药物转运体在药代动力学方面起到非常重要的作用,它与药物的吸收、分布、排泄、药效发挥、以及药物毒性作用等密切相关。基于转运体的药物间相互作用,还能影响到临床合并治疗药物之间的药代动力学关系。本研究室已经建立了一整套的实用于药代动力学研究和药物间相互作用评价,高效表达人药物转运体蛋白的体外筛选系统,并已将其应用于新药的筛选研究。此方法的特点在于,以表达人药物转运体蛋白的宿主培养细胞为研究对象,在临床前期提供与临床试验相似的研究结果,今后必将成为药物研发领域有用的评价方法。 Drug transporters play a very important role in pharmacokinetics, which is closely related to the absorption, distribution, excretion, drug efficacy and drug toxicity of drugs. Transporter-based drug-drug interactions can also affect the pharmacokinetic relationship between clinically pooled therapies. In our laboratory, we have established a set of in vitro screening systems that are useful in pharmacokinetic studies and drug-drug interactions to efficiently express human drug transporter proteins and have been used in the screening of new drugs. This method is characterized by the host cultured cells expressing human drug transporter protein as the research object, providing clinical research in preclinical similar research results, the future will become a useful evaluation method in the field of drug development.