9-aminocamptothecin

9-Aminocamptothecin is a synthetic, water-insoluble derivative of camptothecin and belongs to the class of pyranoindolizinoquinoline alkaloids. It acts as a potent inhibitor of the nuclear enzyme topoisomerase I, thereby preventing the repair of single-strand DNA breaks during DNA replication. This leads to cytotoxicity in rapidly dividing cells, making it an investigational antineoplastic agent. The drug was first synthesized by Wani and Wall in 1986 and entered clinical trials in the early 1990s for various cancers including lymphoma, gastric cancer, ovarian cancer, esophageal cancer, and ovarian neoplasms. Its development has been limited by myelosuppression as a dose-limiting toxicity and instability of its active lactone form under physiological conditions[2][3][4][6]. Both oral and intravenous routes have been explored; however, clinical efficacy has generally been modest compared to other topoisomerase I inhibitors such as irinotecan or topotecan[6].

Other names

9-amino-camptothecin91421-43-1