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.
Roche’s investigational drug, Fenebrutinib has shown brain penetration and significant reduction in lesions in patients with relapsing multiple sclerosis (MS) from the recent release of new data from Phase II FENopta study. Fenebrutinib is a potent and highly selective Bruton’s tyrosine kinase (BTK) inhibitor, and currently the only reversible inhibitor being tested in Phase III MS trials. BTK inhibitor is involved in key pathological features of MS, including B-cell development and activation.
Dec. 26, 2023, Amgen announced that the U.S. FDA has completed its review of the company's supplemental New Drug Application seeking full approval of LUMAKRAS (sotorasib).
LUMAKRAS (sotorasib) is an oral, first-in-class therapy indicawithted for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) following at least one previous systemic therapy.
Sotorasib is the first approved targeted therapy for patients with tumors with any KRAS mutation, which accounts for approximately 25% of mutations in NSCLC. The U.S. FDA granted the application for sotorasib orphan drug, fast track, priority review, and breakthrough therapy designations.