CYP2C8

Summary

Gene Symbol: CYP2C8
Description: cytochrome P450 family 2 subfamily C member 8
Alias: CPC8, CYPIIC8, MP-12/MP-20, cytochrome P450 2C8, P450 form 1, cytochrome P450 IIC2, cytochrome P450 MP-12, cytochrome P450 MP-20, cytochrome P450 form 1, cytochrome P450, family 2, subfamily C, polypeptide 8, cytochrome P450, subfamily IIC (mephenytoin 4-hydroxylase), polypeptide 8, flavoprotein-linked monooxygenase, microsomal monooxygenase, s-mephenytoin 4-hydroxylase, xenobiotic monooxygenase
Species: human
Products:     CYP2C8

Top Publications

  1. Röwer S, Bienzle U, Weise A, Lambertz U, Forst T, Otchwemah R, et al. Short communication: high prevalence of the cytochrome P450 2C8*2 mutation in Northern Ghana. Trop Med Int Health. 2005;10:1271-3 pubmed
    ..The pro-drug AQ is transformed by cytochrome P450 CYP2C8 to the active metabolite N-desethylaminodiaquine...
  2. Lopez Rodriguez R, Novalbos J, Gallego Sandín S, Román Martínez M, Torrado J, Gisbert J, et al. Influence of CYP2C8 and CYP2C9 polymorphisms on pharmacokinetic and pharmacodynamic parameters of racemic and enantiomeric forms of ibuprofen in healthy volunteers. Pharmacol Res. 2008;58:77-84 pubmed publisher
    i) To define the incidence of alleles CYP2C8*1 to *5 in a Spanish population; (ii) to test the impact of such alleles, and those of CYP2C9, on the metabolism of racemic ibuprofen, R-ibuprofen and S-ibuprofen; and (iii) to discern whether ..
  3. Dreisbach A, Japa S, Sigel A, Parenti M, Hess A, Srinouanprachanh S, et al. The Prevalence of CYP2C8, 2C9, 2J2, and soluble epoxide hydrolase polymorphisms in African Americans with hypertension. Am J Hypertens. 2005;18:1276-81 pubmed
    ..Multiple single nucleotide polymorphisms (SNP) in CYP2C8, 2C9, 2J2 and soluble epoxide hydrolase (sEH) have been identified, many of which have altered functional activity ..
  4. Singh R, Ting J, Pan Y, Teh L, Ismail R, Ong C. Functional role of Ile264 in CYP2C8: mutations affect haem incorporation and catalytic activity. Drug Metab Pharmacokinet. 2008;23:165-74 pubmed
    The work described in this study aimed to express CYP2C8 wild-type and mutant proteins in bacterial expression system and to use the expressed proteins to investigate the structural and functional consequences of a reported allele CYP2C8(*..
  5. Niemi M, Backman J, Kajosaari L, Leathart J, Neuvonen M, Daly A, et al. Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Clin Pharmacol Ther. 2005;77:468-78 pubmed
  6. Pedersen R, Brasch Andersen C, Sim S, Bergmann T, Halling J, Petersen M, et al. Linkage disequilibrium between the CYP2C19*17 allele and wildtype CYP2C8 and CYP2C9 alleles: identification of CYP2C haplotypes in healthy Nordic populations. Eur J Clin Pharmacol. 2010;66:1199-205 pubmed publisher
    ..and Norwegian) were genotyped for five frequent and clinically important CYP2C allelic variants: the defective CYP2C8*3, CYP2C9*2, CYP2C9*3, and CYP2C19*2 alleles, and the CYP2C19*17 allele that causes rapid drug metabolism...
  7. Dai D, Zeldin D, Blaisdell J, Chanas B, Coulter S, Ghanayem B, et al. Polymorphisms in human CYP2C8 decrease metabolism of the anticancer drug paclitaxel and arachidonic acid. Pharmacogenetics. 2001;11:597-607 pubmed
    ..In this study, we describe two new CYP2C8 alleles containing coding changes: CYP2C8*2 has an Ile269Phe substitution in exon 5 and CYP2C8*3 includes both ..
  8. Kirchheiner J, Thomas S, Bauer S, Tomalik Scharte D, Hering U, Doroshyenko O, et al. Pharmacokinetics and pharmacodynamics of rosiglitazone in relation to CYP2C8 genotype. Clin Pharmacol Ther. 2006;80:657-67 pubmed
    Rosiglitazone is metabolically inactivated predominantly via the cytochrome P450 (CYP) enzyme CYP2C8. The functional impact of the CYP2C8*3 allele coding for the Arg139Lys and Lys399Arg amino acid substitutions is controversial...
  9. Weise A, Grundler S, Zaumsegel D, Klotzek M, Gröndahl B, Forst T, et al. Development and evaluation of a rapid and reliable method for cytochrome P450 2C8 genotyping. Clin Lab. 2004;50:141-8 pubmed
    ..fast real-time PCR method for the detection of three different allele mutations of Cytochrome P450 isoenzyme 2C8 (CYP2C8*2, *3, and *4), which have been demonstrated to influence drug metabolism (and thus the efficacy) of a variety of ..

