应用药物转运体的药代动力学评价

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。

Pharmacokinetics evaluation on applications of human drug transporter

Drug transporters play an important role in the pharmacokinetics.It is closely related to drug absorption, distribution, elimination, efficacy, and toxicity.And it can also affect the clinical pharmacokinetics by transporter-based drug interactions in the clinical combination therapy.In our laboratory, the high throughput drug transporter screening systems for estimation of human pharmacokinetics and drug-drug interaction were established and have been already applied to the study on drug discovery.In which, cultured cell models expressing human transporter genes are mainly used and should be very useful in the field of drug discovery and development.