BAY-899 is an orally active and selective antagonist of the luteinizing hormone receptor (LH-R), exhibiting IC50 values of 185 nM and 46 nM for human LH (hLH) and rat LH (rLH) respectively. In vivo studies have demonstrated that BAY-899 effectively reduces sex hormone levels[1].

LH (human):185 nM , LH (rat):46nM

BAY-899 (oral; 12.5 mg/kg/day; for 8 days) exhibits an efficiency to reduce serum estradiol levels in intact female rats [1]. BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t 1/2 of 11 hours and 12 hours for iv and po. And the C max is 0.97 kg/L and 0.24 kg/L for iv and po [1]. Animal Model: Intact female rats [1] Dosage: 12.5 mg/kg Administration: Oral; for 8 days Result: Showed an efficiency to reduce serum estradiol levels. Animal Model: Female and male Wistar rats [1] Dosage: 0.5 mg/kg of iv or 2 mg/kg of po Administration: Iv or po Result: Has t 1/2 s of 11 hours and 12 hours for iv and po. And the C max s are 0.97 kg/L and 0.24 kg/L for iv and po.