ASTX295 is a novel small molecule antagonist of human Murine Double Minute 2 (MDM2), which tightly regulates the level and activity of the p53 tumor suppressor. According to the data presented at the AACR 2024 conference, the study enrolled 83 participants across 14 cohorts, investigating various dosing regimens and the impact of food intake. The pharmacokinetic analysis revealed similar total weekly exposure for 400 mg once daily and 660 mg twice weekly, with a median time to maximum concentration of 3 hours and a mean half-life of 4-6 hours. Moreover, the pharmacodynamic assessments showed modulation of the p53 pathway. Nausea, vomiting, diarrhea, and fatigue were i...
