Abstract：
UNASSIGNED: Determining whether a new drug is a substrate, inhibitor or inducer of efflux or uptake membrane transporters has become a routine process during drug discovery and development. In vitro assays are utilized to establish whether a new drug has the potential to be an object (substrate) or precipitant (inhibitor, inducer) in transporter-mediated clinical drug-drug interactions. The findings from these in vitro experiments are then used to determine whether further in vivo drug interaction studies are necessary for a new drug.
UNASSIGNED: This article provides an update on in vitro transporter assays, focusing on new uses of transfected cells, time-dependent inhibition, transporter induction, and complex model systems.
UNASSIGNED: The newer in vitro assays add to the toolbox in defining new drugs as transporter substrates, inhibitors, or inducers. Complex models such as spheroids, organoids, and microphysiological systems require standardization and further research with model transporter substrates and inhibitors. In drug discovery, the more traditional transporter assays may be employed as substrate and inhibitor screening assays. In drug development, more complex cell models can be employed in later drug development to better understand how transporter(s) are involved in the absorption, distribution, and excretion of new drugs.
UNASSIGNED: This article provides an update on in vitro transporter assays, focusing on new uses of transfected cells, time-dependent inhibition, transporter induction, and complex model systems.
UNASSIGNED: The newer in vitro assays add to the toolbox in defining new drugs as transporter substrates, inhibitors, or inducers. Complex models such as spheroids, organoids, and microphysiological systems require standardization and further research with model transporter substrates and inhibitors. In drug discovery, the more traditional transporter assays may be employed as substrate and inhibitor screening assays. In drug development, more complex cell models can be employed in later drug development to better understand how transporter(s) are involved in the absorption, distribution, and excretion of new drugs.
摘要：
■确定新药是否是底物，外排或摄取膜转运蛋白的抑制剂或诱导剂已成为药物发现和开发过程中的常规过程。体外测定用于确定新药是否有可能成为目标（底物）或沉淀剂（抑制剂，诱导剂）在转运蛋白介导的临床药物相互作用中。然后将这些体外实验的发现用于确定新药是否需要进一步的体内药物相互作用研究。
■本文提供了有关体外转运蛋白测定的最新信息，专注于转染细胞的新用途，时间依赖性抑制，转运蛋白诱导，和复杂的模型系统。
■较新的体外测定法在定义新药作为转运底物时增加了工具箱，抑制剂，或诱导物。复杂的模型，如球体，类器官，和微生理系统需要标准化和进一步研究模型转运蛋白底物和抑制剂。在药物发现中，更传统的转运蛋白测定可以用作底物和抑制剂筛选测定。在药物开发中，更复杂的细胞模型可以在以后的药物开发中使用，以更好地了解转运蛋白如何参与吸收，分布，以及新药的排泄.
■本文提供了有关体外转运蛋白测定的最新信息，专注于转染细胞的新用途，时间依赖性抑制，转运蛋白诱导，和复杂的模型系统。
■较新的体外测定法在定义新药作为转运底物时增加了工具箱，抑制剂，或诱导物。复杂的模型，如球体，类器官，和微生理系统需要标准化和进一步研究模型转运蛋白底物和抑制剂。在药物发现中，更传统的转运蛋白测定可以用作底物和抑制剂筛选测定。在药物开发中，更复杂的细胞模型可以在以后的药物开发中使用，以更好地了解转运蛋白如何参与吸收，分布，以及新药的排泄.
