Belotecan

Belotecan
Clinical data
ATC code
Identifiers
IUPAC name
  • (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)
SMILES
  • O=C\1N4\C(=C/C2=C/1COC(=O)[C@]2(O)CC)c3nc5c(c(c3C4)CCNC(C)C)cccc5
InChI
  • 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 has been marketed by ChongKunDang 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

  1. ↑ "Camtobell Inj. 2mg". Chong Kun Dang pharmaceutical Corp. Archived from the original on 12 November 2016.
  2. ↑ "Camtobell Inj. 2mg". Chong Kun Dang pharmaceutical Corp. Archived from the original on 12 November 2016.
  3. ↑ 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
  4. ↑ "Belotecan". drugcentral.org. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-12.
  5. ↑ 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.
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