More Information

Publications87

  1. Pedersen R, Damkier P, Brosen K. The effects of human CYP2C8 genotype and fluvoxamine on the pharmacokinetics of rosiglitazone in healthy subjects. Br J Clin Pharmacol. 2006;62:682-9 pubmed
    To determine the effect of CYP2C8 genotype and of fluvoxamine on the pharmacokinetics of rosiglitazone.
  2. Lai X, Yang L, Li X, Liu J, Zhou Z, Zhou S. Human CYP2C8: structure, substrate specificity, inhibitor selectivity, inducers and polymorphisms. Curr Drug Metab. 2009;10:1009-47 pubmed
    Human CYP2C8 is a key member of the CYP2C family and metabolizes more than 60 clinical drugs. A number of active site residues in CYP2C8 have been identified based on homology modeling and site-directed mutagenesis studies...
  3. Henningsson A, Marsh S, Loos W, Karlsson M, Garsa A, Mross K, et al. Association of CYP2C8, CYP3A4, CYP3A5, and ABCB1 polymorphisms with the pharmacokinetics of paclitaxel. Clin Cancer Res. 2005;11:8097-104 pubmed
    To retrospectively evaluate the effects of six known allelic variants in the CYP2C8, CYP3A4, CYP3A5, and ABCB1 genes on the pharmacokinetics of the anticancer agent paclitaxel (Taxol)...
  4. Cavaco I, Strömberg Nörklit J, Kaneko A, Msellem M, Dahoma M, Ribeiro V, et al. CYP2C8 polymorphism frequencies among malaria patients in Zanzibar. Eur J Clin Pharmacol. 2005;61:15-8 pubmed
    The determination of the prevalence of the CYP2C8 main alleles in a typical set of malaria patients in Zanzibar, as these patients represent a typical population exposed to amodiaquine, an antimalarial mainly metabolized by CYP2C8...
  5. Hichiya H, Tanaka Kagawa T, Soyama A, Jinno H, Koyano S, Katori N, et al. Functional characterization of five novel CYP2C8 variants, G171S, R186X, R186G, K247R, and K383N, found in a Japanese population. Drug Metab Dispos. 2005;33:630-6 pubmed
    b>Cytochrome P450 2C8 is one of the primary enzymes responsible for the metabolism of a wide range of drugs such as paclitaxel, cerivastatin, and amiodarone...
  6. Lee C, North K, Bray M, Couper D, Heiss G, Zeldin D. CYP2J2 and CYP2C8 polymorphisms and coronary heart disease risk: the Atherosclerosis Risk in Communities (ARIC) study. Pharmacogenet Genomics. 2007;17:349-58 pubmed
    The cytochromes P450 epoxygenases CYP2J2 and CYP2C8 synthesize epoxyeicosatrienoic acids, which regulate endothelial function...
  7. Saito Y, Katori N, Soyama A, Nakajima Y, Yoshitani T, Kim S, et al. CYP2C8 haplotype structures and their influence on pharmacokinetics of paclitaxel in a Japanese population. Pharmacogenet Genomics. 2007;17:461-71 pubmed
    b>CYP2C8 is known to metabolize various drugs including an anticancer drug paclitaxel...
  8. Goldstein J, de Morais S. Biochemistry and molecular biology of the human CYP2C subfamily. Pharmacogenetics. 1994;4:285-99 pubmed
    ..Four members of this subfamily have been identified in humans: CYP2C8, CYP2C9, CYP2C18, and CYP2C19...
  9. Daily E, Aquilante C. Cytochrome P450 2C8 pharmacogenetics: a review of clinical studies. Pharmacogenomics. 2009;10:1489-510 pubmed publisher
    ..g., thiazolidinediones, meglitinides, NSAIDs, antimalarials and chemotherapeutic taxanes). The CYP2C8 enzyme is encoded by the CYP2C8 gene, and several common nonsynonymous polymorphisms (e.g...
  10. Tornio A, Niemi M, Neuvonen P, Backman J. Trimethoprim and the CYP2C8*3 allele have opposite effects on the pharmacokinetics of pioglitazone. Drug Metab Dispos. 2008;36:73-80 pubmed
    We studied the effects of the CYP2C8 inhibitor trimethoprim and CYP2C8 genotype on the pharmacokinetics of the antidiabetic pioglitazone...
  11. Martinez C, Garcia Martin E, Blanco G, Gamito F, Ladero J, Agundez J. The effect of the cytochrome P450 CYP2C8 polymorphism on the disposition of (R)-ibuprofen enantiomer in healthy subjects. Br J Clin Pharmacol. 2005;59:62-9 pubmed
    To study the effect of CYP2C8*3, the most common CYP2C8 variant allele on the dis-position of (R)-ibuprofen and the association of CYP2C8*3 with variant CYP2C9 alleles...
  12. Yasar U, Lundgren S, Eliasson E, Bennet A, Wiman B, de Faire U, et al. Linkage between the CYP2C8 and CYP2C9 genetic polymorphisms. Biochem Biophys Res Commun. 2002;299:25-8 pubmed
    Cytochrome P450 (CYP) 2C8 and 2C9 are polymorphic enzymes. The CYP2C8*3 and CYP2C9*2 are the major variant alleles in Caucasian populations...
