esorubicin

Esorubicin (4'-deoxydoxorubicin) is a semi-synthetic anthracycline analogue of doxorubicin, characterized by the absence of the hydroxyl group at the 4' position of the amino sugar moiety. Developed by Farmitalia Carlo Erba, the compound was designed to maintain the potent antineoplastic activity of doxorubicin while potentially reducing the characteristic dose-limiting cardiotoxicity associated with parent anthracyclines. The drug functions primarily through DNA intercalation and the inhibition of Topoisomerase II, which stabilizes the DNA-enzyme cleavable complex, induces double-strand DNA breaks, and triggers apoptosis. Clinical development in the 1980s reached Phase II trials across a broad range of indications, including breast, pancreatic, and colorectal cancers, as well as non-Hodgkin lymphoma. However, esorubicin demonstrated significant myelosuppression, specifically leukopenia, as its primary dose-limiting toxicity and did not show a sufficient therapeutic advantage over existing agents like doxorubicin or epirubicin to justify further development.

Other names

4'-deoxydoxorubicindeoxydoxorubicin4'-deoxy-doxorubicin4'-deoxyadriamycin