Drug intelligence / Profile preview

camonsertib

Development stage
Phase 2
Lead developer
Repare Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Camonsertib is an investigational oral small molecule inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. It selectively targets and inhibits ATR activity, a critical regulator in the DNA damage response (DDR) pathway that responds to DNA replication stress and maintains genomic stability. By inhibiting ATR, camonsertib blocks downstream phosphorylation of checkpoint kinase 1 (CHK1), leading to impaired DNA repair and increased cancer cell death—particularly in tumors with deficiencies in other DDR genes such as ATM or BRCA1/2 mutations. Camonsertib is being developed primarily for the treatment of advanced solid tumors with specific genomic alterations that sensitize them to ATR inhibition. It has demonstrated clinical benefit both as monotherapy and in combination with other agents including PARP inhibitors (talazoparib, olaparib, niraparib), gemcitabine, and lunresertib (a PKMYT1 inhibitor). The drug is currently undergoing Phase 2 clinical trials for solid tumors; a registrational Phase 3 trial in endometrial cancer is planned for late 2025[2][4][5][7][9].

Other names
camonsertib
02

Targets

ATR (ATR serine/threonine kinase)

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