Background: Drug transporters and drug metabolism enzymes govern drug absorption, distribution, metabolism and elimination. There were many reports about the environmental pollutants metabolism. However, there are few studies on influence of drug transporters by environmental pollutants such as polychlorinated biphenyl, diesel exhaust particles, permethrin, heavy metals. Herein, an up-to-date review on this topic is presented. Aim: To review the potential regulatory effects of environmental pollutants on the activities of ATP-binding cassette (ABC) efflux, solute carrier (SLC) uptake drug transporters and other transporters. Method: Routinely collected literatures from Pubmed database were utilized. Results: The approaches utilized to study environmental pollutants-transporter interaction include inhibition experiments of specific transporters in cell models (e.g. Caco-2 cells), transport study using drug resistance cell lines or transgenic cell lines expressing transporters in wild type or variant. Many of transporters have been reported to exhibit either positive or negative regulator recognition such as Breast Cancer Resistance Protein (BCRP), Multidrug Resistance Proteins (MRPs), P-glycoprotein (P-gp), Organic Anion Transporters (OATs), Organic Anion Transporting Polypeptides (OATPs), Organic Cation Transporters (OCTs), Multidrug and Toxin Extrusion Transporters (MATEs), Dopamine Transporters (DATs), Glucose transporter (GLUT), Bile Salt Export Pump (BSEP), Divalent Metal Transporter 1 (DMT1). Conclusion: Some environmental pollutants can act as regulators of the drug transporters activity, making contributions to toxicity in human exposed to environmental pollutants. Therefore, it is important to understand the mechanism of pollutants toxicity mediated by drug transporters for the effective management of environmental pollutants.