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 recently announces the initiation of the pivotal Phase 3 randomized MK-3543-006 clinical trial of Bomedemstat for Essential Thrombocythemia (ET). Lysine-specific demethylase 1 (LSD1) is critical for the regulation of hematopoietic stem and progenitor cells. Bomedemstat is an investigational small molecule irreversible inhibitor of LSD1 by suppressing progenitor cells during blood cell maturation. It is generally well tolerated in ET patients and demonstrates significant clinical activity as a monotherapy.
Bomedemstat has been granted Orphan Drug and Fast Track Designation for the treatment of ET and myelofibrosis (MF) by the U.S. FDA.