Belotecan

Belotecan
Clinical data
ATC code	L01XX68 (WHO) ;
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	256411-32-2;
PubChem CID	6456014;
ChemSpider	4958253 ;
UNII	27Z82M2G1N;
ChEMBL	ChEMBL2107315;
CompTox Dashboard (EPA)	DTXSID60180332 ;
Chemical and physical data
Formula	C25H27N3O4
Molar mass	433.50 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	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 ; Key:LNHWXBUNXOXMRL-VWLOTQADSA-N ;
(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(R), 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

http://www.ckdpharm.com/eng/ckd/product/productView.ckd?seq=2463
http://www.ckdpharm.com/eng/ckd/index.ckd
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
"belotecan". drugcentral.org. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-12.

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[1] ttp://www.ckdpharm.com/eng/ckd/product/productView.ckd?seq=2463

[2] ttp://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.