Description
InformationRelugolix Relugolix (RVT-601, TAK-385) is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.Targetsmonkey GnRHR (Cell-free assay); human GnRHR (Cell-free assay) 0.32 nM; 0.33 nMIn vitroRelugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM).In vivoTAK-385 acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis