Drug intelligence / Profile preview

tuvusertib

Development stage
Phase 2
Lead developer
Merck KGaA
Modality
Small Molecules
Administration
Oral
01

Overview

Tuvusertib is a potent, selective, orally administered small molecule inhibitor of ataxia telangiectasia and Rad3-related (ATR) protein kinase. ATR plays a critical role in the DNA damage response by facilitating DNA repair and promoting cancer cell survival under genotoxic stress. By inhibiting ATR kinase activity, tuvusertib disrupts the ability of cancer cells to repair damaged DNA, leading to cell death—particularly in tumors with existing defects in other DNA repair pathways. Tuvusertib is being investigated primarily as an antineoplastic agent for various advanced solid tumors and gynecological cancers. It has shown manageable safety and exposure-related target engagement in early-phase clinical trials[1][2][6][8].

Other names
2-amino-6-fluoro-N-[5-fluoro-4-(1-methyl-1H-imidazol-5-yl)pyridin-3-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
02

Targets

ATR (ATR serine/threonine kinase)

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