Phase 1 Study of Rezatapopt, a p53 Reactivator, in TP53 Y220C-Mutated Tumors - PubMed
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- #p53 reactivator
- #TP53 Y220C mutation
- #Phase 1 clinical trial
- Rezatapopt is an oral, selective p53 reactivator targeting Y220C-mutated p53.
- Phase 1 study involved 77 patients with TP53 Y220C-mutated solid tumors.
- Maximum tolerated dose was 1500 mg twice daily; recommended Phase 2 dose was 2000 mg once daily with food.
- 99% of patients experienced at least one adverse event, with nausea (58%) and vomiting (44%) being most common.
- Overall response rate was 20% (30% in KRAS wild-type patients receiving ≥1150 mg once daily).
- Confirmed responses observed in multiple tumor types, including ovarian and breast cancers.
- Study provides proof of concept for p53 reactivation therapy.