  13. Zhang S, Surapureddi S, Coulter S, Ferguson S, Goldstein J. Human CYP2C8 is post-transcriptionally regulated by microRNAs 103 and 107 in human liver. Mol Pharmacol. 2012;82:529-40 pubmed publisher
    ..Among these were a MRE for the miRNAs miR-103 and miR-107 in the 3'-UTR of human CYP2C8. CYP2C8 protein levels (measured through immunoblot analyses) did not correlate with CYP2C8 mRNA levels (measured ..
  14. Dorado P, Cavaco I, Cáceres M, Piedade R, Ribeiro V, LLerena A. Relationship between CYP2C8 genotypes and diclofenac 5-hydroxylation in healthy Spanish volunteers. Eur J Clin Pharmacol. 2008;64:967-70 pubmed publisher
    b>CYP2C8 seems to be involved in diclofenac 5-hydroxylation, while, in vitro, the 4'-hydroxylation and 3'-hydroxylation seem to be mediated mainly by CYP2C9...
  15. Gray I, Nobile C, Muresu R, Ford S, Spurr N. A 2.4-megabase physical map spanning the CYP2C gene cluster on chromosome 10q24. Genomics. 1995;28:328-32 pubmed
    ..The cluster spans approximately 500 kb on proximal 10q24 and comprises four genes arranged in the order CYP2C8-CYP2C9-CYP2C19-CYP2C18. The map also includes an adjacent gene, the serum retinol binding protein gene (RBP4)...
  16. Enayetallah A, French R, Grant D. Distribution of soluble epoxide hydrolase, cytochrome P450 2C8, 2C9 and 2J2 in human malignant neoplasms. J Mol Histol. 2006;37:133-41 pubmed
    ..Here we provide a comprehensive analysis of the distribution of sEH, CYP2C8, 2C9 and 2J2 in human neoplastic tissues using tissue micro-arrays...
  17. Zeldin D, DuBois R, Falck J, Capdevila J. Molecular cloning, expression and characterization of an endogenous human cytochrome P450 arachidonic acid epoxygenase isoform. Arch Biochem Biophys. 1995;322:76-86 pubmed
    ..Karara et al., 1990, FEBS Lett. 268, 227-230). Hence, we propose that Cyp 2C8 is one of the human cytochrome P450 isoforms responsible for the metabolism of endogenous arachidonic acid pools. ..
  18. Speed W, Kang S, Tuck D, Harris L, Kidd K. Global variation in CYP2C8-CYP2C9 functional haplotypes. Pharmacogenomics J. 2009;9:283-90 pubmed publisher
    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...
  19. Garcia Martin E, Martinez C, Ladero J, Agundez J. Interethnic and intraethnic variability of CYP2C8 and CYP2C9 polymorphisms in healthy individuals. Mol Diagn Ther. 2006;10:29-40 pubmed
    Cytochrome P450 (CYP) superfamily members CYP2C8 and CYP2C9 are polymorphically expressed enzymes that are involved in the metabolic inactivation of several drugs, including, among others, antiepileptics, NSAIDs, oral hypoglycemics, and ..
  20. Rodriguez Antona C, Niemi M, Backman J, Kajosaari L, Neuvonen P, Robledo M, et al. Characterization of novel CYP2C8 haplotypes and their contribution to paclitaxel and repaglinide metabolism. Pharmacogenomics J. 2008;8:268-77 pubmed
    b>Cytochrome P450 2C8 (CYP2C8) plays a major role in the metabolism of therapeutically important drugs which exhibit large interindividual differences in their pharmacokinetics...
  21. Shuldiner A, O Connell J, Bliden K, Gandhi A, Ryan K, Horenstein R, et al. Association of cytochrome P450 2C19 genotype with the antiplatelet effect and clinical efficacy of clopidogrel therapy. JAMA. 2009;302:849-57 pubmed publisher
    ..73; P < .001). Thirteen single-nucleotide polymorphisms on chromosome 10q24 within the CYP2C18-CYP2C19-CYP2C9-CYP2C8 cluster were associated with diminished clopidogrel response, with a high degree of statistical significance (P = ..
  22. Deng Y, Edin M, Theken K, Schuck R, Flake G, Kannon M, et al. Endothelial CYP epoxygenase overexpression and soluble epoxide hydrolase disruption attenuate acute vascular inflammatory responses in mice. FASEB J. 2011;25:703-13 pubmed publisher
    ..inflammatory responses to endotoxin in transgenic mice with endothelial expression of the human CYP2J2 and CYP2C8 epoxygenases and mice with targeted disruption of Ephx2...
  23. Garcia Martin E, Martinez C, Tabares B, Frias J, Agundez J. Interindividual variability in ibuprofen pharmacokinetics is related to interaction of cytochrome P450 2C8 and 2C9 amino acid polymorphisms. Clin Pharmacol Ther. 2004;76:119-27 pubmed
    ..Genomic deoxyribonucleic acid was analyzed for common mutations at CYP2C8 and CYP2C9 genes that cause amino acid substitutions. Ibuprofen clearance values were 4...
