Abstract : Pomegranate (Punica granatum L.) is an ancient fruit that is still part of diet all over the world. Health-promoting effects have long been attributed to this fruit; modern research supports the use of pomegranate as a folk remedy for diabetes, metabolic syndrome, and many other ailments. Many interactions have been reported between different food substances and drugs that would alter the effect of the drug, and some are known to cause serious consequences on the health. The importance of diet-drug interactions has prompted the study of the effect of concurrent admiration of different food substances to determine drugs’ dosing, timing, and formulation for new drug candidates before being marketed. This review provides an overview of current knowledge of the effect of pomegranate juice on different enzymes and transporters that modulate the pharmacokinetic parameters by using different liquid chromatographic bioanalytical methods.