Chemistry:Belotecan
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| Formula | C25H27N3O4 |
| Molar mass | 433.508 g·mol−1 |
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Belotecan is a drug used in chemotherapy. It is a semi-synthetic camptothecin analogue indicated for small-cell lung cancer and ovarian cancer, approved in South Korea under the trade name Camtobell, presented in 2 mg vials for injection.[1] The drug has been marketed by Chong Kun Dang Pharmaceuticals[2] since 2003.[3]
Mechanism of action
Belotecan blocks topoisomerase I with a pIC50 of 6.56,[4] 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 topoisomerase 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.[5]
References
- ↑ "Camtobell Inj. 2mg". Chong Kun Dang pharmaceutical Corp. http://www.ckdpharm.com/eng/ckd/product/productView.ckd?seq=2463.
- ↑ "Camtobell Inj. 2mg". Chong Kun Dang pharmaceutical Corp. http://www.ckdpharm.com/eng/ckd/index.ckd.
- ↑ Clinical Research in Asia: Opportunities and Challenges. Oxford: Woodhead Publishing Limited. 2012. pp. 152. ISBN 978-1-908818-13-3. "New drugs approved in South Korea"
- ↑ "Belotecan". UNM School of Medicine. 2016-07-31. http://drugcentral.org/drugcard/296/view?q=belotecan.
- ↑ "Camptothecin (CPT) and its derivatives are known to target topoisomerase I (Top1) as their mechanism of action: did we miss something in CPT analogue molecular targets for treating human disease such as cancer?". American Journal of Cancer Research 7 (12): 2350–2394. 2017. PMID 29312794.
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