Search Results - "Rottmann, Antje"

Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis by Bäurle, Stefan, Nagel, Jens, Peters, Olaf, Bräuer, Nico, ter Laak, Antonius, Preusse, Cornelia, Rottmann, Antje, Heldmann, Dieter, Bothe, Ulrich, Blume, Thorsten, Zorn, Ludwig, Walter, Daryl, Zollner, Thomas M, Steinmeyer, Andreas, Langer, Gernot

“…The presence and growth of endometrial tissue outside the uterine cavity in endometriosis patients are primarily driven by hormone-dependent and inflammatory…”
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Discovery of Vilaprisan (BAY 1002670): A Highly Potent and Selective Progesterone Receptor Modulator Optimized for Gynecologic Therapies by Möller, Carsten, Bone, Wilhelm, Cleve, Arwed, Klar, Ulrich, Rotgeri, Andrea, Rottmann, Antje, Schultze‐Mosgau, Marcus‐Hillert, Wagenfeld, Andrea, Schwede, Wolfgang

“…Progesterone plays an important role in the female reproductive system. However, there is also evidence that gynecologic disorders/diseases such as uterine…”
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Hepatotoxicity of AKR1C3 Inhibitor BAY1128688: Findings from an Early Terminated Phase IIa Trial for the Treatment of Endometriosis by Hilpert, Jan, Groettrup-Wolfers, Esther, Kosturski, Hristiyan, Bennett, Laura, Barnes, Catriona L. K., Gude, Kerstin, Gashaw, Isabella, Reif, Stefanie, Steger-Hartmann, Thomas, Scheerans, Christian, Solms, Alexander, Rottmann, Antje, Mao, Guangping, Chapron, Charles

“…Introduction BAY1128688 is a selective inhibitor of aldo-keto reductase family 1 member C3 (AKR1C3), an enzyme implicated in the pathology of endometriosis and…”
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The Starch-Related R1 Protein is an α-Glucan, Water Dikinase by Ritte, Gerhard, Lloyd, James R., Eckermann, Nora, Rottmann, Antje, Kossmann, Jens, Steup, Martin

“…To determine the enzymatic function of the starch-related R1 protein it was heterologously expressed in Escherichia coli and purified to apparent homogeneity…”
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Metabolism and Disposition of Vatalanib (PTK787/ZK-222584) in Cancer Patients by JOST, Lorenz M, GSCHWIND, Hans-Peter, MASSON, Eric, LAURENT, Dirk, JALAVA, Tarja, YONGYU WANG, GUENTHER, Clemens, SOUPPART, Claire, ROTTMANN, Antje, DENNER, Karsten, WALDMEIER, Felix, GROSS, Gerhard

“…Vatalanib (PTK787/ZK-222584) is a new oral antiangiogenic molecule that inhibits all known vascular endothelial growth factor receptors. Vatalanib is under…”
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Pharmacokinetics, Safety, and Tolerability of the Novel Tetrameric, High-Relaxivity, Macrocyclic Gadolinium-Based Contrast Agent Gadoquatrane in Healthy Adults by Hofmann, Birte Maria, Riecke, Kai, Klein, Stefan, Berse, Matthias, Rottmann, Antje, Sutter, Gabriele, Ebert, Wolfgang

“…Gadolinium (Gd)-based contrast agents are well established in clinical routine and have been proven safe and effective. However, there is a need for…”
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Preclinical and Clinical Pharmacokinetics and Bioavailability in Healthy Volunteers of a Novel Formulation of the Selective P2X3 Receptor Antagonist Eliapixant by Francke, Klaus, Chattopadhyay, Niladri, Klein, Stefan, Rottmann, Antje, Krickau, Dennis, van de Wetering, Jeroen, Friedrich, Christian

“…Background and Objectives The potent, selective P2X3 receptor antagonist eliapixant (BAY 1817080) is under development for conditions characterized by neuronal…”
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Quantitative Systems Toxicology Identifies Independent Mechanisms for Hepatotoxicity and Bilirubin Elevations Due to AKR1C3 Inhibitor BAY1128688 by Battista, Christina, Shoda, Lisl K.M., Watkins, Paul B., Groettrup‐Wolfers, Esther, Rottmann, Antje, Raschke, Marian, Generaux, Grant T.

