Camonsertib

Camonsertib
Clinical data
Other names	RP-3500
Identifiers
	IUPAC name (1R,5S)-3-[6-[(3R)-3-methylmorpholin-4-yl]-1-(1H-pyrazol-5-yl)pyrazolo[3,4-b]pyridin-4-yl]-8-oxabicyclo[3.2.1]octan-3-ol;
CAS Number	2417489-10-0;
PubChem CID	156487652;
IUPHAR/BPS	12073;
ChemSpider	127408990;
UNII	S1Z7Y5G56T;
KEGG	D12321;
ChEBI	CHEBI:229722;
ChEMBL	ChEMBL5095260;
Chemical and physical data
Formula	C21H26N6O3
Molar mass	410.478 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H]1COCCN1C2=NC3=C(C=NN3C4=CC=NN4)C(=C2)C5(C[C@H]6CC[C@@H](C5)O6)O;
	InChI InChI=InChI=1S/C21H26N6O3/c1-13-12-29-7-6-26(13)19-8-17(21(28)9-14-2-3-15(10-21)30-14)16-11-23-27(20(16)24-19)18-4-5-22-25-18/h4-5,8,11,13-15,28H,2-3,6-7,9-10,12H2,1H3,(H,22,25)/t13-,14-,15+,21?/m1/s1; Key:YIHHYCIYAIVQKX-YNOVCBQDSA-N;

Camonsertib is an investigational new drug that is being evaluated for the treatment of cancer. It is a selective oral small molecule inhibitor of ATR (Ataxia telangiectasia and Rad3 related), developed by Repare Therapeutics. This drug targets tumors with specific genetic alterations that create vulnerabilities in DNA damage response (DDR) pathways, particularly those with ATM or BRCA1/BRCA2 mutations.^[1] It is currently in Phase 2 clinical trials both as a monotherapy and in combination with other agents, including PARP inhibitors, gemcitabine, and lunresertib.^[2]

References

^ Black WC, Abdoli A, An X, Auger A, Beaulieu P, Bernatchez M, et al. (February 2024). "Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)". Journal of Medicinal Chemistry. 67 (4): 2349–2368. doi:10.1021/acs.jmedchem.3c01917. PMID 38299539.
^ Halder P, Rai A, Talukdar V, Das P, Lakkaniga NR (May 2024). "Pyrazolopyridine-based kinase inhibitors for anti-cancer targeted therapy". RSC Medicinal Chemistry. 15 (5): 1452–1470. doi:10.1039/d4md00003j. PMC 11110789. PMID 38784451.

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[Black_2024-1] Black WC, Abdoli A, An X, Auger A, Beaulieu P, Bernatchez M, et al. (February 2024). "Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)". Journal of Medicinal Chemistry. 67 (4): 2349–2368. doi:10.1021/acs.jmedchem.3c01917. PMID 38299539.

[Halder_2024-2] Halder P, Rai A, Talukdar V, Das P, Lakkaniga NR (May 2024). "Pyrazolopyridine-based kinase inhibitors for anti-cancer targeted therapy". RSC Medicinal Chemistry. 15 (5): 1452–1470. doi:10.1039/d4md00003j. PMC 11110789. PMID 38784451.

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