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Impact of ABCC2, ABCG2 and SLCO1B1 polymorphisms on the pharmacokinetics of pitavastatin in humans

 Eun Sil OH  ;  Choon OK KIM  ;  Sung Kweon CHO  ;  Min Soo PARK  ;  Jae-Yong CHUNG 
 Drug Metabolism and Pharmacokinetics, Vol.28(3) : 196-202, 2013 
Journal Title
 Drug Metabolism and Pharmacokinetics 
Issue Date
Pitavastatin, a 3-hydroxyl-3-methylglutaryl-coenzyme A reductase inhibitor is distributed to the liver, a target organ of action and excreted mainly into the bile. To investigate the impact of influx (OATP1B1) and efflux (MRP2, BCRP) transporter alleles on its disposition, the pharmacokinetic (PK) parameters were compared among the following groups: SLCO1B1 (*15 carrier and non-carrier), ABCC2 (G1249A, C3972T, C−24T, G1549A, and G1774T), and ABCG2 (C421A) single nucleotide polymorphisms in 45 healthy Korean volunteers. Pitavastatin AUClast was higher in individuals carrying the SLCO1B1*15 allele than those not carrying it (144.1 ± 55.3 vs. 84.7 ± 25.7 h·ng/mL [mean ± SD], p = 0.002). The AUClast varied significantly according to the ABCC2 C−24T allele (103.4 ± 42.2, 80.2 ± 23.8, and 39.0 h·ng/mL in CC, CT and TT, respectively; p = 0.027). Other SNPs of ABCC2 and ABCG2 were not significant. The effect of these transporters and body weight on the AUClast and Cmax were tested, and only SLCO1B1 and ABCC2 C−24T genotypes were significant factors by analysis of covariance. These variants accounted for almost 50% of the variation in AUClast and Cmax of pitavastatin. Therefore, ABCC2 C−24T was significantly associated with pitavastatin human PK when the known effect of SLCO1B1*15 was also considered.
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1. College of Medicine (의과대학) > Dept. of Pediatrics (소아청소년과학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Pharmacology (약리학교실) > 1. Journal Papers
Yonsei Authors
Kim, Choon Ok(김춘옥) ORCID logo https://orcid.org/0000-0002-2319-1108
Park, Min Soo(박민수) ORCID logo https://orcid.org/0000-0002-4395-9938
Chung, Jae Yong(정재용)
Cho, Sung Kweon(조성권)
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