Diflomotecan is an organic heteropentacyclic compound, specifically (5R)-8-[(6,7-difluoroquinolin-3-yl)methyl]-5-ethyl-5-hydroxy-1,4,5,8-tetrahydrooxepino[3,4-c]pyridine-3,9-dione, where position 7 of the oxepinopyridine moiety is linked by a single bond to position 3 of the difluoroquinoline ring. It is an E-ring modified camptothecin analogue with enhanced lactone stability in plasma compared to other topoisomerase I inhibitors. Diflomotecan functions as a DNA topoisomerase inhibitor (EC 5.99.1.2) and an antineoplastic agent. It is classified as an organofluorine compound, tertiary alcohol, epsilon-lactone, and organonitrogen heterocyclic compound. It is functionally related to (R)-homocamptothecin.