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 RAS driven PI3Kα-AKT signaling in tumors while minimizing the off-target effects and toxicities commonly associated with the broader class of kinase inhibitors.
In preclinical models, FMC-242 has shown potent anti-tumor activity demonstrating the potential to impact patients with lung, colorectal, breast and other cancers that are driven by RTK activation, RAS mutation and PI3Kα mutations either as a single-agent or in combination with other therapies including KRAS inhibitors.
PI3Kα
PI3Kα is the second most commonly mutated oncogene and plays an essential role in both KRAS- and RTK-driven cancers, such as colorectal, lung, and breast cancers, among others.