BPI-442096

BPI-442096 is a novel, potent, and highly selective oral small molecule inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP2). It was developed by Betta Pharmaceuticals and is being co-developed with Xcovery. The drug specifically targets the SHP2 protein's variable configuration site, inhibiting its activation. By blocking SHP2 activity, BPI-442096 disrupts downstream signaling pathways such as RAS-MAPK and PD-L1/PD-1, which are critical for tumor cell proliferation, growth, survival, motility, and metabolism. This mechanism ultimately leads to inhibition of tumor growth. Preclinical studies have shown significant activity against various cancer cells harboring mutations including KRAS G12C/D/V/A mutations, BRAF Class III mutation, NF1 loss-of-function mutation, and RTK mutations. The drug is currently in Phase 1 clinical trials for advanced solid tumors in both China and the United States.