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  • 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. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C64772\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C64772\' NCI Thesaurus)
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