adagrasib + palbociclib

**adagrasib + palbociclib** is an investigational, orally administered combination of two small molecule inhibitors for the treatment of solid tumors harboring KRAS G12C mutations. Adagrasib is a covalent inhibitor of KRAS G12C, selectively and irreversibly binding to and disabling this mutated oncogene, which is implicated in driving cell proliferation and survival in many cancers. Palbociclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), thereby inducing cell cycle arrest at G1/S phase. The combination is being developed to exploit potential synergy by simultaneously targeting the KRAS-driven MAPK signaling pathway and the downstream CDK4/6-mediated cell cycle machinery. In the KRYSTAL-16 (NCT05178888) phase I/Ib trial, the combination is being evaluated for safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy in patients with advanced cancers harboring KRAS G12C mutations who have received at least one prior standard therapy[1][3][4][5].

Brand names

Kisqali

Other names

adagrasib + palbociclibMRTX849 + palbociclib