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Interplay of UDP-Glucuronosyltransferase and CYP2C8 for CYP2C8 Mediated Drug Oxidation and Its Impact on Drug–Drug Interaction Produced by Standardized CYP2C8 Inhibitors, Clopidogrel and Gemfibrozil

Clinical Pharmacokinetics, 2023
Early investigations into drug-drug interactions (DDIs) involving cytochrome P450 2C8 (CYP2C8) have highlighted the complexity of interactions between CYP2C8 substrate drugs, including montelukast, desloratadine, pioglitazone, repaglinide, and cerivastatin (the latter two being OATP1B1 substrates), and standardized CYP2C8 inhibitors such as clopidogrel
Katsumi Iga, Akiko Kiriyama
openaire   +2 more sources

Global variation in CYP2C8–CYP2C9 functional haplotypes [PDF]

open access: yesPharmacogenomics Journal, 2009
We have studied the global frequency distributions of 10 single nucleotide polymorphisms (SNPs) across 132 kb of CYP2C8 and CYP2C9 in approximately 2500 individuals representing 45 populations. Five of the SNPs were in noncoding sequences; the other five involved the more common missense variants (four in CYP2C8, one in CYP2C9) that change amino acids ...
Kenneth Kidd   +2 more
exaly   +3 more sources

Evaluation of CYP2C8 Inhibition In Vitro: Utility of Montelukast as a Selective CYP2C8 Probe Substrate

Drug Metabolism and Disposition, 2011
Understanding the potential for cytochrome P450 (P450)-mediated drug-drug interactions is a critical step in the drug discovery process. Although in vitro studies with CYP3A4, CYP2C9, and CYP2C19 have suggested the presence of multiple binding regions within the P450 active site based on probe substrate-dependent inhibition profiles, similar studies ...
Brooke M, VandenBrink   +4 more
openaire   +2 more sources

GENETIC POLYMORPHISMS OF CYP2C8 IN JAPANESE POPULATION

Drug Metabolism and Disposition, 2003
CYP2C8 plays important roles in metabolizing therapeutic drugs and endogenous compounds. Although genetic polymorphisms of CYP2C8 were reported, there is little information on CYP2C8 polymorphisms in the Japanese population. In the present study, we screened for previously described polymorphisms in the coding region of this gene using polymerase chain
Miki, Nakajima   +8 more
openaire   +2 more sources

Linkage between the CYP2C8 and CYP2C9 genetic polymorphisms

Biochemical and Biophysical Research Communications, 2002
Cytochrome P450 (CYP) 2C8 and 2C9 are polymorphic enzymes. The CYP2C8*3 and CYP2C9*2 are the major variant alleles in Caucasian populations. The enzymes encoded by these variant alleles have impaired function for the metabolism of several drug substrates.
Umit, Yasar   +6 more
openaire   +2 more sources

In Silico Prediction of CYP2C8 Inhibition with Machine-Learning Methods

Chemical Research in Toxicology, 2021
Cytochrome P450 2C8 (CYP2C8) is a major drug-metabolizing enzyme in humans and is responsible for the metabolism of ∼5% drugs in clinical use. Thus, inhibition of CYP2C8, which causes potential adverse drug events, cannot be neglected. The in vitro drug interaction studies guidelines for industry issued by the FDA also point out that it needs to be ...
Xiaoxiao Zhang   +6 more
openaire   +2 more sources

Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide

European Journal of Clinical Pharmacology, 2006
Pioglitazone, a thiazolidinedione antidiabetic, inhibits cytochrome P450 (CYP) 2C8 and CYP3A4 enzymes in vitro. Repaglinide, a meglitinide analogue antidiabetic, is metabolised by CYP2C8 and CYP3A4. In patients with type 2 diabetes, the pioglitazone-repaglinide combination has acted synergistically on glycaemic parameters.
Lauri I, Kajosaari   +3 more
openaire   +2 more sources

Polymorphisms in CYP2C8 and CYP3A5 genes in the Nigerian population

Drug Metabolism and Pharmacokinetics, 2017
Polymorphisms in CYP2C8 and CYP3A5 genes have implications for responses elicited by the ingestion of some xenobiotics, the metabolism of which are mediated by these enzymes. CYP2C8*2, CYP2C8*3, CYP3A5*3, CYP3A5*6 and CYP3A5*7 are a few functionally-relevant variants of these genes which this study provides data for, in the Nigerian population.
Ayorinde Adehin   +2 more
openaire   +2 more sources

Role of gemfibrozil as an inhibitor of CYP2C8 and membrane transporters

Expert Opinion on Drug Metabolism & Toxicology, 2016
Cytochrome P450 (CYP) 2C8 is a drug metabolizing enzyme of major importance. The lipid-lowering drug gemfibrozil has been identified as a strong inhibitor of CYP2C8 in vivo. This effect is due to mechanism-based inhibition of CYP2C8 by gemfibrozil 1-O-β-glucuronide.
Aleksi, Tornio   +3 more
openaire   +2 more sources

Inhibitory Effects of Danshen components on CYP2C8 and CYP2J2

Chemico-Biological Interactions, 2018
The use of Chinese herbal medicines and natural products has become increasingly popular in both China and Western societies as an alternative medicine for the treatment of diseases or as a health supplement. Danshen, the dried root of Salvia miltiorrhiza (Fam.Labiatae), which is rich in phenolic acids and tanshinones, is a widely used herbal medicine ...
Mei-Juan, Xu   +9 more
openaire   +2 more sources

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