  24. Yasar U, Bennet A, Eliasson E, Lundgren S, Wiman B, de Faire U, et al. Allelic variants of cytochromes P450 2C modify the risk for acute myocardial infarction. Pharmacogenetics. 2003;13:715-20 pubmed
    ..This study describes the relationship between genetic variants of CYP2C8 and CYP2C9, and morbidity in myocardial infarction in a large Swedish patient material...
  25. Bahadur N, Leathart J, Mutch E, Steimel Crespi D, Dunn S, Gilissen R, et al. CYP2C8 polymorphisms in Caucasians and their relationship with paclitaxel 6alpha-hydroxylase activity in human liver microsomes. Biochem Pharmacol. 2002;64:1579-89 pubmed
    ..cDNA sequences suggest the existence of non-synonymous single nucleotide polymorphisms in the cytochrome P450 CYP2C8. To determine whether these polymorphisms could be confirmed in a Caucasian population and to investigate whether ..
  26. Grover S, Gourie Devi M, Baghel R, Sharma S, Bala K, Gupta M, et al. Genetic profile of patients with epilepsy on first-line antiepileptic drugs and potential directions for personalized treatment. Pharmacogenomics. 2010;11:927-41 pubmed publisher
    ..Interethnic differences were elucidated for several polymorphisms that might be responsible for differential serum drug levels and optimal dose requirement for efficacious treatment. ..
  27. Karonen T, Neuvonen P, Backman J. CYP2C8 but not CYP3A4 is important in the pharmacokinetics of montelukast. Br J Clin Pharmacol. 2012;73:257-67 pubmed publisher
    According to product information, montelukast is extensively metabolized by CYP3A4 and CYP2C9. However, CYP2C8 was also recently found to be involved...
  28. Pechandová K, Buzková H, Matousková O, Perlík F, Slanar O. Genetic polymorphisms of CYP2C8 in the Czech Republic. Genet Test Mol Biomarkers. 2012;16:812-6 pubmed publisher
    b>CYP2C8 represents 7% of the hepatic cytochrome system and metabolizes around 5% of drugs in phase I processes. It also plays a significant role in metabolism of endogenous compounds...
  29. Granger Joly de Boissel P, Fournier M, Rodriguez Lecompte J, McKenna P, Kibenge F, Siah A. Functional and molecular responses of the blue mussel Mytilus edulis' hemocytes exposed to cadmium - An in vitro model and transcriptomic approach. Fish Shellfish Immunol. 2017;67:575-585 pubmed publisher
    ..The induction of super oxide dismutase (SOD), glutathion-s-transferase (GST), cytochrome P450 2C8 (CYP2C8), multidrug resistance protein (MRP1) and heat shock protein 70 (HSP70) suggests that Cd can ..
  30. Lazarska K, Dekker S, Vermeulen N, Commandeur J. Effect of UGT2B7*2 and CYP2C8*4 polymorphisms on diclofenac metabolism. Toxicol Lett. 2018;284:70-78 pubmed publisher
    ..Previous association studies showed that possession of the UGT2B7*2 and CYP2C8*4 alleles is more common in cases of diclofenac-induced DILI...
  31. Garimella T, Tao X, Sims K, Chang Y, Rana J, Myers E, et al. Effects of a Fixed-Dose Co-Formulation of Daclatasvir, Asunaprevir, and Beclabuvir on the Pharmacokinetics of a Cocktail of Cytochrome P450 and Drug Transporter Substrates in Healthy Subjects. Drugs R D. 2018;18:55-65 pubmed publisher
    ..n = 20) given single-dose caffeine (CYP1A2 substrate), metoprolol (CYP2D6), flurbiprofen (CYP2C9), montelukast (CYP2C8), omeprazole (CYP2C19), midazolam (CYP3A4), digoxin (P-glycoprotein), and pravastatin (organic anion-transporting ..
  32. Li A, Ho M, Amaral K, Loretz C. A Novel In Vitro Experimental System for the Evaluation of Drug Metabolism: Cofactor-Supplemented Permeabilized Cryopreserved Human Hepatocytes (MetMax Cryopreserved Human Hepatocytes). Drug Metab Dispos. 2018;46:1608-1616 pubmed publisher
    ..In this study, we compared MMHHs and CCHHs in CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, CYP3A4, CYP2J2, monoamine oxidase A, aldehyde oxidase, flavin-containing monooxygenase, ..
  33. Karaźniewicz Łada M, Luczak M, Główka F. Pharmacokinetic studies of enantiomers of ibuprofen and its chiral metabolites in humans with different variants of genes coding CYP2C8 and CYP2C9 isoenzymes. Xenobiotica. 2009;39:476-85 pubmed publisher
    ..biological fluids were used to calculate their pharmacokinetic parameters in subjects with different variants of CYP2C8 and CYP2C9 isoenzymes...
