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Belotecan

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Belotecan
Clinical data
ATC code
Identifiers
  • (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
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H27N3O4
Molar mass433.508 g·mol−1
3D model (JSmol)
  • 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 checkY
  • Key:LNHWXBUNXOXMRL-VWLOTQADSA-N checkY
  (verify)

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 is marketed by ChongKunDang Pharmaceuticals [2] since 2003.[3]

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.

References

  1. ^ http://www.ckdpharm.com/eng/ckd/product/productView.ckd?seq=2463
  2. ^ http://www.ckdpharm.com/eng/ckd/index.ckd
  3. ^ Sahoo, Umakanta (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
  4. ^ "belotecan". drugcentral.org. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-12.