectable (Adriblastin, generic). It has been approved in many countries since 1989. Caelyx is a pegylated and liposomal formulation of the drug and was registered in 1997. Myocet is a liposomal and nonpegylated formulation.
Structure and properties
Doxorubicin (C27H29NO11, Mr = 543.5 g/mol) is structurally closely related to daunorubicin and epirubicin. It is present in drugs as doxorubicin hydrochloride, an orange-red, crystalline, hygroscopic powder that is soluble in water. Doxorubicin is obtained from var. and certain strains of. It has an active metabolite, doxorubicinol (adriamycinol, 13-hydroxydoxorubicin).
Effects
Doxorubicin (ATC L01DB01) has cytotoxic properties. The effects are due to inhibition of nucleic acid synthesis by intercalation into DNA and inhibition of topoisomerase II. This also reduces protein synthesis.
Indications
Doxorubicin is a cytostatic agent that is widely used in chemotherapy (e.g., breast cancer, bronchial carcinoma, sarcomas, thyroid carcinoma, non-Hodgkin’s lymphoma, Hodgkin’s disease).
Dosage
According to the SmPC. The drug is administered intravenously.
Contraindications
For complete precautions, see the drug label.
Interactions
Doxorubicin is a substrate of CYP3A4 and CYP2D6 and is transported by P-glycoprotein. Corresponding drug-drug interactions with CYP inducers and CYP inhibitors have been described. Other interactions are possible with ciclosporin and other cytostatic drugs.
Adverse effects
The most common potential adverse effects include hair loss, hand-foot syndrome, weakness, blood count abnormalities (leukopenia, neutropenia, anemia, thrombocytopenia), infection, fever, chills, abnormal ECG, mucosal inflammation, vomiting, poor appetite, nausea, diarrhea, and elevated liver enzymes. Serious side effects include bone marrow depression and heart disease (cardiomyopathies).
