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Mechanism of Action: ASTX295 is a synthetic small molecule that acts as an antagonist of human Murine Double Minute 2 (MDM2; human homolog also known as HDM2). MDM2 is an E3 ubiquitin ligase which tightly regulates the level and activity of the p53 tumor suppressor. ASTX295 is designed to block the interaction of MDM2 with p53 and to restore p53 function.

Indication: Advanced Solid Tumors

How this therapy can help

ASTX295 is an investigational agent designed to target and bind to MDM2 and to block its interaction with p53. ASTX295 has the potential to activate p53 and its tumor-suppressor functions and induce antitumor responses in cancers with a wild-type p53 gene.

Clinical status

ASTX295 has completed a Phase 1 study in patients with advanced solid tumors characterized by wild-type p53 to determine safety, pharmacokinetics and preliminary activity.

ASTX295 was discovered under a Strategic Alliance agreement between Astex, Newcastle University and Cancer Research Horizons, and is licensed to Mosaic Therapeutics for further research, development and commercialisation using its proprietary platform.

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