Bezuclastinib — Investigational Agent
KIT Inhibitor · Phase 3 · Cogent Biosciences
Mechanism of Action
Selective, potent small-molecule inhibitor of mutant KIT, designed to target activation-loop mutations (KIT exon 17/18, e.g., D816V and D820/N822 substitutions) that drive resistance to earlier KIT TKIs. It has minimal activity against wild-type KIT-related kinases (e.g., PDGFR, VEGFR/KDR), aiming to reduce off-target toxicity. Poor CNS penetration is intended to limit CNS-mediated adverse effects.
Investigational Indications
- Gastrointestinal stromal tumor (GIST), including in combination with sunitinib
- Advanced/aggressive systemic mastocytosis (separate program)