Identification of genetic variants associated with response to statin therapy

Arterioscler Thromb Vasc Biol. 2009 Sep;29(9):1310-5. doi: 10.1161/ATVBAHA.109.188474. Epub 2009 Aug 10.

Abstract

Objective: The purpose of this study was to test the association between polymorphisms in genes involved in either LDL cholesterol (LDL-C) metabolism or statin pharmacokinetics and LDL-C reduction with statins.

Methods and results: 49 tagging and candidate polymorphisms in 9 genes were genotyped in 1507 post-ACS subjects randomized to atorvastatin or pravastatin. Two polymorphisms (rs7412, rs429358) that define the epsilon2, epsilon3, and epsilon4 isoforms of apolipoprotein E were significantly associated with percent reduction in LDL-C with atorvastatin (epsilon2 carriers 53.8%, epsilon3/epsilon3 48.1%, and epsilon4 carriers 46.4%, respectively, P=0.00039) and replicated in the pravastatin arm (epsilon2 carriers 22.1%, epsilon3/epsilon3 21.8%, and epsilon4 carriers 16.6%, respectively, P=0.00038). The proportion of subjects achieving an LDL-C < or =70 mg/dL at day 30 was higher for epsilon2 than epsilon4 carriers (P=1.3 x 10(-5)). In the pravastatin group, the triallelic rs2032582 variant (G2677T/A) in ABCB1 was associated with the percent reduction in LDL-C (GG 23.3%, non-G heterozygote 20.3%, and non-G homozygote 17.4%, P=0.042).

Conclusions: Carriers of APOE epsilon2 versus epsilon4 had significantly greater LDL-C reduction with atorvastatin and with pravastatin, and more frequently achieved a guideline-recommended LDL-C < or =70 mg/dL. Polymorphisms in triallelic G2677T/A variant in ABCB1 were associated with the degree of LDL-C lowering with pravastatin.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics*
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Acute Coronary Syndrome / drug therapy*
  • Acute Coronary Syndrome / genetics*
  • Acute Coronary Syndrome / metabolism
  • Apolipoproteins E / genetics*
  • Apolipoproteins E / metabolism
  • Atorvastatin
  • Biotransformation / genetics
  • Cholesterol, LDL / blood
  • Haplotypes
  • Heptanoic Acids / pharmacokinetics
  • Heptanoic Acids / therapeutic use*
  • Heterozygote
  • Homozygote
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use*
  • Lipid Metabolism / drug effects
  • Lipid Metabolism / genetics
  • Phenotype
  • Polymorphism, Genetic*
  • Practice Guidelines as Topic
  • Pravastatin / pharmacokinetics
  • Pravastatin / therapeutic use*
  • Pyrroles / pharmacokinetics
  • Pyrroles / therapeutic use*
  • Treatment Outcome

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Apolipoproteins E
  • Cholesterol, LDL
  • Heptanoic Acids
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Pyrroles
  • Atorvastatin
  • Pravastatin