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
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Comparative Study
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Randomized Controlled Trial
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily G, Member 2
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ATP-Binding Cassette Transporters / genetics*
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Adult
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Aged
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Asian People / genetics
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Cholesterol, LDL / blood*
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Cholesterol, LDL / genetics
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Double-Blind Method
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Female
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Fluorobenzenes / pharmacokinetics
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Fluorobenzenes / therapeutic use*
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Follow-Up Studies
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Humans
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Hypercholesterolemia / blood
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Hypercholesterolemia / drug therapy*
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Hypercholesterolemia / genetics*
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Male
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Middle Aged
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Neoplasm Proteins / genetics*
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Polymorphism, Single Nucleotide / genetics*
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Pyrimidines / pharmacokinetics
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Pyrimidines / therapeutic use*
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Rosuvastatin Calcium
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Sulfonamides / pharmacokinetics
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Sulfonamides / therapeutic use*
Substances
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ABCG2 protein, human
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ATP Binding Cassette Transporter, Subfamily G, Member 2
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ATP-Binding Cassette Transporters
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Cholesterol, LDL
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Fluorobenzenes
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Neoplasm Proteins
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Pyrimidines
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Sulfonamides
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Rosuvastatin Calcium