ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin

Clin Pharmacol Ther. 2010 May;87(5):558-62. doi: 10.1038/clpt.2009.232. Epub 2010 Feb 3.

Abstract

The ATP-binding cassette G2 (ABCG2) c.421C>A (rs2231142) polymorphism influences the pharmacokinetics of rosuvastatin. We examined whether this polymorphism influences the low-density lipoprotein cholesterol (LDL-C)-lowering efficacy of the drug. In 305 Chinese patients with hypercholesterolemia who were treated with rosuvastatin at a dosage of 10 mg daily, the c.421A variant was found to be significantly associated with greater reduction in LDL-C level, in a gene-dose-dependent manner. As compared with subjects with the c.421CC genotype, those with the c.421AA genotype showed a 6.9% greater reduction in LDL-C level, which would be equivalent to the effect obtained by doubling the dose of rosuvastatin.

Publication types

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

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters / genetics*
  • Adult
  • Aged
  • Asian Continental Ancestry Group / genetics
  • Cholesterol, LDL / blood*
  • Cholesterol, LDL / genetics
  • Double-Blind Method
  • Female
  • Fluorobenzenes / pharmacokinetics
  • Fluorobenzenes / therapeutic use*
  • Follow-Up Studies
  • Humans
  • Hypercholesterolemia / blood
  • Hypercholesterolemia / drug therapy*
  • Hypercholesterolemia / genetics*
  • Male
  • Middle Aged
  • Neoplasm Proteins / genetics*
  • Polymorphism, Single Nucleotide / genetics*
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / therapeutic use*
  • Rosuvastatin Calcium
  • Sulfonamides / pharmacokinetics
  • Sulfonamides / therapeutic use*

Substances

  • ABCG2 protein, human
  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters
  • Cholesterol, LDL
  • Fluorobenzenes
  • Neoplasm Proteins
  • Pyrimidines
  • Sulfonamides
  • Rosuvastatin Calcium