Diflomotecan, formerly known as BN80915, is an E-ring modified camptothecin analogue, which possesses greater lactone stability in plasma compared with other topoisomerase I inhibitors. Diflomotecan is also a 10,11-difluoro-homocamptothecin, represents a new promising class of topoisomerase I inhibitors with enhanced plasma stability and superior preclinical anti-tumour activity as compared to the established camptothecins, irinotecan and topotecan. Diflomotecan was the first homocamptothecin to enter clinical studies. Phase I data are summarized for both the intravenous and orally bioavailable schedules. The toxicity is primarily haematological while no severe gastrointestinal toxicity has been observed in contrast to other topoisomerase I inhibitors. Diflomotecan has a high orally bioavailable bioavailability (72 - 95%) and the orally bioavailable day 1 - 5 every 3 weeks regimen is recommended for Phase II testing because it is relatively well tolerated, convenient and mimics protracted exposure. References: Mangas-Sanjuan V, Buil-Bruna N, Garrido MJ, Soto E, Trocóniz IF. Semimechanistic Cell-Cycle Type-Based Pharmacokinetic/Pharmacodynamic Model of Chemotherapy-Induced Neutropenic Effects of Diflomotecan under Different Dosing Schedules. J Pharmacol Exp Ther. 2015 Jul;354(1):55-64. doi: 10.1124/jpet.115.223776. Epub 2015 May 6. PubMed PMID: 25948593.

纯度：≥98%

CAS：220997-97-7