Abstract
ABCB1 haplotypes were determined in 534 healthy Finnish volunteers, of whom 24 participated in a pharmacokinetic study on simvastatin and atorvastatin. The frequencies of occurrence of haplotypes c.1236T-c.2677T-c.3435T and c.1236C-c.2677G-c.3435C were 42.7 and 34.4%, respectively. The simvastatin acid AUC(0-12h) was 60% larger, the atorvastatin AUC(0-infinity) 55% larger, and the atorvastatin half-life 24% longer in subjects with the ABCB1 TTT/TTT genotype (n = 12) than in those with the CGC/CGC genotype (n = 12) (P < 0.05), but there were no differences between the two genotypes with respect to the pharmacokinetics of the lactones of these drugs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics*
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Area Under Curve
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Atorvastatin
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Cross-Over Studies
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Female
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Finland
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Half-Life
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Haplotypes
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Heptanoic Acids / pharmacokinetics*
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Humans
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Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics*
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Lactones / pharmacokinetics*
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Male
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Polymorphism, Single Nucleotide
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Pyrroles / pharmacokinetics*
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Simvastatin / pharmacokinetics*
Substances
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ABCB1 protein, human
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Heptanoic Acids
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Hydroxymethylglutaryl-CoA Reductase Inhibitors
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Lactones
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Pyrroles
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Atorvastatin
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Simvastatin