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CYP3A5*3 genotype associated with intrasubject pharmacokinetic variation toward tacrolimus in bioequivalence study

 Jin-Oh Kwak  ;  Sung Hee Lee  ;  Gwan Sun Lee  ;  Maeng Sup Kim  ;  Young-Gil Ahn  ;  Ji Hyun Lee  ;  So Won Kim  ;  Kyung Hwan Kim  ;  Min Goo Lee 
 THERAPEUTIC DRUG MONITORING, Vol.32(1) : 67-72, 2010 
Journal Title
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Area Under Curve ; Asian Continental Ancestry Group ; Cross-Over Studies ; Cytochrome P-450 CYP3A/genetics* ; Female ; Genetic Variation ; Genotype ; Humans ; Immunosuppressive Agents/pharmacokinetics* ; Korea ; Male ; Randomized Controlled Trials as Topic ; Tacrolimus/pharmacokinetics* ; Therapeutic Equivalency
tacrolimus ; CYP3A5 ; pharmacokinetics ; intrasubject variation ; bioequivalence
Tacrolimus is metabolized by CYP3A and has highly variable pharmacokinetics. To study the factors contributing to this high variability in pharmacokinetics and to investigate the possibility of genotype-specific clinical applications, the effect of differing CYP3A5 genotypes on the intrasubject coefficients of variation for tacrolimus was investigated. Genotyping for CYP3A5*3 was performed in healthy volunteers who had previously participated in the pharmacokinetic study of 2 tacrolimus formulations with a 2 x 2 cross-over design. Intrasubject coefficients of variation calculated from analysis of variation in CYP3A5*1/*1+*1/*3 (n = 16) and CYP3A5*3/*3 (n = 13) groups were compared. The intrasubject CVs of AUClast and Cmax in the CYP3A5*3/*3 group were about 41.1% and 52.4% greater than those in the CYP3A5*1*1+*1/*3 group. The estimated total sample size for the bioequivalence study of tacrolimus with a 2 x 2 cross-over design was increased by 93.3% for AUClast (n = 30 versus 58) and 121.4% for Cmax (n = 28 versus 62) in the CYP3A5*3/*3 group compared with the CYP3A5*1/*1+*1/*3 group. The intraindividual variability of tacrolimus PK parameters may be associated with the CYP3A5 genotype. We propose that genotyping for CYP3A5 will provide a more efficient approach for bioequivalence designs and therapeutic drug monitoring
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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, Kyung Hwan(김경환)
Park, Min Soo(박민수) ORCID logo https://orcid.org/0000-0002-4395-9938
Lee, Yoon Jung(이윤정)
Lim, Lay Ahyoung(임아영)
Jang, Seong Bok(장성복)
Chung, Jae Yong(정재용)
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