Home LiteratureArticle Details
PMID: 21270790 Published · ppublish English Journal Article

The missing association: sequencing-based discovery of novel SNPs in VKORC1 and CYP2C9 that affect warfarin dose in African Americans.

Clinical pharmacology and therapeutics ·Vol. 89 ·No. 3 ·2011-03-00 ·Pages 408-15

Perera MA, Gamazon E, Cavallari LH, Patel SR, Poindexter S, Kittles RA, Nicolae D, Cox NJ

Abstract

It is well recognized that the genetic variants VKORC1-1639, CYP2C9*2, and CYP2C9*3 contribute to warfarin dose response. This has led to warfarin dosing algorithms that include these polymorphisms and explains between 47% and 56% of variability in dose in Caucasians. However, these polymorphisms explain significantly less of the variance in dose among African Americans. In order to identify novel variations that affect warfarin dose in African Americans, we used a targeted resequencing strategy that examined evolutionarily conserved sequences and regions of putative transcriptional binding. Through ethnicity-specific warfarin dose model building in 330 African Americans, we identified two novel genetic associations with higher warfarin dose, namely, VKORC1-8191 (rs61162043, P = 0.0041) and 18786 in CYP2C9 (rs7089580, P = 0.035). These novel finds are independent of the previous associations with these genes. Our regression model, encompassing both genetic and clinical variables, explained 40% of the variability in warfarin dose in African-American subjects, significantly more than any model thus far.

