Definition

An orally bioavailable, brain penetrating, non-peptide neurokinin/tachykinin 3 receptor (NK1-receptor; NK3R; NK-3R) antagonist, that may potentially be used to treat vasomotor symptoms (VMS) in menopausal woman and in men on androgen deprivation therapy (ADT) and to suppress the production of certain hormones. Upon oral administration, osanetant targets, competitively binds to and blocks the activity of NK3R in the central nervous system (CNS), thereby inhibiting NK3R-mediated signal transduction and may prevent certain menopausal symptoms such as hot flashes and VMS in men deprived of androgen. Neurokinin-mediated signaling may increase during hormone deficiency and may cause hot flashes. In addition, osanetant may, by inhibiting NK3R, suppress secretion of various hormones, such as testosterone, luteinizing hormone (LH) and follicle-stimulating hormone (FSH). By suppressing testosterone production, osanetant may inhibit the proliferation of hormone-sensitive prostate cancer.