In vitro identification of the human cytochrome p450 enzymes involved in the oxidative metabolism of loxapine

2011 ◽  
Vol 32 (7) ◽  
pp. 398-407 ◽  
Author(s):  
Jiang Ping Luo ◽  
Sarvesh C. Vashishtha ◽  
Edward M. Hawes ◽  
Gordon McKay ◽  
Kamal K. Midha ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Oxidative Metabolism ◽  
Cytochrome P450 Enzymes ◽  
Human Cytochrome

scholarly journals Metabolism and Disposition of Siponimod, a Novel Selective S1P1/S1P5 Agonist, in Healthy Volunteers and In Vitro Identification of Human Cytochrome P450 Enzymes Involved in Its Oxidative Metabolism

2018 ◽  
Vol 46 (7) ◽  
pp. 1001-1013 ◽  
Author(s):  
Ulrike Glaenzel ◽  
Yi Jin ◽  
Robert Nufer ◽  
Wenkui Li ◽  
Kirsten Schroer ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Healthy Volunteers ◽  
Oxidative Metabolism ◽  
Cytochrome P450 Enzymes ◽  
Human Cytochrome

In vitro inhibitory mechanisms and molecular docking of 1′-S-1′-acetoxychavicol acetate on human cytochrome P450 enzymes

Phytomedicine ◽  
2017 ◽  
Vol 31 ◽  
pp. 1-9 ◽  
Author(s):  
A.K.M. Mahmudul Haque ◽  
Kok Hoong Leong ◽  
Yoke Lin Lo ◽  
Khalijah Awang ◽  
Noor Hasima Nagoor
Keyword(s):  
Cytochrome P450 ◽  
Molecular Docking ◽  
Cytochrome P450 Enzymes ◽  
Inhibitory Mechanisms ◽  
Human Cytochrome

scholarly journals In vitro inhibition of human cytochrome P450 enzymes by the novel atypical antipsychotic drug asenapine: a prediction of possible drug–drug interactions

2020 ◽  
Vol 72 (3) ◽  
pp. 612-621 ◽  
Author(s):  
Jacek Wójcikowski ◽  
Przemysław J. Danek ◽  
Agnieszka Basińska-Ziobroń ◽  
Renata Pukło ◽  
Władysława A. Daniel
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Atypical Antipsychotic ◽  
Antipsychotic Drug ◽  
The Novel ◽  
Cytochrome P450 Enzymes ◽  
Atypical Antipsychotic Drug ◽  
Human Cytochrome ◽  
In Vitro Inhibition

scholarly journals Pathways of Carbamazepine Bioactivation in Vitro. III. The Role of Human Cytochrome P450 Enzymes in the Formation of 2,3-Dihydroxycarbamazepine

2008 ◽  
Vol 36 (8) ◽  
pp. 1637-1649 ◽  
Author(s):  
Robin E. Pearce ◽  
Wei Lu ◽  
YongQiang Wang ◽  
Jack P. Uetrecht ◽  
Maria Almira Correia ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
Human Cytochrome

Enantioselective capillary electrophoresis for identification and characterization of human cytochrome P450 enzymes which metabolize ketamine and norketamine in vitro

2010 ◽  
Vol 1217 (51) ◽  
pp. 7942-7948 ◽  
Author(s):  
Simone Portmann ◽  
Hiu Ying Kwan ◽  
Regula Theurillat ◽  
Andrea Schmitz ◽  
Meike Mevissen ◽  
...  
Keyword(s):  
Capillary Electrophoresis ◽  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
Human Cytochrome ◽  
Identification And Characterization

scholarly journals In vitro inhibitory effects of plumbagin, the promising antimalarial candidate, on human cytochrome P450 enzymes

2015 ◽  
Vol 8 (11) ◽  
pp. 914-918 ◽  
Author(s):  
Wiriyaporn Sumsakul ◽  
Wanna Chaijaroenkul ◽  
Kesara Na-Bangchang
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
Inhibitory Effects ◽  
Human Cytochrome

scholarly journals Assessment of inhibitory effects on major human cytochrome P450 enzymes by spasmolytics used in the treatment of overactive bladder syndrome

2017 ◽  
Vol 9 (7) ◽  
pp. 163-177
Author(s):  
Dominik Dahlinger ◽  
Sevinc Aslan ◽  
Markus Pietsch ◽  
Sebastian Frechen ◽  
Uwe Fuhr
Keyword(s):  
Cytochrome P450 ◽  
Liver Microsomes ◽  
Fold Increase ◽  
Pharmacokinetic Data ◽  
Cytochrome P450 Enzymes ◽  
Trospium Chloride ◽  
Screening Experiments ◽  
Human Cytochrome

Background: The objective of this study was to examine the inhibitory potential of darifenacin, fesoterodine, oxybutynin, propiverine, solifenacin, tolterodine and trospium chloride on the seven major human cytochrome P450 enzymes (CYP) by using a standardized and validated seven-in-one cytochrome P450 cocktail inhibition assay. Methods: An in vitro cocktail of seven highly selective probe substrates was incubated with human liver microsomes and varying concentrations of the seven test compounds. The major metabolites of the probe substrates were simultaneously analysed using a validated liquid chromatography tandem mass spectrometry (LC-MS/MS) method. Enzyme kinetics were estimated by determining IC50 and Ki values via nonlinear regression. Obtained Ki values were used for predictions of potential clinical impact of the inhibition using a static mechanistic prediction model. Results: In this study, 49 IC50 experiments were conducted. In six cases, IC50 values lower than the calculated threshold for drug–drug interactions (DDIs) in the gut wall were observed. In these cases, no increase in inhibition was determined after a 30 min preincubation. Considering a typical dosing regimen and applying the obtained Ki values of 0.72 µM (darifenacin, 15 mg daily) and 7.2 µM [propiverine, 30 mg daily, immediate release (IR)] for the inhibition of CYP2D6 yielded a predicted 1.9-fold and 1.4-fold increase in the area under the curve (AUC) of debrisoquine (CYP2D6 substrate), respectively. Due to the inhibition of the particular intestinal CYP3A4, the obtained Ki values of 14 µM of propiverine (30 mg daily, IR) resulted in a predicted doubling of the AUC for midazolam (CYP3A4 substrate). Conclusions: In vitro/ in vivo extrapolation based on pharmacokinetic data and the conducted screening experiments yielded similar effects of darifenacin on CYP2D6 and propiverine on CYP3A4 as obtained in separately conducted in vivo DDI studies. As a novel finding, propiverine was identified to potentially inhibit CYP2D6 at clinically occurring concentrations.

In Vitro Inhibitory Effect of 1-Aminobenzotriazole on Drug Oxidations Catalyzed by Human Cytochrome P450 Enzymes: A Comparison with SKF-525A and Ketoconazole

2003 ◽  
Vol 18 (5) ◽  
pp. 287-295 ◽  
Author(s):  
Chie Emoto ◽  
Shigeo Murase ◽  
Yasufusa Sawada ◽  
Barry C. Jones ◽  
Kazuhide Iwasaki
Keyword(s):  
Cytochrome P450 ◽  
Inhibitory Effect ◽  
Cytochrome P450 Enzymes ◽  
Human Cytochrome
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