Lirafugratinib — Investigational Agent
FGFR Inhibitor · Phase 1/2 · Relay Therapeutics
Mechanism of Action
Highly selective, irreversible (covalent) inhibitor of FGFR2, engineered to spare FGFR1, FGFR3, and FGFR4. This selectivity is designed to avoid the off-target toxicities of pan-FGFR inhibitors — notably FGFR1-driven hyperphosphatemia and FGFR4-driven diarrhea — while achieving deep, sustained FGFR2 inhibition and retaining activity against several FGFR2 resistance mutations.
Investigational Indications
- FGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma
- FGFR2-altered advanced solid tumors (including breast, gastric, pancreatic)