Pharmacometrics，developed from the conventional pharmacokinetics，is the science of applying mathematical and statistical methods to characterize，understand，and predict a drug′s pharmacokinetic，pharmacodynamic，and biomarker-outcome behaviors.Pharmacometrics has been widely valued for its utility of modeling and simulation in drug research and development，therapeutic drug monitoring and individualized therapy.This paper reviewed the advances of pharmacometrics employed in new drug research and development and therapeutic drug monitoring both at home and abroad.