alexa ABCB1 haplotypes differentially affect the pharmacokinetics of the acid and lactone forms of simvastatin and atorvastatin.
Pharmaceutical Sciences

Pharmaceutical Sciences

Journal of Pharmacogenomics & Pharmacoproteomics

Author(s): Keskitalo JE, Kurkinen KJ, Neuvoneni PJ, Niemi M

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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.
This article was published in Clin Pharmacol Ther and referenced in Journal of Pharmacogenomics & Pharmacoproteomics

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