Pharmacokinetics and pharmacodynamics constitute the foundation of modern pharmacology. PK/PD modeling is to profile the time process of pharmacological effects after a certain dosage is given. Investigating the relationship between PK and PD is helpful not only in instructing the clinical application, but also in the evaluation of new drugs and exploitation of new preparations etc. The present situation concerning the application of PK/PD modeling in the pharmacology,toxicology and development of new medicine is reviewed.