Pharmacogenetics of OATP transporters reveals that SLCO1B1 c.388A>G variant is determinant of increased atorvastatin response

Int J Mol Sci. 2011;12(9):5815-27. doi: 10.3390/ijms12095815. Epub 2011 Sep 9.

Abstract

Aims: The relationship between variants in SLCO1B1 and SLCO2B1 genes and lipid-lowering response to atorvastatin was investigated.

Material and methods: One-hundred-thirty-six unrelated individuals with hypercholesterolemia were selected and treated with atorvastatin (10 mg/day/4 weeks). They were genotyped with a panel of ancestry informative markers for individual African component of ancestry (ACA) estimation by SNaPshot(®) and SLCO1B1 (c.388A>G, c.463C>A and c.521T>C) and SLCO2B1 (-71T>C) gene polymorphisms were identified by TaqMan(®) Real-time PCR.

Results: Subjects carrying SLCO1B1 c.388GG genotype exhibited significantly high low-density lipoprotein (LDL) cholesterol reduction relative to c.388AA+c.388AG carriers (41 vs. 37%, p = 0.034). Haplotype analysis revealed that homozygous of SLCO1B1*15 (c.521C and c.388G) variant had similar response to statin relative to heterozygous and non-carriers. A multivariate logistic regression analysis confirmed that c.388GG genotype was associated with higher LDL cholesterol reduction in the study population (OR: 3.2, CI95%:1.3-8.0, p < 0.05).

Conclusion: SLCO1B1 c.388A>G polymorphism causes significant increase in atorvastatin response and may be an important marker for predicting efficacy of lipid-lowering therapy.

Keywords: OATP; atorvastatin; pharmacogenetics; single nucleotide polymorphisms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Anticholesteremic Agents / therapeutic use
  • Atorvastatin
  • Female
  • Gene Frequency
  • Genotype
  • Haplotypes
  • Heptanoic Acids / therapeutic use*
  • Humans
  • Hypercholesterolemia / drug therapy*
  • Hypercholesterolemia / genetics*
  • Linkage Disequilibrium
  • Liver-Specific Organic Anion Transporter 1
  • Logistic Models
  • Male
  • Middle Aged
  • Multivariate Analysis
  • Organic Anion Transporters / genetics*
  • Pharmacogenetics / methods
  • Polymorphism, Single Nucleotide*
  • Pyrroles / therapeutic use*
  • Treatment Outcome

Substances

  • Anticholesteremic Agents
  • Heptanoic Acids
  • Liver-Specific Organic Anion Transporter 1
  • Organic Anion Transporters
  • Pyrroles
  • SLCO1B1 protein, human
  • Atorvastatin