sitneprotafib

Sitneprotafib (JAB-3312) is a highly selective, orally administered small molecule allosteric inhibitor of SHP2 (protein tyrosine phosphatase non-receptor type 11, PTPN11). Developed by Jacobio Pharmaceuticals, it targets and inhibits SHP2 activity by binding to an allosteric site on the protein. This inhibition blocks the RTK/RAS/MAPK signaling pathway, suppresses tumor cell growth and proliferation—especially in tumors driven by RTK or with KRAS, BRAF Class 3, or NF1 loss-of-function mutations—and enhances anti-tumor immunity by blocking PD-1 signaling and reducing immunosuppression in the tumor microenvironment. Sitneprotafib has demonstrated high potency in preclinical models and is currently being evaluated in multiple clinical trials for various solid tumors including non-small cell lung cancer and esophageal cancer. It has received orphan drug designation for esophageal cancer from the US FDA.

Other names

CSC-884CSC884CSC 884