tenifatecan
A lipophilic preparation of 7-ethyl-10-hydroxycamptothecin (SN-38) with potential antineoplastic activity. Tenifatecan is an oil-in-water emulsion of tocopherol covalently linked, via a succinate linker, to SN-38, an active metabolite of the camptothecin derivative irinotecan. After the succinate linker is hydrolyzed in vivo, the active moiety SN-38 is released and selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks and inducing lethal double-stranded DNA breaks; DNA replication is inhibited and apoptosis is triggered. This agent may provide greater delivery and exposure of SN-38 to the tumor than can be achieved with irinotecan.
| Synonym: | tocopherol-conjugated camptothecin derivative SN2310 |
|---|---|
| Code name: | SN2310 |
| Chemical structure: | (4S)-4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H- pyrano[3',4':6,7]indolizino[1,2-b]quinolin- 9-yl (2R)-2,5,7,8-tetramethyl-2-[(4R,8R)- 4,8,12-trimethyltridecyl]-3,4-dihydro-2H-1-benzopyran-6-yl butanedioate Butanedioic acid, (4S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H- pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl (2R)-3,4-dihydro-2,5,7,8-tetramethyl-2- [(4R,8R)-4,8,12-trimethyltridecyl]-2H-1-benzopyran-6-yl ester |