Belotecan
- L01CE04 (WHO)
- (4S)-4-Ethyl-4-hydroxy-11-[2-(isopropylamino)ethyl]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
- 256411-32-2
- 6456014
- DB12459 Y
- 4958253 Y
- 27Z82M2G1N
- D03225
- ChEMBL2107315
- DTXSID60180332
- Interactive image
- O=C\1N4\C(=C/C2=C/1COC(=O)[C@]2(O)CC)c3nc5c(c(c3C4)CCNC(C)C)cccc5
- InChI=1S/C25H27N3O4/c1-4-25(31)19-11-21-22-17(12-28(21)23(29)18(19)13-32-24(25)30)15(9-10-26-14(2)3)16-7-5-6-8-20(16)27-22/h5-8,11,14,26,31H,4,9-10,12-13H2,1-3H3/t25-/m0/s1 Y
- Key:LNHWXBUNXOXMRL-VWLOTQADSA-N Y
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. Archived from the original on 12 November 2016.
- ^ "Camtobell Inj. 2mg". Chong Kun Dang pharmaceutical Corp. Archived from the original on 12 November 2016.
- ^ Sahoo U, ed. (2012). Clinical Research in Asia: Opportunities and Challenges. Oxford: Woodhead Publishing Limited. p. 152. ISBN 978-1-908818-13-3.
New drugs approved in South Korea
- ^ "Belotecan". drugcentral.org. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-12.
- ^ Li F, Jiang T, Li Q, Ling X (2017). "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. PMC 5752681. PMID 29312794.
- v
- t
- e
(M phase)
Block microtubule assembly | |
---|---|
Block microtubule disassembly |
inhibitor
DNA precursors/ antimetabolites (S phase) |
| ||||||||
---|---|---|---|---|---|---|---|---|---|
Topoisomerase inhibitors (S phase) |
| ||||||||
Crosslinking of DNA (CCNS) |
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it. |
- v
- t
- e