  34. Mace K, Bowman E, Vautravers P, Shields P, Harris C, Pfeifer A. Characterisation of xenobiotic-metabolising enzyme expression in human bronchial mucosa and peripheral lung tissues. Eur J Cancer. 1998;34:914-20 pubmed
    ..Reverse transcription-polymerase chain reaction (RT-PCR) analysis of phase I enzymes showed CYP1A1 and CYP2C (CYP2C8 and CYP2C18) mRNA expression in all of the 14 bronchial mucosa specimens...
  35. Qi G, Li D, Zhang X. Genetic variation of cytochrome P450 in Uyghur Chinese population. Drug Metab Pharmacokinet. 2018;33:55-60 pubmed publisher
    ..studies of genetic variations in Uyghur Chinese of fifteen CYP450 genes including CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP2J2, CYP2W1, CYP3A4, CYP3A5, CYP4A11, and CYP17A1, which totally covered 277 ..
  36. Itkonen M, Tornio A, Filppula A, Neuvonen M, Neuvonen P, Niemi M, et al. Clopidogrel but not Prasugrel Significantly Inhibits the CYP2C8-mediated Metabolism of Montelukast in Humans. Clin Pharmacol Ther. 2017;: pubmed publisher
    ..Our results imply that clopidogrel is at least moderate inhibitor of CYP2C8, but prasugrel is not a clinically relevant CYP2C8 inhibitor...
  37. Kong T, Kim J, Kwon S, Cheong J, Kim H, In M, et al. Inhibition of cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferases by MAM-2201 in human liver microsomes. Arch Pharm Res. 2017;40:727-735 pubmed publisher
    ..6, 5.4 and 5.0 µM, respectively. MAM-2201 exhibited mechanism-based inhibition of CYP2C8-catalyzed amodiaquine N-de-ethylation with K i and k inact values of 1.0 µM and 0...
  38. Zhu S, Wang L, Cao Z, Wang J, Jing M, Xia Z, et al. Inducible CYP4F12 enhances Hepatitis C virus infection via association with viral nonstructural protein 5B. Biochem Biophys Res Commun. 2016;471:95-102 pubmed publisher
    ..Our results showed that HCV infection induced expression of CYP4F12 protein, which bound to the HCV replication complex to facilitate viral replication. ..
  39. Lesche D, Sigurdardottir V, Setoud R, Englberger L, Fiedler G, Largiadèr C, et al. Influence of CYP3A5 genetic variation on everolimus maintenance dosing after cardiac transplantation. Clin Transplant. 2015;29:1213-20 pubmed publisher
    ..Variants in CYP3A5, CYP3A4, CYP2C8, POR, NR1I2, and ABCB1 were genotyped, and clinical data were retrieved from patient charts...
  40. Gertz M, Tsamandouras N, Säll C, Houston J, Galetin A. Reduced physiologically-based pharmacokinetic model of repaglinide: impact of OATP1B1 and CYP2C8 genotype and source of in vitro data on the prediction of drug-drug interaction risk. Pharm Res. 2014;31:2367-82 pubmed publisher
    ..In addition, the reduced PBPK model was used to assess the effect of both CYP2C8*3 and SLCO1B1 c...
  41. Finta C, Zaphiropoulos P. The human CYP2C locus: a prototype for intergenic and exon repetition splicing events. Genomics. 2000;63:433-8 pubmed
    ..Moreover, chimeric RNA species consisting of exons originating not only from the CYP2C8 and CYP2C18 genes, but also from the CYP2C19 gene were detected...
  42. VandenBrink B, Foti R, Rock D, Wienkers L, Wahlstrom J. Evaluation of CYP2C8 inhibition in vitro: utility of montelukast as a selective CYP2C8 probe substrate. Drug Metab Dispos. 2011;39:1546-54 pubmed publisher
    ..active site based on probe substrate-dependent inhibition profiles, similar studies have not been performed with CYP2C8. The ability to understand CYP2C8 probe substrate sensitivity will enable appropriate in vitro and in vivo probe ..
  43. Kimura S, Pastewka J, Gelboin H, Gonzalez F. cDNA and amino acid sequences of two members of the human P450IIC gene subfamily. Nucleic Acids Res. 1987;15:10053-4 pubmed
  44. Shemesh C, Yu R, Warren M, Liu M, Jahic M, Nichols B, et al. Assessment of the Drug Interaction Potential of Unconjugated and GalNAc3-Conjugated 2'-MOE-ASOs. Mol Ther Nucleic Acids. 2017;9:34-47 pubmed publisher
    ..The inhibition on CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 and induction on CYP1A2, CYP2B6, and CYP3A4 were investigated in ..
  45. Chen J, Zhang J, Zhang X, Qi M, Shi M, Yang J, et al. Effects of diosmetin on nine cytochrome P450 isoforms, UGTs and three drug transporters in vitro. Toxicol Appl Pharmacol. 2017;334:1-7 pubmed publisher
    ..The intensity of the inhibitory effect was followed by CYP2C8, CYP2C9, CYP2C19 and CYP2E1...
