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Drug metabolism in hepatocyte sandwich cultures of rats and humans.
Rat and human hepatocytes preserve the major forms of CYP isozymes and phase I and phase II activities and respond to inducing drugs such as rifampicin, demonstrating that the novel hepatocyte sandwich culture is suitable for investigating drug metabolism, drug-drug interactions and enzyme induction.
Metabolism of cerivastatin by human liver microsomes in vitro. Characterization of primary metabolic pathways and of cytochrome P450 isozymes involved.
Upon incubation of cerivastatin with human liver microsomes in the presence of the specific CYP3A inhibitor TAO, both hydroxylation and demethylation were considerably reduced, indicating that CYP 3A enzymes play a major role in cerivastsatin metabolism.
Rhizocticin A, an antifungal phosphono-oligopeptide of Bacillus subtilis ATCC 6633: biological properties
Rhizocticin A, the main component of the antifungal, hydrophilic phosphono-oligopeptides of Bacillus subtilis ATCC 6633, was used for sensitivity testing and experiments into the molecular mechanism
Discovery of Riociguat (BAY 63‐2521): A Potent, Oral Stimulator of Soluble Guanylate Cyclase for the Treatment of Pulmonary Hypertension
Direct stimulation of soluble guanylate cyclase with Optimization of the unfavorable DMPK profile of previous sGC stimulators provided riociguat, which is currently being investigated in phase’III clinical trials for the oral treatment of PH.
Biotransformation of cerivastatin in mice, rats, and dogs in vivo.
Biotransformation of cerivastatin was investigated in mice, rats, and dogs in vivo using the 14C-labeled drug. Marked species differences exist, both in pathways and extent of cerivastatin
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.
These studies resulting in the discovery of once daily sGC stimulator vericiguat (compound 24, BAY 1021189), currently in phase 3 trials for chronic heart failure, are reported.
The use of Long-term Hepatocyte Cultures for Detecting Induction of Drug Metabolising Enzymes: The Current Status
A prevalidation proposal for the use of the collagen gel sandwich hepatocyte culture system for drug metabolising enzyme induction was designed, focusing on the induction of the cytochrome P450 enzymes as the principal enzymes of interest.
Metabolic products from microorganisms. 230. Amiclenomycin-peptides, new antimetabolites of biotin. Taxonomy, fermentation and biological properties.
Four new and two known peptide antibiotics containing amiclenomycin (Acm) have been isolated from a culture of Streptomyces venezuelae Tü 2460 and are presented here as examples for the illicit transport concept.
Discovery of the Soluble Guanylate Cyclase Activator Runcaciguat (BAY 1101042).
The discovery, mode of action, and preclinical characterization of the soluble guanylate cyclase (sGC) activator runcaciguat is described, which is currently investigated in clinical phase 2 studies for the treatment of patients with chronic kidney disease and nonproliferative diabetic retinopathy.
Metabolites of orally active NO-independent pyrazolopyridine stimulators of soluble guanylate cyclase.
The pyrazolopyridine stimulators of soluble guanylate cyclase Bays 41-2272 and 41-8543 were oxidised in rats and dogs at their 5-pyrimidinyl-cyclopropyl and -morpholino residue and thereby may contribute to the in vivo activity of BAY 41- 2272 and BAY 8543.