diflomotecan

Diflomotecan is a small molecule chemotherapeutic agent and an E-ring modified camptothecin analogue that functions as a DNA topoisomerase I inhibitor. It differs from other camptothecin-based inhibitors like topotecan by having a 7-membered oxepan-2-one (E-ring), which confers greater lactone stability in plasma. This increased stability may enhance antitumor activity and oral bioavailability compared to established agents such as irinotecan and topotecan. Diflomotecan was the first homocamptothecin to enter clinical trials, initially developed for the treatment of cancer—primarily small cell lung cancer (SCLC). Its mechanism involves stabilizing the cleavable complex between DNA and topoisomerase I during replication, leading to single-strand breaks that ultimately result in apoptosis of rapidly dividing tumor cells. The drug was investigated in both intravenous and oral formulations; its main toxicity is hematological with relatively mild gastrointestinal side effects[1][3][4][5][7].

Brand names

Diflomotecan

Other names

diflomotecanumDiflomotecan [INN]220997-97-7