Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women
Olaf Panknin, Andrea Wagenfeld, Wilhelm Bone, Eckhard Bender, Katrin Nowak‐Reppel, Amaury E. Fernández‐Montalván, Reinhard Nubbemeyer, Stefan Bäurle, Sven Ring, Norbert Schmees, Olaf Prien, Martina Schäfer, Christian Friedrich, Thomas M. Zollner, Andreas Steinmeyer, Thomas Mueller, Gernot Langer
Abstract
. In a first-in-human study in postmenopausal women, once daily treatment with BAY 1214784 effectively lowered plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability.
Topics & Concepts
AntagonistHormoneLuteinizing hormoneChemistryGonadotropin-releasing hormone receptorEstrogenPharmacologyHormone receptorEndocrinologyInternal medicineTolerabilityEstrogen receptorReceptorGonadotropin-releasing hormoneMedicineAdverse effectCancerBreast cancerEstrogen and related hormone effectsUterine Myomas and TreatmentsHypothalamic control of reproductive hormones