In Vitro Characterization of Sarizotan Metabolism: Hepatic Clearance, Identification and Characterization of Metabolites, Drug-Metabolizing Enzyme Identification, and Evaluation of Cytochrome P450 Inhibition

2010 ◽  
Vol 38 (6) ◽  
pp. 905-916 ◽  
Author(s):  
Dieter Gallemann ◽  
Elmar Wimmer ◽  
Constance C. Höfer ◽  
Achim Freisleben ◽  
Markus Fluck ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Hepatic Clearance ◽  
In Vitro Characterization ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme ◽  
Identification And Characterization

scholarly journals In Vitro Characterization of Ertugliflozin Metabolism by UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes

2020 ◽  
Vol 48 (12) ◽  
pp. 1350-1363
Author(s):  
Kimberly Lapham ◽  
Ernesto Callegari ◽  
Julie Cianfrogna ◽  
Jian Lin ◽  
Mark Niosi ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
In Vitro Characterization ◽  
Udp Glucuronosyltransferase

IN VITRO CHARACTERIZATION OF CLOBAZAM METABOLISM BY RECOMBINANT CYTOCHROME P450 ENZYMES: IMPORTANCE OF CYP2C19

2004 ◽  
Vol 32 (11) ◽  
pp. 1279-1286 ◽  
Author(s):  
Carole Giraud ◽  
Agnès Tran ◽  
Elisabeth Rey ◽  
Jean Vincent ◽  
Jean-Marc Tréluyer ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
In Vitro Characterization

scholarly journals A Novel System for Evaluating the Inhibition Effect of Drugs on Cytochrome P450 Enzymes in vitro Based on Human-Induced Hepatocytes (hiHeps)

2021 ◽  
Vol 12 ◽  
Author(s):  
Yan Li ◽  
Ying-Yuan Lu ◽  
Jun Jia ◽  
Meng Fang ◽  
Lin Zhao ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Evaluation System ◽  
Human Fibroblasts ◽  
Liver Microsomes ◽  
Cytochrome P450 Enzymes ◽  
Cyp Enzymes ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme ◽  
Toxicity Of Drugs

Cytochrome P450 (CYP) is the most important phase I drug-metabolizing enzyme, and the effect of drugs on CYP enzymes can lead to decreased pharmacological efficacy or enhanced toxicity of drugs, but there are many deficiencies in the evaluation models of CYP enzymes in vitro. Human-induced hepatocytes (hiHeps) derived from human fibroblasts by transdifferentiation have mature hepatocyte characteristics. The aim was to establish a novel evaluation system for the effect of drugs on CYP3A4, 1A2, 2B6, 2C9, and 2C19 in vitro based on hiHeps. Curcumin can inhibit many CYP enzymes in vitro, and so the inhibition of curcumin on CYP enzymes was compared by human liver microsomes, human hepatocytes, and hiHeps using UPLC-MS and the cocktail method. The results showed that the IC50 values of CYP enzymes in the hiHeps group were similar to those in the hepatocytes group, which proved the effectiveness and stability of the novel evaluation system in vitro. Subsequently, the evaluation system was applied to study the inhibitory activity of notoginseng total saponins (NS), safflower total flavonoids (SF), and the herb pair of NS–SF on five CYP enzymes. The mechanism of improving efficacy after NS and SF combined based on CYP enzymes was elucidated in vitro. The established evaluation system will become a powerful tool for the research of the effect of drugs on the activity of CYP enzymes in vitro, which has broad application prospects in drug research.

In vitro characterization of cytochrome P450 catalysed metabolism of the antiemetic tropisetron

1995 ◽  
Vol 49 (12) ◽  
pp. 1777-1784 ◽  
Author(s):  
Lucie Firkusny ◽  
Heyo K. Kroemer ◽  
Michel eichelbaum
Keyword(s):  
Cytochrome P450 ◽  
In Vitro Characterization
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