fezolinetant

An orally bioavailable, neurokinin/tachykinin 3 receptor (NK1-receptor; NK3R; NK-3R) antagonist, that can be used to treat vasomotor symptoms (VMS) in menopausal woman. Upon oral administration, fezolinetant targets, competitively binds to and blocks the activity of NK3R in the central nervous system (CNS). Specifically, this blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDgamma) neuron in the thermoregulatory center and inhibits NK3R-mediated signal transduction. This prevents VMS. Neurokinin-mediated signaling may increase during hormone deficiency and may cause VMS.