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Camonsertib

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Pharmaceutical compound
Camonsertib
Clinical data
Other namesRP-3500
Identifiers
IUPAC name
  • (1R,5S)-3--1-(1H-pyrazol-5-yl)pyrazolopyridin-4-yl]-8-oxabicyclooctan-3-ol
CAS Number
PubChem CID
IUPHAR/BPS
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC21H26N6O3
Molar mass410.478 g·mol
3D model (JSmol)
SMILES
  • C1COCCN1C2=NC3=C(C=NN3C4=CC=NN4)C(=C2)C5(C6CC(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. It is currently in Phase 2 clinical trials both as a monotherapy and in combination with other agents, including PARP inhibitors, gemcitabine, and lunresertib.

References

  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.
  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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