ArticleDrug metabolism and disposition: the biological fate of chemicals2010
Human liver expression of CYP2C8: gender, age, and genotype effects.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 83 citations in OpenAlex.
- Gender differences in the efficacy of pioglitazone treatment in nonalcoholic fatty liver disease patients with abnormal glucose metabolism.Biology of sex differences · 2021Trial
- Genetic markers in the EET metabolic pathway are associated with outcomes in patients with aneurysmal subarachnoid hemorrhage.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2015Trial
- Factors Affecting the Treatment Heterogeneity of PPARγ and Pan-PPAR Agonists in Type 2 Diabetes Mellitus: A Systematic Review and Machine Learning-Based Meta-Regression Analysis.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Sex differences in hepatic enzymes and transporters involved in pharmacokinetics.Liver research (Beijing, China) · 2025Review
- Mechanisms of altered hepatic drug disposition during pregnancy: small molecules.Expert opinion on drug metabolism & toxicology · 2025Review
- Article
- Role of Genetic Polymorphisms in Drug-Metabolizing Enzyme-Mediated Toxicity and Pharmacokinetic Resistance to Anti-Cancer Agents: A Review on the Pharmacogenomics Aspect.Clinical pharmacokinetics · 2022Review
- Gephyrin andPharmacogenomics and personalized medicine · 2021Article
- How Can Drug Metabolism and Transporter Genetics Inform Psychotropic Prescribing?Frontiers in genetics · 2020Review
- Pharmacogenetics of Statin-Induced Myotoxicity.Frontiers in genetics · 2020Review
- Effect of pterostilbene onSaudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2019Article
- Prediction of olanzapine exposure in individual patients using physiologically based pharmacokinetic modelling and simulation.British journal of clinical pharmacology · 2018Article
- Concentration-dependent response to pioglitazone in nonalcoholic steatohepatitis.Alimentary pharmacology & therapeutics · 2017Article
- Clinical Pharmacokinetics and Pharmacodynamics of Antihyperglycemic Medications in Children and Adolescents with Type 2 Diabetes Mellitus.Clinical pharmacokinetics · 2017Review
- In vitro metabolism of exemestane by hepatic cytochrome P450s: impact of nonsynonymous polymorphisms on formation of the active metabolite 17Pharmacology research & perspectives · 2017Article
- Physiologically Based Pharmacokinetic Modeling to Predict Drug-Drug Interactions with Efavirenz Involving Simultaneous Inducing and Inhibitory Effects on Cytochromes.Clinical pharmacokinetics · 2017Article
- Systematic tracking of disrupted modules identifies significant genes and pathways in hepatocellular carcinoma.Oncology letters · 2016Article
- Peroxisome proliferator-activated receptor alpha, PPARα, directly regulates transcription of cytochrome P450 CYP2C8.Frontiers in pharmacology · 2015Article
- Cytochrome P450 single nucleotide polymorphisms in an indigenous Tanzanian population: a concern about the metabolism of artemisinin-based combinations.Malaria journal · 2014Article
- CYP2C8 and CYP2C9 mRNA expression profile in the human fetus.Frontiers in genetics · 2014Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Research investigating CYP2C8 as a drug-metabolizing enzyme has gained momentum over the past few years. CYP2C8 is estimated to oxidatively metabolize approximately 5% of therapeutically prescribed drugs. It is polymorphically expressed, and several single nucleotide polymorphisms have been identified with varying effects on the clearance of CYP2C8 substrates. However, the human liver expression of CYP2C8 and effects of genetic variation, age, and gender on mRNA and protein levels have not been fully explored. In this report, interindividual variation in CYP2C8 mRNA and protein expression in 60 livers from white individuals was examined. The livers were genotyped for CYP2C8*3 and CYP2C8*4 polymorphisms. The effects of genotype, age, and gender on hepatic CYP2C8 expression and the correlation of CYP2C8 mRNA expression with CYP3A4 and other CYP2C members were evaluated. The mean +/- S.D. protein levels in CYP2C8*1/*1 livers was 30.8 +/- 17.5 pmol/mg protein, and a trend for decreased protein levels was observed for CYP2C8*1/*4 livers (15.8 +/- 9.7 pmol/mg, p = 0.07). The mean expression levels of CYP2C8 was comparable in males and females (p = 0.18). The mRNA expression of CYP2C8, CYP2C9, CYP2C19, and CYP3A4, but not CYP2C18, was highly correlated (p < 0.0001). Moreover, the hepatic CYP2C8 and CYP3A4 protein levels were strongly correlated (r = 0.76, p < 0.0001). This correlation is most likely due to common regulation factors for both genes. CYP2C8 mRNA or protein expression levels were not significantly affected by CYP2C8*3 or *4 genotype, gender, or age, and variation observed clinically in CYP2C8 activity warrants further investigation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.