Michaela Bairlein

Predicting in vitro assays related to liver function using probabilistic machine learning

Flavio M. Morelli, Marian Raschke, Natalia A. Jungmann, Michaela Bairlein et autres

de (code pays fourni par la source)

Abstract C126: Translational pharmacokinetic/pharmacodynamic (PK/PD) modeling of novel covalent Kelch-like ECH-associated protein 1 (KEAP1) activators

Conrad Housand, Nil Roy, Tine L Wyseure, Christie L. Eissler et autres

Abstract Introduction: The KEAP1-nuclear factor erythroid 2-related factor 2 (NRF2) signaling axis is a key homeostatic mechanism for cells to maintain redox balance. In oxidative stress, reactive oxygen species (ROS) modify residues on KEAP1, impairing its binding and ubiquitination of NRF2. This …

us (code pays fourni par la source)

In vivo Metabolism of Nifurtimox and the Drug-Drug Interaction Potential Including its Major Metabolites

Simone I. Schulz, Dieter H. Lang, Gabriele Schmuck, Michael Gerisch et autres

Background: Nifurtimox is an effective treatment for patients with Chagas disease, but knowledge of its biotransformation and excretion is limited. Objective: This study aimed to better understand the fate of oral nifurtimox in vivo. Methods: We investigated the exposure and excretion pathways …

de (code pays fourni par la source)

CCDC 1906048: Experimental Crystal Structure Determination

Martina Schaefer, Hartmut Beck, Raimund Kast, Tobias Thaler et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Potent and Selective Human Prostaglandin F (FP) Receptor Antagonist (BAY-6672) for the Treatment of Idiopathic Pulmonary Fibrosis (IPF)

Hartmut Beck, Tobias Thaler, Daniel Meibom, Mark Meininghaus et autres

Abstract Idiopathic pulmonary fibrosis (IPF) is a rare and devastating chronic lung disease of unknown etiology. Despite the approved treatment options nintedanib and pirfenidone, the medical need for a safe and well-tolerated antifibrotic treatment of IPF remains high. The human prostaglandin F …

de (code pays fourni par la source)

Results from Drug–Drug Interaction Studies In Vitro and In Vivo Investigating the Effect of Finerenone on the Pharmacokinetics of Comedications

Roland Heinig, Michael Gerisch, Michaela Bairlein, Johannes Nagelschmitz et autres

de (code pays fourni par la source)

Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N -[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile

Stefan Werner, Stefanie Mesch, Roman Christian Hillig, Antonius ter Laak et autres

The P2X4 receptor is a ligand-gated ion channel that is expressed on a variety of cell types, especially those involved in inflammatory and immune processes. High-throughput screening led to a new class of P2X4 inhibitors with substantial CYP 3A4 induction in human …

de (code pays fourni par la source)

Drug–Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies

Christian Zurth, Mikko Koskinen, Robert E. Fricke, Olaf Prien et autres

BACKGROUND AND OBJECTIVES: Darolutamide is a novel androgen receptor (AR) antagonist approved for the treatment of nonmetastatic castration-resistant prostate cancer (nmCRPC). Accordingly, the drug-drug interaction (DDI) potential of darolutamide was investigated in both nonclinical and clinical studies. METHODS: In vitro studies were …

de, fi (code pays fourni par la source)

Highly Variable Expression of CYP1A1 in Human Liver and Impact on Pharmacokinetics of Riociguat and Granisetron in Humans

Dieter H. Lang, Martin Radtke, Michaela Bairlein

Cytochrome P450s (CYPs), a superfamily of enzymes, are involved in the biotransformation of endogenous and xenobiotic chemicals and mainly responsible for the metabolic clearance of widely prescribed drugs. Out of the 57 human isoforms, only a few, most notably CYP3A4, are considered …

de (code pays fourni par la source)

Current Approaches for Absorption, Distribution, Metabolism, and Excretion Characterization of Antibody-Drug Conjugates: An Industry White Paper

Eugenia A. Kraynov, Markus Walles, Edit Tarcsa, Antoine Deslandes et autres

ch, us, gb, fr, de (code pays fourni par la source)

Characterization of the small molecule kinase inhibitor SU11248 (Sunitinib/ SUTENT) in vitro and in vivo

Michaela Bairlein

SU11248 is a multitargeted kinase inhibitor approved for the treatment of metastatic renal cell carcinoma and gastrointestinal stromal tumors. For an optimal clinical impact of the drug and its precise response prediction in patients including adverse side-effects, drug target interaction profiles and …

Proteomics strategy for quantitative protein interaction profiling in cell extracts

Kirti Sharma, Christoph K. Weber, Michaela Bairlein, Zoltán Greff et autres

de, hu (code pays fourni par la source)