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  • A synthetic analogue of camptothecin with potential antineoplastic and radio-sensitizing activities. Camptothecin analogue TLC388 selectively stabilizes topoisomerase I-DNA covalent complexes during S-phase, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. Topoisomerase I relaxes negative super-coiled DNA during replication and transcription. This agent has been chemically modified to enhance the potency and stability of camptothecin. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C80047\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C80047\' NCI Thesaurus)
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