scholarly journals The influences of SLCO1B1 and ABCB1 genotypes on the pharmacokinetics of simvastatin, in relation to CYP3A4 inhibition

2017 ◽  
Vol 18 (5) ◽  
pp. 459-469 ◽  
Author(s):  
Fen Jiang ◽  
Jong-Yeol Choi ◽  
Ju-Hyun Lee ◽  
Sunae Ryu ◽  
Ze-Won Park ◽  
...  
Keyword(s):  
Cyp3a4 Inhibition

scholarly journals A Novel In Vitro Approach for Simultaneous Evaluation of CYP3A4 Inhibition and Kinetic Aqueous Solubility

2014 ◽  
Vol 20 (2) ◽  
pp. 254-264 ◽  
Author(s):  
José Pérez ◽  
Caridad Díaz ◽  
Francisco Asensio ◽  
Alexandra Palafox ◽  
Olga Genilloud ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Physicochemical Properties ◽  
Safety Concern ◽  
Aqueous Solubility ◽  
Cyp3a4 Inhibition ◽  
Use Of Resources ◽  
Simultaneous Evaluation ◽  
New Chemical Entities ◽  
Further Development

In the early stages of the drug discovery process, evaluation of the drug metabolism and physicochemical properties of new chemical entities is crucial to prioritize those candidates displaying a better profile for further development. In terms of metabolism, drug–drug interactions mediated through CYP450 inhibition are a significant safety concern, and therefore the effect of new candidate drugs on CYP450 activity should be screened early. In the initial stages of drug discovery, when physicochemical properties such as aqueous solubility have not been optimized yet, there might be a large number of candidate compounds showing artificially low CYP450 inhibition, and consequently potential drug–drug interaction toxicity might be overlooked. In this work, we present a novel in vitro approach for simultaneous evaluation of CYP3A4 inhibition potential and kinetic aqueous solubility (NIVA-CYPI-KS). This new methodology is based on fluorogenic CYP450 activities and turbidimetric measurements for compound solubility, and it provides a significant improvement in the use of resources and a better understanding of CYP450 inhibition data.

Saikosaponins and the deglycosylated metabolites exert liver meridian guiding effect through PXR/CYP3A4 inhibition

2021 ◽  
pp. 114344
Author(s):  
Qiwei Liu ◽  
Yunwen Xue ◽  
Jingjing Liu ◽  
Siqi Ren ◽  
Jie Xu ◽  
...  
Keyword(s):  
Cyp3a4 Inhibition ◽  
Guiding Effect

scholarly journals Evaluation of CYP3A4 inhibition and hepatotoxicity using DMSO-treated human hepatoma HuH-7 cells

2015 ◽  
Vol 31 (4-5) ◽  
pp. 221-230 ◽  
Author(s):  
Yitong Liu ◽  
Thomas J. Flynn ◽  
Menghang Xia ◽  
Paddy L. Wiesenfeld ◽  
Martine S. Ferguson
Keyword(s):  
Human Hepatoma ◽  
Cyp3a4 Inhibition

Metabolism of Amprenavir in Liver Microsomes: Role of CYP3A4 Inhibition for Drug Interactions

1998 ◽  
Vol 87 (7) ◽  
pp. 803-807 ◽  
Author(s):  
Caroline J. Decker ◽  
Leena M. Laitinen ◽  
Gary W. Bridson ◽  
Scott A. Raybuck ◽  
Roger D. Tung ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Liver Microsomes ◽  
Cyp3a4 Inhibition

scholarly journals Accurate Prediction of Dose-Dependent CYP3A4 Inhibition by Itraconazole and Its Metabolites From In Vitro Inhibition Data

2010 ◽  
Vol 88 (4) ◽  
pp. 499-505 ◽  
Author(s):  
I Templeton ◽  
C-C Peng ◽  
K E Thummel ◽  
C Davis ◽  
K L Kunze ◽  
...  
Keyword(s):  
Accurate Prediction ◽  
Cyp3a4 Inhibition ◽  
Inhibition Data ◽  
In Vitro Inhibition ◽  
Dose Dependent
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