Zobrazeno 1 - 10
of 56
pro vyhledávání: '"Kunze, A"'
Publikováno v:
Drug Metabolism and Disposition. 42:1514-1521
Organic anion-transporting polypeptides (OATP) 1B1 and OATP1B3 are drug transporters mediating the active hepatic uptake of their substrates. Because they exhibit overlapping substrate specificities, the contribution of each isoform to the net hepati
Autor:
Cornelia Boerger, Gudrun Ott, Ingolf Cascorbi, Florian Bittner, Bernd Clement, Thomas Kunze, Antje Havemeyer, Debora Reichmann, Ralf-Rainer Mendel
Publikováno v:
Drug Metabolism and Disposition. 42:718-725
Human molybdenum-containing enzyme mitochondrial amidoxime reducing component (mARC), cytochrome b5 type B, and NADH cytochrome b5 reductase form an N-reductive enzyme system that is capable of reducing N-hydroxylated compounds. Genetic variations ar
Autor:
Justin D. Lutz, Wendel L. Nelson, Katipudi N. Babu, Brooke M. VandenBrink, Nina Isoherranen, Kent L. Kunze
Publikováno v:
Drug Metabolism and Disposition. 41:2056-2065
Recent guidance on drug-drug interaction (DDI) testing recommends evaluation of circulating metabolites. However, there is little consensus on how to quantitatively predict and/or assess the risk of in vivo DDIs by multiple time-dependent inhibitors
Autor:
Jun O. Liu, Wei Shi, Wendel L. Nelson, Justin D. Lutz, Nina Isoherranen, Kent L. Kunze, Chi Chi Peng
Publikováno v:
Drug Metabolism and Disposition. 40:426-435
Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. However, (2R,4S,2'R)-ITZ and (2R,4S,2'S)-ITZ also undergo stereoselective sequential metabolism by CYP3A4 at
Autor:
Kelsey L. Hanson, Kyle E. Allen, Brooke M. VandenBrink, Wendel L. Nelson, Kent L. Kunze, Kantipudi N. Babu
Publikováno v:
Drug Metabolism and Disposition. 38:963-972
Three secondary amines desipramine (DES), (S)-fluoxetine [(S)-FLX], and N-desmethyldiltiazem (MA) undergo N-hydroxylation to the corresponding secondary hydroxylamines [N-hydroxydesipramine, (S)-N-hydroxyfluoxetine, and N-hydroxy-N-desmethyldiltiazem
Publikováno v:
Drug Metabolism and Disposition. 33:853-861
Irreversible CYP3A inhibition by drugs constitutes one of the major causes of inhibition-based drug interactions. We evaluated time-dependent inactivation of CYP3A in cryopreserved human hepatocytes for six structurally diverse compounds known to exh
Publikováno v:
Drug Metabolism and Disposition. 32:1083-1091
Publikováno v:
Drug Metabolism and Disposition. 32:1121-1131
Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. However, unbound plasma concentrations of ITZ are much lower than its reported in vitro Ki, and no clinically significant interactions would be expected based on a reversible mechanism of inh
Publikováno v:
Drug Metabolism and Disposition. 31:1043-1048
The goal of the study was to test the assumption that a competitive inhibition constant determined in vivo, Kiiv, like its corresponding in vitro counterpart, Ki, is independent of inhibitor concentration. Inhibition of the CYP2C9-dependent formation
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