Precision Pipeline
FMC-242:
Preventing PI3Kα -RAS tumor signaling without impacting normal PI3Kα functions
FMC-242
FMC-242 is a covalent allosteric inhibitor that breaks the interaction between PI3Kα and RAS to inhibit downstream signaling in tumors without impacting normal functions such as glucose homeostasis. The mechanism of action inhibits PI3Kα signaling in tumors while minimizing the off-target effects and toxicities commonly associated with the broader class of kinase inhibitors.
Covalent fragments identified from the Frontier screening library were optimized leveraging the Frontier™ platform technology to deliver and PI3Kα-RAS breaker profile with unprecedented potency and selectivity along with optimal drug properties. FMC-242 has the potential to impact patients with lung, colorectal and breast cancers both as a single agent and in combination to combat drug resistance.