  46. Yu J, Ritchie T, Zhou Z, Ragueneau Majlessi I. Key Findings from Preclinical and Clinical Drug Interaction Studies Presented in New Drug and Biological License Applications Approved by the Food and Drug Administration in 2014. Drug Metab Dispos. 2016;44:83-101 pubmed publisher
    ..when coadministered with potent inhibitors): paritaprevir and naloxegol (CYP3A), eliglustat (CYP2D6), dasabuvir (CYP2C8), and tasimelteon and pirfenidone (CYP1A2)...
  47. Lee A, Conney A, Zhu B. Human cytochrome P450 3A7 has a distinct high catalytic activity for the 16alpha-hydroxylation of estrone but not 17beta-estradiol. Cancer Res. 2003;63:6532-6 pubmed
  48. Weise A, Prause S, Eidens M, Weber M, Kann P, Forst T, et al. Prevalence of CYP450 gene variations in patients with type 2 diabetes. Clin Lab. 2010;56:311-8 pubmed
    ..Genomic DNA was isolated from EDTA blood. Mutation analysis for CYP2C8 (*2/*3/*4), CYP2C9 (*2/*3), CYP2C19 (*2/*3), CYP2D6 (*3/*4/*5/*6) and PPARgamma (P12A) was performed by means of ..
  49. Patel O, Muller C, Joubert E, Louw J, Rosenkranz B, Awortwe C. Inhibitory Interactions of Aspalathus linearis (Rooibos) Extracts and Compounds, Aspalathin and Z-2-(?-d-Glucopyranosyloxy)-3-phenylpropenoic Acid, on Cytochromes Metabolizing Hypoglycemic and Hypolipidemic Drugs. Molecules. 2016;21: pubmed
    ..Cytochrome P450 enzymes, CYP2C8, CYP2C9, and CYP3A4, are important in the metabolism of hypoglycemic drugs, such as thiazolidinediones (TZDs) and ..
  50. Lee M, Apellániz Ruiz M, Johansson I, Vikingsson S, Bergmann T, Brøsen K, et al. Role of cytochrome P450 2C8*3 (CYP2C8*3) in paclitaxel metabolism and paclitaxel-induced neurotoxicity. Pharmacogenomics. 2015;16:929-37 pubmed publisher
    The CYP2C8*3 allele has been suggested as a risk factor for paclitaxel-induced neuropathy but the data hitherto published are conflicting...
  51. Inoue K, Inazawa J, Suzuki Y, Shimada T, Yamazaki H, Guengerich F, et al. Fluorescence in situ hybridization analysis of chromosomal localization of three human cytochrome P450 2C genes (CYP2C8, 2C9, and 2C10) at 10q24.1. Jpn J Hum Genet. 1994;39:337-43 pubmed
    Chromosomal localization of three human cytochrome P450 genes belonging to the CYP2C subfamily (CYP2C8, 2C9, and 2C10) was identified by fluorescence in situ hybridization (FISH)...
  52. Fasinu P, Gutmann H, Schiller H, James A, Bouic P, Rosenkranz B. The potential of Sutherlandia frutescens for herb-drug interaction. Drug Metab Dispos. 2013;41:488-97 pubmed publisher
    ..0 µg/ml), CYP2A6 (IC(50) = 160 µg/ml), CYP2B6 (IC(50) = 20.0 µg/ml), CYP2C8 (IC(50) = 22.4 µg/ml), CYP2C9 (IC(50) = 23.0 µg/ml), CYP2C19 (IC(50) = 35.9 µg/ml), and CYP3A4/5 (IC(50) = 17...
  53. Ufer M, Mosyagin I, Muhle H, Jacobsen T, Haenisch S, Häsler R, et al. Non-response to antiepileptic pharmacotherapy is associated with the ABCC2 -24C>T polymorphism in young and adult patients with epilepsy. Pharmacogenet Genomics. 2009;19:353-62 pubmed
    ..5+/-6.54 years) were genotyped for nine putatively functionally relevant ABCB1, ABCC2, CYP2C8, CYP2C9, and CYP2C19 polymorphisms. In addition, 70 adult patients (35 females, age: 41.9+/-11...
  54. Shao Z, Fu Z, Stahl A, Joyal J, Hatton C, Juan A, et al. Cytochrome P450 2C8 ?3-long-chain polyunsaturated fatty acid metabolites increase mouse retinal pathologic neovascularization--brief report. Arterioscler Thromb Vasc Biol. 2014;34:581-6 pubmed publisher
    ..Cytochrome P450 epoxygenases (CYP2C8) also metabolize LCPUFAs, producing bioactive epoxides, which are inactivated by soluble epoxide hydrolase (sEH) ..
  55. Nakajima M, Fujiki Y, Kyo S, Kanaya T, Nakamura M, Maida Y, et al. Pharmacokinetics of paclitaxel in ovarian cancer patients and genetic polymorphisms of CYP2C8, CYP3A4, and MDR1. J Clin Pharmacol. 2005;45:674-82 pubmed
    ..its metabolites in Japanese ovarian cancer patients were investigated in relation to genetic polymorphisms of the CYP2C8, CYP3A4, and MDR1 genes...
