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Genetic Variation Impacts Pharmacokinetics of Exemestane

Significant differences in plasma exemestane area under the curve for OATP1B1 genotype groups


THURSDAY, Aug. 3, 2017 (HealthDay News) -- The OATP1B1 c.521>C single nucleotide polymorphism (SNP) influences exemestane pharmacokinetics in healthy postmenopausal women, according to a study published online July 29 in the Journal of Clinical Pharmacy and Therapeutics.

B.J. Gregory, Pharm.D., from the Harding University College of Pharmacy in Searcy, Ark., and colleagues conducted a retrospective pharmacogenetic study to examine the impact of the OATP1B1 c.521T>C SNP (rs4149056) on the pharmacokinetics of exemestane in healthy volunteers. Exemestane was administered orally to 14 healthy postmenopausal women; they were all sampled for pharmacokinetic analyses and genotyped retrospectively.

The researchers found that five of the subjects were carriers of the minor C allele (OATP1B1 c.521TC+ CC) and nine were carriers of OATP1B1 c.521TT genotype. Over eight-hours post-dosing, pharmacokinetics were analyzed. The OATP1B1 genotype groups had statistically significant differences in the plasma exemestane area under the curve (AUC0-8) (P = 0.04). Statistically significant differences were also seen in the plasma AUC0-8 of 17-hydroexemestane between the OATP1B1 genotype groups (P = 0.04).

"Our data suggest that the OATP1B1 c.521T>C SNP may influence exemestane pharmacokinetics in humans," the authors write.

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