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Influence of CYP2D6 gene polymorphisms on the pharmacokinetics of aripiprazole in healthy Chinese subjects

    Xiaodan Zhang‡

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ‡Authors contributed equally

    Search for more papers by this author

    ,
    Chengquan Liu‡

    Department of Clinical Pharmacology, The First Affiliated Hospital of Hunan University of Medicine, Huaihua, Hunan 418000, China

    ‡Authors contributed equally

    Search for more papers by this author

    ,
    Shuang Zhou

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Ran Xie

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Xu He

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Zhiqi Wang

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Honghong Yi

    Department of Clinical Pharmacology, The First Affiliated Hospital of Hunan University of Medicine, Huaihua, Hunan 418000, China

    ,
    You Shu

    Department of Clinical Pharmacology, The First Affiliated Hospital of Hunan University of Medicine, Huaihua, Hunan 418000, China

    ,
    Zining Wang

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Kun Hu

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Lingyue Ma

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    ,
    Yimin Cui

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    Institute of Clinical Pharmacology, Peking University, No. 38, Xue Yuan Street, Haidian District, Beijing 100191, China

    ,
    Xia Zhao

    *Author for correspondence: Tel.: +86 10 6611 0802;

    E-mail Address: zxyjk@126.com

    Department of Pharmacy, Base for Clinical Trial, Peking University First Hospital, Beijing 100034, China

    &
    Jin Xiang

    **Author for correspondence:

    E-mail Address: 11679295@qq.com

    GCP Center, West China Hospital, Sichuan University, Chengdu 610041, China

    Published Online:https://doi.org/10.2217/pgs-2020-0134

    Background: Pharmacogenetics study was added into 2 bioequivalence trials of aripiprazole. The correlation between CYP2D6 polymorphisms and aripiprazole pharmacokinetics (PK) was analyzed. Materials & methods: A total of 140 subjects were included. A total of 26 CYP2D6 gene alleles were detected. The plasma concentration of aripiprazole was measured by liquid chromatography-tandem mass spectrometry. SPSS Statistics 21 was used to analyze the correlation between CYP2D6 polymorphisms and aripiprazole PK parameters. Results: All of the four PK parameters were significantly influenced by CYP2D6rs1058164 and rs28371699. t1/2 and area under the concentration-time curve exhibited significant difference between CYP2D6 extensive metabolizers and intermediate metabolizers. Conclusion: Aripiprazole PK was greatly influenced by CYP2D6. Attention should be paid to the possible dose adjustment for CYP2D6 intermediate metabolizer population when the drug is used in Chinese patients.

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