  56. Zhou W, Johnson T, Bui K, Cheung S, Li J, Xu H, et al. Predictive Performance of Physiologically Based Pharmacokinetic (PBPK) Modeling of Drugs Extensively Metabolized by Major Cytochrome P450s in Children. Clin Pharmacol Ther. 2017;: pubmed publisher
    ..predictive performance of the PBPK approach for 10 drugs extensively metabolized by CYP1A2 (theophylline), CYP2C8 (desloratidine, montelukast), CYP2C9 (diclofenac), CYP2C19 (esomeprazole, lansoprazole), CYP2D6 (tramadol), and ..
  57. Cuyàs E, Olano Martin E, Khymenets O, Hernandez L, Jofre Monseny L, Grandoso L, et al. Errors and reproducibility of DNA array-based detection of allelic variants in ADME genes: PHARMAchip. Pharmacogenomics. 2010;11:257-66 pubmed publisher
    ..Some of the discrepancies between tests were related to allelic variants not monitored in a particular microarray and the quality of the genomic DNA used. ..
  58. Gandara D, Kawaguchi T, Crowley J, Moon J, Furuse K, Kawahara M, et al. Japanese-US common-arm analysis of paclitaxel plus carboplatin in advanced non-small-cell lung cancer: a model for assessing population-related pharmacogenomics. J Clin Oncol. 2009;27:3540-6 pubmed publisher
    ..Genotypic variants of CYP3A4, CYP3A5, CYP2C8, NR1I2-206, ABCB1, ERCC1, and ERCC2 were analyzed by pyrosequencing or by PCR restriction fragment length ..
  59. Tan M, Yoshida K, Zhao P, Zhang L, Nolin T, Piquette Miller M, et al. Effect of Chronic Kidney Disease on Nonrenal Elimination Pathways: A Systematic Assessment of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and OATP. Clin Pharmacol Ther. 2017;: pubmed publisher
    ..Therefore, the effect of CKD on the disposition of CYP1A2-metabolized, CYP2C8-metabolized, CYP2C9-metabolized, CYP2C19-metabolized, and organic anion-transporting polypeptide (OATP)-..
  60. Yi X, Lin J, Wang Y, Zhou J, Zhou Q. Interaction among CYP2C8, GPIIIa and P2Y12 variants increase susceptibility to ischemic stroke in Chinese population. Oncotarget. 2017;8:70811-70820 pubmed publisher
    ..The aim of the present study was to investigate the association of fifteen variants with IS and to determine whether these gene-gene interactions increase the risk of IS...
  61. Kahma H, Filppula A, Neuvonen M, Tarkiainen E, Tornio A, Holmberg M, et al. Clopidogrel Carboxylic Acid Glucuronidation is Mediated Mainly by UGT2B7, UGT2B4, and UGT2B17: Implications for Pharmacogenetics and Drug-Drug Interactions . Drug Metab Dispos. 2018;46:141-150 pubmed publisher
    ..drug clopidogrel is metabolized to an acyl-β-d-glucuronide, which causes time-dependent inactivation of CYP2C8. Our aim was to characterize the UDP-glucuronosyltransferase (UGT) enzymes that are responsible for the formation ..
  62. Wormhoudt L, Ploemen J, De Waziers I, Commandeur J, Beaune P, van Bladeren P, et al. Inter-individual variability in the oxidation of 1,2-dibromoethane: use of heterologously expressed human cytochrome P450 and human liver microsomes. Chem Biol Interact. 1996;101:175-92 pubmed
    ..Out of ten heterologously expressed human P450 isoenzymes (CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2E1, CYP2C8, CYP2C9, CYP2C18, CYP3A4 and CYP3A5), only human CYP2A6, CYP2B6 and CYP2E1 metabolized 1,2-DBE, albeit with ..
  63. Drozdzik M, Busch D, Lapczuk J, Muller J, Ostrowski M, Kurzawski M, et al. Protein abundance of clinically relevant drug metabolizing enzymes in the human liver and intestine: A comparative analysis in paired tissue specimens. Clin Pharmacol Ther. 2017;: pubmed publisher
    ..We explored gene expression (qPCR) and protein abundance (LC-MS/MS) of CYP1A2, CYP2B6, CYP2C8/9/19, CYP2D6, CYP2E1, CYP3A4/5, UGT1A1/3, UGT2B7/15 in the liver, duodenum, jejunum, ileum and colon in paired ..
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  65. Bidstrup T, Damkier P, Olsen A, Ekblom M, Karlsson A, Brøsen K. The impact of CYP2C8 polymorphism and grapefruit juice on the pharmacokinetics of repaglinide. Br J Clin Pharmacol. 2006;61:49-57 pubmed
    The primary aim of the study was to investigate the possible effect of the CYP2C8*3 allele and of grapefruit juice on the pharmacokinetics of repaglinide...
  66. Bergheim I, Bode C, Parlesak A. Distribution of cytochrome P450 2C, 2E1, 3A4, and 3A5 in human colon mucosa. BMC Clin Pharmacol. 2005;5:4 pubmed
    ..Therefore, expression and protein levels of four representative CYPs (CYP2C(8), CYP2E1, CYP3A4, and CYP3A5) were determined in human colon mucosa biopsies obtained from ascending, descending and sigmoid colon...
