Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite positions in the ring. The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. Pyrimidines and piperazines are known to be the backbone of many bulk compounds and important core structures for approved drugs; studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity.
Merck initiates Phase 3 clinical trial of MK-1084, an investigational oral KRAS G12C inhibitor, in combination with KEYTRUDA® (pembrolizumab) for first-line treatment of certain patients with metastatic non-small cell lung cancer. KRAS mutations are one of the most frequently observed mutations in human cancers, making them a crucial target for precision oncology therapy.
MK-1084 is an investigational, oral covalent inhibitor of KRAS G12C, that is found in about 14% of people with non-small cell lung cancer. MK-1084 is currently under Phase 1 evaluation as monotherapy and as combined therapies in patients with KRAS G12C mutant advanced solid tumors.