Drug transporters and metabolizing enzymes are integral components of drug disposition, governing the absorption, distribution, metabolism, and excretion (ADME) of pharmaceuticals. Their activities critically determine therapeutic efficacy and toxicity profiles, particularly for antimicrobial agents, one of the most widely prescribed drug classes frequently co-administered with other medications. Emerging evidence highlights the clinical significance of the drug-drug interactions (DDIs) mediated by these systems, which may alter antimicrobial pharmacokinetics, compromise treatment outcomes, or precipitate adverse events. With the continuous introduction of novel antimicrobial agents into clinical practice, the role of drug transporters and metabolizing enzymes in the pharmacokinetics of antibiotics and the DDIs between antibiotics and other drugs mediated by these transporters and enzymes are important to determine in order to provide a theoretical basis for the safe and effective use of antimicrobial drugs in clinical use.
Keywords: antimicrobial drugs; drug transporters; drug–drug interactions; metabolizing enzymes; pharmacokinetics.