setidegrasib

Setidegrasib (ASP3082) is a first-in-class, selective protein degrader developed by Astellas Pharma that specifically targets the KRAS G12D mutation. Unlike traditional small molecule inhibitors that block protein function, setidegrasib utilizes targeted protein degradation (TPD) technology to facilitate the degradation of the mutant KRAS protein. It is primarily being developed for the treatment of KRAS G12D-mutated solid tumors, with a focus on metastatic pancreatic ductal adenocarcinoma, non-small cell lung cancer, and colorectal cancer. Clinical development includes a pivotal Phase 3 study evaluating setidegrasib in combination with chemotherapy (mFOLFIRINOX or NALIRIFOX) as a first-line treatment for pancreatic cancer.

Other names

KRAS G12D degrader ASP3082