  67. Chimusa E, Zaitlen N, Daya M, Möller M, van Helden P, Mulder N, et al. Genome-wide association study of ancestry-specific TB risk in the South African Coloured population. Hum Mol Genet. 2014;23:796-809 pubmed publisher
    ..This study provides insights into identifying disease genes and ancestry-specific disease risk in multi-way admixed populations. ..
  68. Perera M, Cavallari L, Limdi N, Gamazon E, Konkashbaev A, Daneshjou R, et al. Genetic variants associated with warfarin dose in African-American individuals: a genome-wide association study. Lancet. 2013;382:790-6 pubmed publisher
    ..National Institutes of Health, American Heart Association, Howard Hughes Medical Institute, Wisconsin Network for Health Research, and the Wellcome Trust. ..
  69. Ma Y, Fu Y, Khojasteh S, Dalvie D, Zhang D. Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8). J Med Chem. 2017;60:8691-8705 pubmed publisher
    ..However, there is growing evidence to suggest that glucuronides can be ligands of human CYP2C8, making CYP2C8 distinct from the other CYP isoforms...
  70. Bergheim I, Wolfgarten E, Bollschweiler E, Holscher A, Bode C, Parlesak A. Cytochrome P450 levels are altered in patients with esophageal squamous-cell carcinoma. World J Gastroenterol. 2007;13:997-1002 pubmed
    ..Protein levels of CYP2E1, CYP2C8, CYP3A4, and CYP3A5 were measured by Western blot...
  71. Han L, Mao G, Chen Y, Li C, Liu Z, Wang Y, et al. [Association of single nucleotide polymorphisms of cytochrome P450 gene with susceptibility to gout in ethnic Han males from coastal regions of Shandong province]. Zhonghua Yi Xue Yi Chuan Xue Za Zhi. 2015;32:538-42 pubmed publisher
    ..Genotyping was carried out with a custom Illumina GoldenGate Genotyping assay to detect SNP rs2275620 of CYP2C8 gene, SNP rs2070676 of CYP2E1 gene, SNP rs837395 of CYP4B1 gene, and SNP rs194150 of TBXAS1 gene...
  72. Liu W, Wang B, Ding H, Wang D, Zeng H. A potential therapeutic effect of CYP2C8 overexpression on anti-TNF-? activity. Int J Mol Med. 2014;34:725-32 pubmed publisher
    ..The present study was conducted to determine whether CYP2C8 gene overexpression was able to increase the level of EETs, and subsequently prevent TNF-? induced inflammation ..
  73. Lampreabe I, Gainza de los Rios F, Arrieta Gutiérrez A, Jofre Monseny L, Rodriguez M, Amenabar Iribar J, et al. Toward personalized medicine in renal transplantation. Transplant Proc. 2010;42:2864-7 pubmed publisher
    ..Determination of the CYP3A5 genotype might be used to predict initial TRL requirements, although other genetic variants also provide important information to adjust the drug dose. ..
  74. Muthiah Y, Lee W, Teh L, Ong C, Salleh M, Ismail R. A simple multiplex PCR method for the concurrent detection of three CYP2C8 variants. Clin Chim Acta. 2004;349:191-8 pubmed
    ..We developed and optimized a variant-specific PCR techniques to detect CYP2C8*2, CYP2C8*3 and CYP2C8*4. Genomic DNA was extracted from blood using standard extraction methods...
  75. Hanioka N, Matsumoto K, Saito Y, Narimatsu S. Influence of CYP2C8*13 and CYP2C8*14 alleles on amiodarone N-deethylation. Basic Clin Pharmacol Toxicol. 2011;108:359-62 pubmed publisher
  76. Arun Kumar A, Chakradhara Rao U, Umamaheswaran G, Ramu P, Kesavan R, Shewade D, et al. Haplotype structures of common variants of CYP2C8, CYP2C9, and ADRB1 genes in a South Indian population. Genet Test Mol Biomarkers. 2011;15:407-13 pubmed publisher
    ..and genotype frequencies, linkage disequilibrium (LD) patterns, and haplotype structures of common variants of the CYP2C8, CYP2C9, and ADRB1 genes located on chromosome 10...
  77. Grau J, Caballero M, Campayo M, Jansa S, Vargas M, Alos L, et al. Gene single nucleotide polymorphism accumulation improves survival in advanced head and neck cancer patients treated with weekly paclitaxel. Laryngoscope. 2009;119:1484-90 pubmed publisher
    ..We evaluated the presence of SNPs in six genes (CYP2C8, GSTT1, GSTP1, MDR1-57, MDR1-62, and ERCC1) and the response rate (RR), time to progression (TTP), and overall ..
  78. Nakajima M, Fujiki Y, Noda K, Ohtsuka H, Ohkuni H, Kyo S, et al. Genetic polymorphisms of CYP2C8 in Japanese population. Drug Metab Dispos. 2003;31:687-90 pubmed
    b>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...