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BAY 1214784 is an orally available, potent, and selective small molecule antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). It was developed to lower plasma luteinizing hormone (LH) levels as a mechanism to manage hormone-driven symptoms of uterine fibroids. In first-in-human studies in postmenopausal women, once-daily treatment with BAY 1214784 effectively reduced plasma LH levels by up to 49% and demonstrated good tolerability with low pharmacokinetic variability. The drug was designed to address limitations of existing GnRH-R blockers that can induce menopausal symptoms and affect bone mineralization. The developer is Bayer.
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