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.