ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin.
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.
Tomlinson
B
B
Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Prince of Wales Hospital, Shatin, Hong Kong. btomlinson@cuhk.edu.hk
Hu
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M
Lee
V W Y
VW
Lui
S S H
SS
Chu
T T W
TT
Poon
E W M
EW
Ko
G T C
GT
Baum
L
L
Tam
L S
LS
Li
E K
EK
D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000235:genetics*; D000328:Adult; D000368:Aged; D044466:Asian People / Q000235:genetics; D008078:Cholesterol, LDL / Q000097:blood* / Q000235:genetics; D004311:Double-Blind Method; D005260:Female; D005464:Fluorobenzenes / Q000493:pharmacokinetics / Q000627:therapeutic use*; D005500:Follow-Up Studies; D006801:Humans; D006937:Hypercholesterolemia / Q000097:blood / Q000188:drug therapy* / Q000235:genetics*; D008297:Male; D008875:Middle Aged; D009363:Neoplasm Proteins / Q000235:genetics*; D020641:Polymorphism, Single Nucleotide / Q000235:genetics*; D011743:Pyrimidines / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides / Q000493:pharmacokinetics / Q000627:therapeutic use*
C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D008078:Cholesterol, LDL; D005464:Fluorobenzenes; D009363:Neoplasm Proteins; D011743:Pyrimidines; D013449:Sulfonamides; D000068718:Rosuvastatin Calcium