camptothecin-20-O-propionate

Camptothecin-20-O-propionate (CZ48) is an orally bioavailable small molecule pro-drug of camptothecin (CPT), a cytotoxic alkaloid originally isolated from the Chinese tree *Camptotheca acuminata*. Developed by the CHRISTUS Stehlin Foundation for Cancer Research, CZ48 is an esterification product of natural camptothecin and propionic anhydride. It was designed to overcome the stability and toxicity issues associated with native camptothecin, specifically by maintaining the active lactone ring structure in human plasma. CZ48 acts as a pro-drug that is converted into the active moiety, camptothecin, by endogenous esterases which are often overexpressed in malignant cells. Once activated, it inhibits topoisomerase I, leading to DNA double-strand breaks and tumor cell apoptosis. Clinical investigation has focused on its potential in treating advanced solid tumors and lymphomas while attempting to mitigate dose-limiting toxicities such as diarrhea and cystitis.

Other names

20(S)-Camptothecin propionateCamptothecin-20-O-propionate hydrateCamptothecin20-O-propionate hydrateCamptothecin 20-O-propionate hydratePropionyl camptothecin