belotecan-hydrochloride

Description: Belotecan (CKD-602), a Topoisomerase I inhibitor, is the semi-synthetic camptothecin analogue with potential antitumor activity. Belotecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the top technicaloisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Topoisomerase I is an enzyme that mediates reversible single-strand breaks in DNA during DNA replication.

References: Park YH, Chung CU, Park BM, Park MR, Park DI, Moon JY, Park HS, Kim JH, Jung SS, Kim JO, Kim SY, Lee JE. Lesser Toxicities of Belotecan in Patients with Small Cell Lung Cancer: A Retrospective Single-Center Study of Camptothecin Analogs. Can Respir J. 2016; 2016:3576201. doi: 10.1155/2016/3576201. Epub 2016 Nov 27. PubMed PMID: 28018128; PubMed Central PMCID: PMC5149640.