“…BAY1128688 is a selective inhibitor of AKR1C3, investigated recently in a trial that was prematurely terminated due to drug‐induced liver injury. These…”
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Clinical Pharmacokinetics and Pharmacodynamics of the Selective Progesterone Receptor Modulator Vilaprisan: A Comprehensive Overview by Schultze-Mosgau, Marcus-Hillert, Ploeger, Bart A., Frei, Matthias, Höchel, Joachim, Rottmann, Antje

“…Vilaprisan is a highly potent selective progesterone receptor modulator in development for the treatment of symptomatic uterine fibroids and endometriosis. Its…”
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Novel aldo-keto reductase 1C3 inhibitor affects androgen metabolism but not ovarian function in healthy women: a phase 1 study by Gashaw, Isabella, Reif, Stefanie, Wiesinger, Herbert, Kaiser, Andreas, Zollmann, Frank S, Scheerans, Christian, Grevel, Joachim, Piraino, Paolo, Seidel, Henrik, Peters, Michaele, Rottmann, Antje, Rohde, Beate, Arlt, Wiebke, Hilpert, Jan

“…Aldo-keto reductase 1C3 (AKR1C3) has been postulated to be involved in androgen, progesterone, and estrogen metabolism. Aldo-keto reductase 1C3 inhibition has…”
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The Effects of Weak and Strong CYP3A Induction by Rifampicin on the Pharmacokinetics of Five Progestins and Ethinylestradiol Compared to Midazolam by Wiesinger, Herbert, Klein, Stefan, Rottmann, Antje, Nowotny, Bettina, Riecke, Kai, Gashaw, Isabella, Brudny‐Klöppel, Margarete, Fricke, Robert, Höchel, Joachim, Friedrich, Christian

“…It is known that co‐administration of CYP3A inducers may decrease the effectiveness of oral contraceptives containing progestins as mono‐preparations or…”
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Characterization of the Pharmacokinetics of Vilaprisan: Bioavailability, Excretion, Biotransformation, and Drug–Drug Interaction Potential by Schultze-Mosgau, Marcus-Hillert, Höchel, Joachim, Prien, Olaf, Zimmermann, Torsten, Brooks, Ashley, Bush, Jim, Rottmann, Antje

“…Background and objectives In-vitro data suggest that clearance of vilaprisan is mediated by cytochrome P450 3A4 (oxidation) and aldoketoreductases (reduction)…”
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A Novel NAMPT Inhibitor-Based Antibody–Drug Conjugate Payload Class for Cancer Therapy by Böhnke, Niels, Berger, Markus, Griebenow, Nils, Rottmann, Antje, Erkelenz, Michael, Hammer, Stefanie, Berndt, Sandra, Günther, Judith, Wengner, Antje M., Stelte-Ludwig, Beatrix, Mahlert, Christoph, Greven, Simone, Dietz, Lisa, Jörißen, Hannah, Barak, Naomi, Bömer, Ulf, Hillig, Roman C., Eberspaecher, Uwe, Weiske, Jörg, Giese, Anja, Mumberg, Dominik, Nising, Carl Friedrich, Weinmann, Hilmar, Sommer, Anette

“…Inhibition of intracellular nicotinamide phosphoribosyltransferase (NAMPT) represents a new mode of action for cancer-targeting antibody–drug conjugates (ADCs)…”
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Discovery of the potent non-steroidal glucocorticoid receptor modulator BAY 1003803 as clinical candidate by Berger, Markus, May, Ekkehard, Rehwinkel, Hartmut, Schäcke, Heike, Neuhaus, Roland, Rottmann, Antje, Zollner, Thomas M., Jaroch, Stefan

