Drug intelligence / Profile preview

ATX-898

Development stage
Phase 2
Lead developer
Antares Therapeutics
Modality
Small Molecules
Administration
Subcutaneous
01

Overview

ATX-898 is a subcutaneous formulation of **ceralasertib** (formerly AZD6738), a potent and selective small molecule inhibitor of the **Ataxia Telangiectasia and Rad3-related (ATR) kinase**. Developed by **Antares Therapeutics** (now part of **Halozyme Therapeutics**) under license from **AstraZeneca**, ATX-898 was designed to provide an improved pharmacokinetic profile and greater patient convenience compared to oral administration. ATR kinase is a key regulator of the DNA damage response (DDR), specifically responding to replication stress and single-strand breaks. By inhibiting ATR, ATX-898 disrupts DNA repair mechanisms, leading to genomic instability and cell death, particularly in tumors with existing DDR deficiencies such as ATM loss. The program was evaluated in a Phase 1/2 clinical trial for advanced solid tumors, including ovarian, gynecologic, and HR+/HER2- breast cancers, both as a monotherapy and in combination with agents like fulvestrant and CDK4/6 inhibitors. However, the clinical development of ATX-898 was terminated by the sponsor in 2022.

Other names
subcutaneous ceralasertib
02

Targets

ATR (ATR serine/threonine kinase)

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