• Ensem Therapeutics received FDA clearance for ETX-636, a first-in-class allosteric pan-mutant-selective PI3Kα inhibitor and degrader, with clinical trials set to begin in Q2 2025 for patients with PI3Kα-mutated tumors.
• ETX-636 selectively targets mutant PI3Kα while sparing wildtype PI3Kα, potentially avoiding hyperglycemia that limits current PI3Kα inhibitors, addressing a significant challenge in treating HR+/HER2- breast cancers.
• The upcoming Phase 1/2 trial will evaluate ETX-636 as monotherapy and in combination with fulvestrant in advanced solid tumors, with preclinical data to be presented at the AACR Annual Meeting on April 28, 2025.