Pharmacokinetic/pharmacodynamic modeling has become an extremely important tool in evaluating and optimizing anti-infective therapy. By systematically linking the pharmacokinetic and pharmacodynamic properties of the anti-infective agent, it is possible to make educated decisions about the correct drug to be used, correct dosing regimen and to estimate the probability of success with the selected dose regimen. This article gives an overview of the current pharmacokinetic/pharmacodynamic approaches for anti-infective agents and discusses their use in optimizing drug therapy.