Belotecan

Belotecan
Clinical data
ATC code	L01CE04 (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;
DrugBank	DB12459 ;
ChemSpider	4958253 ;
UNII	27Z82M2G1N;
KEGG	D03225;
ChEMBL	ChEMBL2107315;
CompTox Dashboard (EPA)	DTXSID60180332 ;
Chemical and physical data
Formula	C25H27N3O4
Molar mass	433.508 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, 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

"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.

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[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.