药代动力学在新药成药性转换医学研究中的作用

 全新分子实体作为新药的研发是一个长期的创新研究,是一个涉及多学科的系统工程。转换研究可以将新候选药物分子的基础实验室研究、临床前研究、临床评价和临床应用广泛联系在一起,建立新的开发模式,进而缩短研发周期和加快向临床推广速度。在全新研发过程和临床试验中,药物代谢和药物处置的属性特征(吸收、分布、代谢、排泄)是用以评价候选药物成药可能性的重要标准。因此,在整个全新的研发模式里,药代动力学研究对于全新分子实体在转换研究过程中的评估起着至关重要的作用。从实验室到临床,从临床到市场的转换研究方式对于提高效率是一种非常重要的策略,其中每一步都涉及大量的药代动力学研究;某一种化学实体成药可能性、早期失败、早期出局等问题可以在第一时间发现。因此,药代动力学评估在药物发现、设计、研发过程中对提高效率、控制成本并进一步获得安全有效的药物有重要价值。

Role of Pharmacokinetics in Translation Research for Research and Development of New Drugs

The research and development of New Molecular Entities (NMEs) as new drugs is a long-term, systematic project involving multiple disciplines. The translation research recently proposed is able to build connection among basic laboratory research, preclinical studies, clinical evaluation and clinical application of new drug candidates to establish a novel development model, therefore, the R&D cycle can be shortened and the approval of new drugs for marketing will be promoted. Both in innovative research and clinical trials, pharmacokinetics and drug disposition (absorption, distribution, metabolism, excretion) properties are important criteria for assessing drug-likeness of candidates. Thus, pharmacokinetic study plays an important role in the translational research for the evaluation of NMEs throughout entire innovative drug R&D process. The pathways from bench to bedside and from bedside to the market in the course of the translational research are important strategy to improve efficiency, in which each step of R&D is associated with PK studies. Possibility of druggability of a certain chemical entity, early failure and early-out issues or success can be spotted at first place. Therefore, pharmacokinetics evaluation in drug discovery, drug design, research and development is valuable to improve the success rate and maintain low costs, and further access to safe, effective drugs for human beings.