1 October 2025 - Ensem Therapeutics today announced the US FDA granted fast track designation to its clinical stage pan mutant-specific allosteric PI3Kα inhibitor and degrader, ETX-636, for the treatment of adult patients with PIK3CA mutant, hormone receptor positive, human epidermal growth factor negative advanced breast cancer.
ETX-636 was designed using ENSEM’s unique Kinetic Ensemble platform to optimally fit into a specific allosteric binding site in p110α, the catalytic subunit of PI3Kα and can selectively inhibit multiple activating mutant forms of PI3Kα, while sparing wild type PI3Kα.