“…[Display omitted] We report on the discovery of the new clinical candidate BAY 1003803 as glucocorticoid receptor agonist for the topical treatment of…”
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Mass Balance and Metabolic Pathways of Eliapixant, a P2X3 Receptor Antagonist, in Healthy Male Volunteers by Reif, Stefanie, Schultze-Mosgau, Marcus-Hillert, Engelen, Anna, Piel, Isabel, Denner, Karsten, Roffel, Ad, Tiessen, Renger, Klein, Stefan, Francke, Klaus, Rottmann, Antje

“…Background Overactive adenosine triphosphate signaling via P2X3 homotrimeric receptors is implicated in multiple conditions. To fully understand the metabolism…”
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CYP3A4‐mediated effects of rifampicin on the pharmacokinetics of vilaprisan and its UGT1A1‐mediated effects on bilirubin glucuronidation in humans by Chattopadhyay, Niladri, Kanacher, Tobias, Casjens, Manuela, Frechen, Sebastian, Ligges, Sandra, Zimmermann, Torsten, Rottmann, Antje, Ploeger, Bart, Höchel, Joachim, Schultze‐Mosgau, Marcus‐Hillert

“…Aims The primary aim of the present study was to quantify the effects of rifampicin, a strong cytochrome P450 (CYP) 3A4 inducer, on the pharmacokinetics of the…”
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Abstract 2907: Identification and optimization of a novel NAMPT inhibitor-based ADC payload class for cancer therapy by Böhnke, Niels, Berger, Markus, Griebenow, Nils, Giese, Anja, Günther, Judith, Sommer, Anette, Hammer, Stefanie, Berndt, Sandra, Wengner, Antje M., Beier, Rudolf, Stelte-Ludwig, Beatrix, Mahlert, Christoph, Greven, Simone, Dietz, Lisa, Joerissen, Hannah, Rottmann, Antje, Erkelenz, Michael, Barak, Naomi, Bömer, Ulf, Mumber, Dominik, Kreft, Bertolt, Linden, Lars, Nising, Carl Friedrich, Weinmann, Hilmar

“…Abstract Inhibition of intracellular nicotinamide phosphoribosyltransferase (NAMPT) represents a differentiated mode-of-action for tumor-targeting…”
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Front Cover: Discovery of Vilaprisan (BAY 1002670): A Highly Potent and Selective Progesterone Receptor Modulator Optimized for Gynecologic Therapies (ChemMedChem 21/2018) by Möller, Carsten, Bone, Wilhelm, Cleve, Arwed, Klar, Ulrich, Rotgeri, Andrea, Rottmann, Antje, Schultze‐Mosgau, Marcus‐Hillert, Wagenfeld, Andrea, Schwede, Wolfgang

“…The Front Cover shows vilaprisan, a highly selective progesterone receptor modulator (SPRM), bound to the progesterone receptor (PR). Gynecologic diseases such…”
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Determination of rat serum esterase activities by an HPLC method using S-acetylthiocholine iodide and p-nitrophenyl acetate by Koitka, Matthias, Höchel, Joachim, Obst, Detlev, Rottmann, Antje, Gieschen, Hille, Borchert, Hans-Hubert

“…Establishing esterase assays allows the determination and comparison of esteratic activities of tissues of one organism and between organisms. We have…”
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Plasma Pharmacokinetics, Whole-Body Distribution, Metabolism, and Radiation Dosimetry of 68 Ga Bombesin Antagonist BAY 86-7548 in Healthy Men by Roivainen, Anne, Kähkönen, Esa, Luoto, Pauliina, Borkowski, Sandra, Hofmann, Birte, Jambor, Ivan, Lehtiö, Kaisa, Rantala, Tuija, Rottmann, Antje, Sipilä, Henri, Sparks, Rick, Suilamo, Sami, Tolvanen, Tuula, Valencia, Ray, Minn, Heikki

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