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This article reviews the role of pharmacokinetic/pharmacodynamic approaches in the optimization of dosage regimens to maximize antibacterial efficacy while minimizing toxicity and emergence of resistance, and to achieve a high likelihood of therapeutic success. Polymyxin B, an approved drug with a narrow therapeutic window, serves as an illustrative example to highlight the importance of pharmacokinetic/pharmacodynamic modelling in conjunction with experimentation, employing static time-kill studies followed by dynamic in-vitro or in-v