Search Results - "Scheible, Holger"

Open-label, single-center, phase I trial to investigate the mass balance and absolute bioavailability of the highly selective oral MET inhibitor tepotinib in healthy volunteers by Johne, Andreas, Scheible, Holger, Becker, Andreas, van Lier, Jan Jaap, Wolna, Peter, Meyring, Michael

“…Summary Tepotinib (MSC2156119J) is an oral, potent, highly selective MET inhibitor. This open-label, phase I study in healthy volunteers (EudraCT…”
Get full text

Evobrutinib, a covalent Bruton’s tyrosine kinase inhibitor: Mass balance, elimination route, and metabolism in healthy participants by Scheible, Holger, Dyroff, Martin, Seithel‐Keuth, Annick, Harrison‐Moench, Eleanor, Mammasse, Nadra, Port, Andreas, Bachmann, Angelika, Dong, Jennifer, Lier, Jan Jaap, Tracewell, William, Mitchell, David

“…The highly selective, covalent Bruton’s tyrosine kinase inhibitor evobrutinib is under investigation for treatment of patients with multiple sclerosis (MS)…”
Get full text

Pharmacokinetics of ML3403 ({4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-Type p38 Mitogen-Activated Protein Kinase Inhibitor by KAMMERER, Bernd, SCHEIBLE, Holger, ALBRECHT, Wolfgang, GLEITER, Christoph H, LAUFER, Stefan

“…The p38 mitogen-activated protein kinase (MAPK) is a key mediator in cytokine-induced signaling events that are activated in response to a variety of…”
Get full text

Metabolism of the MEK1/2 Inhibitor Pimasertib Involves a Novel Conjugation with Phosphoethanolamine in Patients with Solid Tumors by Scheible, Holger, Kraetzer, Friedrich, Marx, Andreas, Johne, Andreas, Wimmer, Elmar

“…Pimasertib (AS703026 or MSC1936369B) is a selective inhibitor of MEK1/2, the mitogen-activated protein kinase (MAPK) signaling pathway, which is often…”
Get full text

Insights into Praziquantel Metabolism and Potential Enantiomeric Cytochrome P450-Mediated Drug-Drug Interaction by Vendrell-Navarro, Gloria, Scheible, Holger, Lignet, Floriane, Burt, Howard, Luepfert, Christian, Marx, Andreas, Abla, Nada, Swart, Piet, Perrin, Dominique

“…The active enantiomer R-Praziquantel (PZQ) shows a clinically lower relative exposure when administered enantiomerically pure compared with a racemic form. We…”
Get full text

Pimasertib, a selective oral MEK1/2 inhibitor: absolute bioavailability, mass balance, elimination route, and metabolite profile in cancer patients by Richter, Oliver, Massimini, Giorgio, Scheible, Holger, Udvaros, Istvan, Johne, Andreas

“…Aim This trial (NCT: 01713036) investigated the absolute bioavailability, mass balance and metabolite profile of pimasertib in a new design combining these…”
Get full text

Evobrutinib pathway to its major metabolite M463-2 and insights from a biotransformation and DDI perspective by Scheible, Holger, Schieferstein, Hanno, Schmidt, Ralf, Pusecker, Klaus, Gradhand, Ulrike, Gopalakrishnan, Sathej, Iqbal, Khalid, Dong, Jennifer, Jones, Reinaldo, Meli, Claudia, Bolleddula, Jayaprakasam, Dyroff, Martin, Georgi, Katrin

“…Evobrutinib is a highly selective, covalent, central nervous system-penetrant Bruton's tyrosine kinase (BTK) inhibitor, currently in Phase III trials for the…”
Get full text

A Decade in the MIST: Learnings from Investigations of Drug Metabolites in Drug Development under the "Metabolites in Safety Testing" Regulatory Guidance by Schadt, Simone, Bister, Bojan, Chowdhury, Swapan K, Funk, Christoph, Hop, Cornelis E C A, Humphreys, W Griffith, Igarashi, Fumihiko, James, Alexander D, Kagan, Mark, Khojasteh, S Cyrus, Nedderman, Angus N R, Prakash, Chandra, Runge, Frank, Scheible, Holger, Spracklin, Douglas K, Swart, Piet, Tse, Susanna, Yuan, Josh, Obach, R Scott

“…Since the introduction of metabolites in safety testing (MIST) guidance by the Food and Drug Administration in 2008, major changes have occurred in the…”
Get full text

Metabolism and disposition of the αv-integrin ß3/ß5 receptor antagonist cilengitide, a cyclic polypeptide, in humans by Becker, Andreas, von Richter, Oliver, Kovar, Andreas, Scheible, Holger, van Lier, Jan J., Johne, Andreas

“…Cilengitide (EMD 121974, manufactured by Merck KGaA, Darmstadt, Germany) is an αv‐integrin receptor antagonist showing high affinity for αvβ3 and αvβ5.This…”
Get full text

Comparison of the in vitro and in vivo metabolism of Cladribine (Leustatin, Movectro) in animals and human by Scheible, Holger, Laisney, Marc, Wimmer, Elmar, Javornik, Ana, Dolgos, Hugues

“…Abstract 1. New insight into the in vitro and in vivo metabolism of Cladribine (2-chloro-2′-deoxyadenosine, [2-CdA]) are presented. 2. Following incubation of…”
Get full text

Metabolism and disposition of the [alpha]v-integrin ß3/ß5 receptor antagonist cilengitide, a cyclic polypeptide, in humans by Becker, Andreas, von Richter, Oliver, Kovar, Andreas, Scheible, Holger, van Lier, Jan J, Johne, Andreas

“…Cilengitide (EMD 121974, manufactured by Merck KGaA, Darmstadt, Germany) is an [alpha]v-integrin receptor antagonist showing high affinity for [alpha]v[beta]3…”
Get full text

In vitro and in vivo drug disposition of cilengitide in animals and human by Dolgos, Hugues, Freisleben, Achim, Wimmer, Elmar, Scheible, Holger, Krätzer, Friedrich, Yamagata, Tetsuo, Gallemann, Dieter, Fluck, Markus

“…Cilengitide is very low permeable (1.0 nm/sec) stable cyclic pentapeptide containing an Arg‐Gly‐Asp motif responsible for selective binding to αvβ3 and αvβ5…”
Get full text

Pharmacokinetics of ML3403 ({4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3 H -imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-Type p38 Mitogen-Activated Protein Kinase Inhibitor by Kammerer, Bernd, Scheible, Holger, Albrecht, Wolfgang, Gleiter, Christoph H., Laufer, Stefan

Get full text

Overexpression, purification and characterization of SimL, an amide synthetase involved in simocyclinone biosynthesis by LUFT, Thomas, LI, Shu-Ming, SCHEIBLE, Holger, KAMMERER, Bernd, HEIDE, Lutz

“…Simocyclinone D8 is a potent inhibitor of bacterial gyrase, produced by Streptomyces antibioticus Tu 6040. It contains an aminocoumarin moiety, similar to that…”
Get full text