Tenifatecan

**Semantic type:** Organic Chemical|Pharmacologic Substance

**Definition:** A highly lipophilic preparation of 7-Ethyl-10-hydroxycamptothecin (SN-38) with potential antineoplastic activity. SN2310 is an oil-in-water emulsion of tocopherol covalently linked, via a succinate linker, to SN-38, a synthetic derivative of the cytotoxic alkaloid camptothecin. After 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. This inhibits DNA replication and triggers programmed cell death. SN2310 emulsion provides longer circulation time and potentiates drug exposure as compared to the unconjugated SN-38.

**Synonyms:** - (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 - SN-2310 - SN2310 - TENIFATECAN - Tocopherol Succinate 7-Ethyl-10-Hydroxycamptothecin