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- Title
Impact of the OATP1B1 c.521T>C single nucleotide polymorphism on the pharmacokinetics of exemestane in healthy post-menopausal female volunteers.
- Authors
Gregory, B. J.; Chen, S. M.; Murphy, M. A.; Atchley, D. H.; Kamdem, L. K.
- Abstract
What is known and objective OATP1B1 mediates the transport of a diverse range of amphiphilic organic compounds that include bile acids, steroid conjugates and hormones. This retrospective pharmacogenetic study was conducted to assess the impact of the OATP1B1 c.521T>C single nucleotide polymorphism ( SNP) on the pharmacokinetics of the steroidal aromatase inhibitor drug exemestane in healthy volunteers. Methods Exemestane (25 mg) was administered orally to 14 healthy post-menopausal women. All of the 14 subjects were sampled for pharmacokinetic ( PK) analyses and retrospectively genotyped for OATP1B1 c.521T>C (rs 4149056). Results and discussion Of the 14 subjects enrolled in the study, five were carriers of the minor C allele ( OATP1B1 c.521 TC+ CC) and the remaining nine were carriers of the OATP1B1 c.521 TT genotype. PK was assessed over 8 hours post-dosing. Our results showed statistically significant differences ( P=.04) in the plasma exemestane AUC0-8 between the OATP1B1 genotype groups. Our data also showed statistically significant differences ( P=.04) in the plasma AUC0-8 of 17-hydroexemestane (the major biologically active metabolite) between the OATP1B1 genotype groups. What is new and conclusion Our data suggest that the OAPTP1B1 c.521T>C SNP may influence exemestane pharmacokinetics in humans.
- Subjects
GENETIC polymorphisms; PHARMACOGENOMICS; PROBABILITY theory; RESEARCH funding; TREATMENT effectiveness; EXEMESTANE
- Publication
Journal of Clinical Pharmacy & Therapeutics, 2017, Vol 42, Issue 5, p547
- ISSN
0269-4727
- Publication type
Article
- DOI
10.1111/jcpt.12569