Drug intelligence / Profile preview

astx295

Development stage
Phase 1
Lead developer
Mosaic Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

ASTX295 is a synthetic, orally available small molecule antagonist of the human Murine Double Minute 2 (MDM2) protein. By binding to MDM2, ASTX295 blocks its interaction with the tumor suppressor protein p53, preventing p53 degradation and restoring its transcriptional activity. This reactivation of p53 leads to antitumor responses in cancers that retain wild-type p53. ASTX295 has demonstrated potent antiproliferative and pro-apoptotic effects in preclinical models of solid tumors and hematologic malignancies with wild-type TP53. The drug is being developed by Astex Pharmaceuticals (a subsidiary of Otsuka) and was evaluated in Phase 1/2 clinical trials for advanced solid tumors characterized by wild-type p53[1][2][3][4][5].

Other names
P53 programP-53 programP 53 programMDM2-p53 inhibitorMDM-2-p53 inhibitorMDM 2-p53 inhibitorMDM2 antagonistMDM-2 antagonistMDM 2 antagonist
02

Targets

MDM2 (Mouse double minute 2 homolog)

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