RLY-2608 — Investigational Agent
PI3K Inhibitor · Phase 1/2 · Relay Therapeutics
Mechanism of Action
First-in-class oral, mutant-selective, allosteric pan-mutant PI3Kα inhibitor. Exploits a conformational allosteric site to inhibit both kinase-domain (H1047X) and helical-domain (E542X/E545X) PIK3CA mutants while sparing wild-type PI3Kα, minimizing on-target metabolic toxicity (hyperglycemia).
Investigational Indications
- PIK3CA-mutant HR+/HER2- advanced breast cancer
- PIK3CA-mutant advanced solid tumors
- PIK3CA-related overgrowth spectrum (separate program)