SLCO1B1多态性明显影响辛伐他汀酸的药物动力学。
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Pasanen可,Neuvonen M, Neuvonen PJ,尼米M
SLCO1B1多态性明显影响辛伐他汀酸的药物动力学。
Pharmacogenet基因组学。2006年12月,16 (12):873 - 9。fpc.0000230416.82349.90 doi: 10.1097/01.。
- PubMed ID
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17108811 (在PubMed]
- 文摘
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背景和目的:有机阴离子运输多肽1 b1 (OATP1B1)是一个吸收转运体位于人类肝细胞的正弦膜。本研究旨在探讨影响SLCO1B1遗传多态性的基因编码OATP1B1辛伐他汀的药物动力学。方法:四个健康志愿者的纯合子SLCO1B1 c。与杂合的521 cc基因型,12 c。521 tc与纯合基因型和16 c。招募了521 tt基因型(控制)。每个参与者摄取一个40毫克剂量的辛伐他汀。等离子体浓度的辛伐他汀(不活跃的内酯)及其活性代谢物辛伐他汀酸测定12 h。结果:辛伐他汀酸的AUC0-infinity高出221%到120的参与者SLCO1B1 c。521 cc基因型比c。521 tc和c。分别521 tt(参考)基因型(P < 0.001)。辛伐他汀酸的Cmax高出200%到162的参与者c。521 cc基因型比c。521 tc和c。521 tt基因型(P < 0.001)。辛伐他汀酸早些时候发生在参与者的Cmax c。521 cc和c。521TC genotypes than in those with the c.521TT genotype (P<0.05). No association existed between the SLCO1B1 genotype and the elimination half-life of simvastatin acid. Moreover, no statistically significant association was seen between the SLCO1B1 genotype and the pharmacokinetics of simvastatin lactone. CONCLUSIONS: SLCO1B1 polymorphism markedly affects the pharmacokinetics of active simvastatin acid, but has no significant effect on parent simvastatin. Raised plasma concentrations of simvastatin acid in patients carrying the SLCO1B1 c.521C variant allele may enhance the risk of systemic adverse effects during simvastatin treatment. In addition, reduced uptake of simvastatin acid by OATP1B1 into the liver in patients with the c.521C allele could reduce its cholesterol-lowering efficacy.
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药物 转运体 类 生物 药理作用 行动 辛伐他汀 溶质载体有机阴离子转运蛋白家族成员1 b1 蛋白质 人类 未知的底物抑制剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
