Pharmacometrics is an emerging science that interprets drug, disease and trial information in a mathematical fashion to inform and facilitate efficient drug development and/or regulatory decisions. Pharmacometric study is increasingly adopted in the regulatory review of new antimicrobial agents. We summarized and reviewed the 31 antimicrobial agents approved by the US Food and Drug Administration (FDA) and the 26 antimicrobial agents approved by European Medicines Agency (EMA) from January 2001 to May 2019. Regulatory concerns in pharmacometric review of antimicrobial agents were expounded with examples, including modeling and simulation methods, effects of internal/external factors on PK parameters, safety and efficacy evaluation in terms of exposure-response analysis, refinement of the wording of product labeling and package leaflet, and possible post-marketing clinical trial. Ongoing communication among regulators, academia, and industry regarding pharmacometrics is encouraged to streamline and facilitate the development of new antimicrobial agents. The industry can maximize its benefit in drug development through continued pharmacometric education/training.