HRS-4642

HRS-4642 is a highly selective, high-affinity, long-acting, non-covalent small molecule inhibitor targeting the oncogenic KRAS G12D mutation. It demonstrates potent anti-tumor activity in preclinical models and early clinical trials for cancers harboring the KRAS G12D mutation, which is one of the most common and challenging mutations in solid tumors such as pancreatic cancer. The drug binds to KRAS G12D with an affinity constant (Kd) of 0.083 nM and has shown robust efficacy both as a single agent and in combination with other therapies (e.g., proteasome inhibitors like carfilzomib or monoclonal antibodies such as nimotuzumab). In addition to direct tumor inhibition, HRS-4642 can modulate the tumor microenvironment toward an immune-permissive state[3][5][6].

Other names

KRAS G12D inhibitor HRS-4642