MeSH Terms
African Americans/genetics Algorithms Anticoagulants/administration & dosage,pharmacokinetics Aryl Hydrocarbon Hydroxylases/genetics Base Sequence Cohort Studies Cytochrome P-450 CYP2C9 Dose-Response Relationship, Drug Female Genetic Variation Humans Male Middle Aged Mixed Function Oxygenases/genetics Polymorphism, Single Nucleotide Regression Analysis Vitamin K Epoxide Reductases Warfarin/administration & dosage,pharmacokinetics
Chemicals
Anticoagulants Warfarin Mixed Function Oxygenases CYP2C9 protein, human Cytochrome P-450 CYP2C9 Aryl Hydrocarbon Hydroxylases VKORC1 protein, human Vitamin K Epoxide Reductases
Authors & Affiliations
8 authors, click to expand affiliations / ORCID
Perera M A
Department of Medicine, Section of Genetic Medicine, University of Chicago, Chicago, Illinois, USA. [email protected]
Gamazon E
Cavallari L H
Patel S R
Poindexter S
Kittles R A
Nicolae D
Cox N J
References (40)
40 references, click to expand
  1. Detection of cis-element clusters in higher eukaryotic DNA.
    Bioinformatics. 2001 Oct;17(10):878-89 PMID: 11673232
  2. Racial background is a determinant of average warfarin dose required to maintain the INR between 2.0 and 3.0.
    Br J Haematol. 1999 Oct;107(1):207-9 PMID: 10520043
  3. Influence of CYP2C9 Genotype on warfarin dose among African American and European Americans.
    Per Med. 2007 May 1;4(2):157-169 PMID: 19802360
  4. Estimation of the warfarin dose with clinical and pharmacogenetic data.
    N Engl J Med. 2009 Feb 19;360(8):753-64 PMID: 19228618
  5. Pharmacokinetics and pharmacodynamics of the enantiomers of warfarin in man.
    Clin Pharmacol Ther. 1974 Apr;15(4):424-30 PMID: 4821443
  6. PLINK: a tool set for whole-genome association and population-based linkage analyses.
    Am J Hum Genet. 2007 Sep;81(3):559-75 PMID: 17701901
  7. Hydroxylation of warfarin by human cDNA-expressed cytochrome P-450: a role for P-4502C9 in the etiology of (S)-warfarin-drug interactions.
    Chem Res Toxicol. 1992 Jan-Feb;5(1):54-9 PMID: 1581537
  8. CYP4F2 genetic variant alters required warfarin dose.
    Blood. 2008 Apr 15;111(8):4106-12 PMID: 18250228
  9. The pharmacodynamics of the oral anticoagulant drugs.
    Prog Hemost Thromb. 1974;2(0):175-213 PMID: 4137288
  10. Prediction of CYP3A4 enzyme activity using haplotype tag SNPs in African Americans.
    Pharmacogenomics J. 2009 Feb;9(1):49-60 PMID: 18825162
  11. Prioritizing GWAS results: A review of statistical methods and recommendations for their application.
    Am J Hum Genet. 2010 Jan;86(1):6-22 PMID: 20074509
  12. Factors influencing warfarin dose requirements in African-Americans.
    Pharmacogenomics. 2007 Nov;8(11):1535-44 PMID: 18034618
  13. The association of vitamin K status with warfarin sensitivity at the onset of treatment.
    Br J Haematol. 2001 Mar;112(3):572-7 PMID: 11260056
  14. Regulatory polymorphism in vitamin K epoxide reductase complex subunit 1 (VKORC1) affects gene expression and warfarin dose requirement.
    Blood. 2008 Aug 15;112(4):1013-21 PMID: 18523153
  15. Primer3 on the WWW for general users and for biologist programmers.
    Methods Mol Biol. 2000;132:365-86 PMID: 10547847
  16. Systematic overview of warfarin and its drug and food interactions.
    Arch Intern Med. 2005 May 23;165(10):1095-106 PMID: 15911722
  17. Potential role of pharmacogenomics in reducing adverse drug reactions: a systematic review.
    JAMA. 2001 Nov 14;286(18):2270-9 PMID: 11710893
  18. Human P450 metabolism of warfarin.
    Pharmacol Ther. 1997;73(1):67-74 PMID: 9014207
  19. TRANSFAC: an integrated system for gene expression regulation.
    Nucleic Acids Res. 2000 Jan 1;28(1):316-9 PMID: 10592259
  20. The structure of haplotype blocks in the human genome.
    Science. 2002 Jun 21;296(5576):2225-9 PMID: 12029063
  21. A new statistical method for haplotype reconstruction from population data.
    Am J Hum Genet. 2001 Apr;68(4):978-89 PMID: 11254454
  22. Identification of two evolutionarily conserved and functional regulatory elements in intron 2 of the human BRCA1 gene.
    Genomics. 2005 Sep;86(3):316-28 PMID: 15990270
  23. Selecting a maximally informative set of single-nucleotide polymorphisms for association analyses using linkage disequilibrium.
    Am J Hum Genet. 2004 Jan;74(1):106-20 PMID: 14681826
  24. Vitamin K intake and sensitivity to warfarin in patients consuming regular diets.
    Thromb Haemost. 1999 Mar;81(3):396-9 PMID: 10102468
  25. VKORC1 polymorphisms, haplotypes and haplotype groups on warfarin dose among African-Americans and European-Americans.
    Pharmacogenomics. 2008 Oct;9(10):1445-58 PMID: 18855533
  26. Contribution of age, body size, and CYP2C9 genotype to anticoagulant response to warfarin.
    Clin Pharmacol Ther. 2004 Mar;75(3):204-12 PMID: 15001972
  27. Oral anticoagulants: mechanism of action, clinical effectiveness, and optimal therapeutic range.
    Chest. 1998 Nov;114(5 Suppl):445S-469S PMID: 9822057
  28. Management and dosing of warfarin therapy.
    Am J Med. 2000 Oct 15;109(6):481-8 PMID: 11042238
  29. Effect of VKORC1 haplotypes on transcriptional regulation and warfarin dose.
    N Engl J Med. 2005 Jun 2;352(22):2285-93 PMID: 15930419
  30. Warfarin pharmacogenetics: a single VKORC1 polymorphism is predictive of dose across 3 racial groups.
    Blood. 2010 May 6;115(18):3827-34 PMID: 20203262
  31. Role of dietary vitamin K intake in chronic oral anticoagulation: prospective evidence from observational and randomized protocols.
    Am J Med. 2004 May 15;116(10):651-6 PMID: 15121490
  32. Influence of CYP2C9 and VKORC1 on warfarin dose, anticoagulation attainment and maintenance among European-Americans and African-Americans.
    Pharmacogenomics. 2008 May;9(5):511-26 PMID: 18466099
  33. Extending and evaluating a warfarin dosing algorithm that includes CYP4F2 and pooled rare variants of CYP2C9.
    Pharmacogenet Genomics. 2010 Jul;20(7):407-13 PMID: 20442691
  34. Ability of VKORC1 and CYP2C9 to predict therapeutic warfarin dose during the initial weeks of therapy.
    J Thromb Haemost. 2010 Jan;8(1):95-100 PMID: 19874474
  35. Use of pharmacogenetic and clinical factors to predict the therapeutic dose of warfarin.
    Clin Pharmacol Ther. 2008 Sep;84(3):326-31 PMID: 18305455
  36. Dosing algorithms to predict warfarin maintenance dose in Caucasians and African Americans.
    Clin Pharmacol Ther. 2008 Sep;84(3):332-9 PMID: 18596683
  37. Genetic and clinical predictors of warfarin dose requirements in African Americans.
    Clin Pharmacol Ther. 2010 Apr;87(4):459-64 PMID: 20072124
  38. A genome-wide association study confirms VKORC1, CYP2C9, and CYP4F2 as principal genetic determinants of warfarin dose.
    PLoS Genet. 2009 Mar;5(3):e1000433 PMID: 19300499
  39. Sequence diversity and haplotype structure at the human CYP3A cluster.
    Pharmacogenomics J. 2006 Mar-Apr;6(2):105-14 PMID: 16314882
  40. Patient-specific factors predictive of warfarin dosage requirements.
    Ann Pharmacother. 2002 Oct;36(10):1512-7 PMID: 12243598
Article Info
Journal
Clinical pharmacology and therapeutics
Abbr.
Clin Pharmacol Ther
ISSN
1532-6535
Published
2011-03-00
Epub
2011-00-26
Pages
408-15
Language
English
Region
United States
NLM ID
0372741
PMCID
PMC3625373
Subset
IM
Grants
NHLBI NIH HHS · K23 HL089808 · United States
Analysis Services
Analysis Services

Contact

No. 2 Wenbo Road, Zhangqiu District, Jinan, Shandong

Qilu Normal University · Genelibs Bioinformatics Lab

750 Shunhua Rd, Jinan

2F, Bldg F, University Science Park

Tel: 0531-88819269

WeChat Official Account

Follow our WeChat subscription account for real-time updates and the latest in medical and biological research.


Business Email

E-mail: [email protected]