garsorasib + AST2169

Garsorasib + AST2169 is an investigational combination therapy being developed by Elis Pharmaceutical Technology (Allist) for the treatment of non-small cell lung cancer (NSCLC) harboring the KRAS G12C mutation. Garsorasib (D-1553) is a potent, selective, and orally bioavailable small molecule that covalently binds to the cysteine residue of the KRAS G12C mutant protein, locking it in its inactive GDP-bound state. AST2169 is a small molecule inhibitor of SHP2 (Src homology region 2 domain-containing phosphatase 2), a protein tyrosine phosphatase that plays a critical role in the RAS/MAPK signaling pathway by mediating signals from various receptor tyrosine kinases. The combination aims to achieve deeper and more durable responses by simultaneously inhibiting the mutant KRAS protein and blocking the SHP2-mediated feedback loops that often lead to adaptive resistance against KRAS G12C monotherapy. It is currently being evaluated in Phase 1 clinical trials as a first-line treatment for KRAS G12C-mutant NSCLC.

Other names

戈来雷塞 + SHP2 inhibitorgarsorasib + SHP2 inhibitorGarsorasib + SHP2 inhibitor-Elis Pharmaceutical Technology-KRAS G12C-SHP2-small molecule combination-NSCLC (KRAS G12C mutation, 1st line)