On April 3, 2024 Astex Pharmaceuticals, a pharmaceutical company based in Cambridge, UK, dedicated to the discovery and development of novel small molecule therapeutics for oncology and diseases of the central nervous system, reported that it will make five key data presentations at AACR (Free AACR Whitepaper) 2024 focusing on its Phase II-ready MDM2 antagonist, ASTX295 (Press release, Astex Pharmaceuticals, APR 3, 2024, View Source [SID1234641731]). AACR (Free AACR Whitepaper) 2024 will take place from April 5-10, 2024, at the San Diego Convention Center, San Diego, USA.

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ASTX295 data presentations at AACR (Free AACR Whitepaper) 2024

Title Presentation Date/Time/Presenter Link to Abstract
Discovery of ASTX295, a potent, next-generation small molecule antagonist of MDM2 with differentiated pharmacokinetic profile. From concept to clinic Oral Tuesday, April 9
3:20 – 3:35pm PT

Session Title: Novel Antitumor Agents 5

Presenter: Maria Ahn, Astex Pharmaceuticals, UK

6588
View Source!/20272/presentation/4100
ASTX295 engages p53-mediated apoptosis and an inflammatory response in patient derived mesothelioma explants Poster Sunday, April 7
1:30 – 5:00pm PT

Presenter: Dean Fennell, University of Leicester, UK

666
linkView Source!/20272/presentation/4103
Identification of biomarkers of response to MDM2 inhibition in solid tumours using computational, multi-omics approaches

Poster Sunday, April 7
1:30 – 5:00pm PT

Presenter: Matthew Davis, Astex Pharmaceuticals, UK

667
View Source!/20272/presentation/4104
Phase 1 study of MDM2 antagonist ASTX295 in patients with solid tumors with wild-type TP53 Poster Monday, April 8, 9:00 -12:30pm PT
Presenter: Ekaterina Dumbrava, The University of Texas MD Anderson Cancer Center, Houston, TX

CT066
View Source!/20272/presentation/11530
Targeting the MDM2-p53 interaction: Time-and concentration-dependent studies in tumor and normal human bone marrow cells reveal strategies for an enhanced therapeutic index

Poster Monday, April 8
1:30 – 5:00pm PT

Presenter: Steve Wedge, Newcastle University, Newcastle upon Tyne, UK

3333
View Source!/20272/presentation/5680
ASTX295 is an oral, potent inhibitor of the p53-MDM2 protein-protein interaction that was discovered by Astex using its proprietary structure-based drug design approach. The compound was specifically designed to overcome the on-target toxicity seen in the first generation MDM2 antagonist compounds which have shown dose-limiting haematological toxicities in the clinic. In contrast, ASTX295 is a potent MDM2 antagonist with a clean CYP/hERG profile and a shorter human half-life allowing for pulsatile pathway modulation while avoiding myelosuppression. ASTX295 therefore has bone-marrow sparing characteristics which permit a differentiated safety profile to be presented at AACR (Free AACR Whitepaper). Astex is interested in discussing the further development of ASTX295 with potential partners.