rubitecan

Rubitecan is a synthetic small molecule and oral topoisomerase I inhibitor derived from camptothecin. It binds to and inhibits the enzyme topoisomerase I, inducing protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells. This action prevents the repair of reversible single-strand DNA breaks, leading to cytotoxicity in rapidly proliferating tumor cells. Rubitecan was primarily developed for the treatment of pancreatic cancer and other solid tumors but has not received regulatory approval due to issues with bioavailability and insufficient clinical data[1][2][3][4]. The drug was originally developed by SuperGen (now Astex Pharmaceuticals, part of Otsuka Group)[3].

Brand names

Orathecin

Other names

9-nitrocamptothecin9-nitro-(20S)-camptothecin9-nitrocamptothecin, (S)-isomer9-NCRubitecánRubitécan