crenigacestat

Crenigacestat (LY3039478) is an orally bioavailable small molecule inhibitor of gamma-secretase, developed by Eli Lilly and Company for the treatment of various cancers. By inhibiting the gamma-secretase complex, crenigacestat prevents the proteolytic cleavage of Notch receptors, thereby blocking the release of the Notch intracellular domain (NICD) and subsequent activation of Notch-mediated gene transcription. This pathway is critical for cell fate determination, and its dysregulation is linked to tumor growth and survival in several solid and hematologic malignancies. Crenigacestat has been evaluated in Phase 1 and Phase 2 clinical trials as both a monotherapy and in combination with other targeted therapies or chemotherapies for advanced solid tumors, including adenoid cystic carcinoma and Notch-mutant cancers.

Other names

crenigacestatLY3039478LY-3039478LY 3039478