Examination of 209 Drugs for Inhibition of Cytochrome P450 2C8

  title={Examination of 209 Drugs for Inhibition of Cytochrome P450 2C8},
  author={Robert L. Walsky and Emily A. Gaman and R. Scott Obach},
  journal={The Journal of Clinical Pharmacology},
Cytochrome P450 2C8 is involved in the metabolism of drugs such as paclitaxel, repaglinide, rosiglitazone, and cerivastatin, among others. An in vitro assessment of 209 frequently prescribed drugs and related xenobiotics was carried out to examine their potential to inhibit CYP2C8. A validated sensitive, moderate‐throughput high‐performance liquid chromatography/tandem mass spectrometry (HPLC/MS/MS) assay was used to detect N‐desethylamodiaquine, the CYP2C8‐derived major metabolite of… 
Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions
Current knowledge on substrates, inhibitors, inducers, and pharmacogenetics of CYP2C8, as well as its role in clinically relevant drug interactions is reviewed.
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Chemical inhibitors of cytochrome P450 isoforms in human liver microsomes: a re-evaluation of P450 isoform selectivity
The majority of marketed small-molecule drugs undergo metabolism by hepatic Cytochrome P450 (CYP) enzymes (Rendic 2002). Since these enzymes metabolize a structurally diverse number of drugs,
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In silico and in vitro methods used are helpful in predicting in vivo drug-drug interactions and the effective utilisation of these models in the early phases of drug discovery could help to target the in vivo studies and to eliminate metabolically unfavourable drug candidates.
Direct inhibition of Re Du Ning Injection and its active compounds on human liver cytochrome P450 enzymes by a cocktail method.
Investigating the direct inhibitory effects of Re Du Ning Injection and its active compounds on the major cytochrome P450 enzyme (CYP) isoforms of human liver microsomes suggested that drug-drug interactions may occur and great caution should be taken when RDN is combined with drugs metabolized by these CYPs.
Further Assessment of 17α-Ethinyl Estradiol as an Inhibitor of Different Human Cytochrome P450 Forms in Vitro
The results implicate intestinal CYP1A1, and possibly CYP2C19, as the loci of EE drug interactions with highly extracted drugs like MEL, which raises the possibility that the concentration of EE during first pass may exceed 1000 nM, sufficient to affect CYP3A4 and other P450s.
Pharmacokinetic Drug Interactions Involving 17α-Ethinylestradiol
This article summarises what is known of the drug-metabolising enzymes and transporters governing the metabolism, disposition and excretion ofα-Ethinylestradiol and related information to known clinical drug-drug interactions.
Effect of pterostilbene on in vitro drug metabolizing enzyme activity
  • A. Albassam, R. Frye
  • Biology, Chemistry
    Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society
  • 2019
Inhibitory effect of six herbal extracts on CYP2C8 enzyme activity in human liver microsomes
A potential for cranberry or saw palmetto extracts to inhibit CYP2C8 activity is suggested, and clinical studies are needed to evaluate the significance of this interaction.
Strong and Selective Inhibitory Effects of the Biflavonoid Selamariscina A against CYP2C8 and CYP2C9 Enzyme Activities in Human Liver Microsomes
It is concluded that selamariscina A has selective and strong inhibitory effects on the CYP 2C8 and CYP2C9 isoforms, which might be useful in predicting herb-drug interaction potential between biflavonoids and co-administered drugs mainly metabolized by CYP1A2 and CYB2C8.


The xenobiotic inhibitor profile of cytochrome P4502C8.
AIMS To investigate inhibition of recombinant CYP2C8 by: (i) prototypic CYP isoform selective inhibitors (ii) imidazole/triazole antifungal agents (known inhibitors of CYP), and (iii) certain CYP3A
Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of rosiglitazone.
CYP2C8 is primarily responsible for the hydroxylation and N-demethylation of rosiglitazone in human liver; with minor contributions from CYP2C9.
Identification of human cytochrome P450s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data
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Drug Interactions of Paclitaxel Metabolism in Human Liver Microsomes
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Data strongly suggested that the structure of the lateral chain and the nature of substituent in position 10 play an important role in determining the regioselective oxidation by P450 proteins and modulate the reaction rate by human liver microsomes.
Oxidation of troglitazone to a quinone-type metabolite catalyzed by cytochrome P-450 2C8 and P-450 3A4 in human liver microsomes.
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Trimethoprim and sulfamethoxazole can be used as selective inhibitors of CYP2C8 and CYP 2C9 in in vitro studies and in vivo in humans, respectively.
Trimethoprim and sulfamethoxazole are selective inhibitors of CYP2C8 and CYP2C9, respectively.
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Polymorphisms in human CYP2C8 decrease metabolism of the anticancer drug paclitaxel and arachidonic acid.
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