OATP transporter-mediated drug absorption and interaction
OATP transporter-mediated drug absorption and interaction
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DOI：
10.1016/j.coph.2013.09.001
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发表时间：
2013-12-01
影响因子：
4
通讯作者：
Nakanishi, Takeo
中科院分区：
文献类型：
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作者：
Tamai, Ikumi;Nakanishi, Takeo
虽然口服给药是最有利的途径，但肠上皮渗透的确切机制尚不清楚。最近，令人信服的证据表明，吸收转运蛋白，如OATP有助于肠道药物吸收。由于肠道转运蛋白活性的变化可能会改变全身暴露量，因此，对整体肠道吸收机制的全面了解对于预测可能的毒性和实现最佳疗效至关重要。肠腔持续暴露于摄入的食物和饮料，并且它们的组分在肠渗透期间与药物的相互作用也可能是显著的。OATP2B1在人肠道中表达，并转运各种药物。本文综述了OATP 2B1在药物吸收中的重要性以及饮料成分对OATP 2B1功能和表达的可能影响。
Although oral administration of drugs is the most favorable route, the precise mechanism of intestinal epithelial permeation is not well understood. Recently, compelling evidence has emerged to show that absorptive transporters such as OATPs contribute to intestinal drug absorption. Since changes in intestinal transporter activity may alter systemic exposure, a thorough understanding of the overall intestinal absorption mechanism is essential to predict possible toxicity and to achieve optimal therapeutic efficacy. The intestinal lumen is exposed continuously to ingested food and beverages, and interaction of their components with drugs during intestinal permeation might also be significant. OATP2B1 is expressed in human intestine and transports various drugs. In this review, we describe the importance of OATP2B1 in drug absorption and the possible influence beverage components have on OATP2B1 function and expression.