The major components, biopharmaceutics (BP), pharmacokinetics (PK), population pharmacokinetics (PopPK), pharmacokinetics/pharmacodynamics (PK/PD), modeling and simulation (M&S), and regulatory sciences included in the field of pharmacometrics were outlined, and the principles of modeling and simulation applied in this field were reviewed briefly thereafter.Furthermore, several case studies were reported, including a study of response surface model for the pharmacodynamic drug-drug interactions;a pharmacokinetics/pharmacodynamics/disease progression (PK/PD/DP) integral model by perindopril with spontaneously hypertensive rats;a preclinical PK/PD model to predict schedule-dependent interaction between erlotinib and gemcitabine.Part of the studies reported by other groups in the field of PK/PD of oncology were also introduced.It was concluded that the integration of modeling and simulation of pharmacokinetics, pharmacodynamics and disease progression (PK/PD/DP) are very useful, and clinical studies and practices are able to be benefited by bridging the gap between animal and human studies with these models.