The human organic anion transporters OAT1, OAT2, OAT3, OAT4 and URAT1 belong to a family of poly-specific transporters mainly located in kidneys. Selected OATs occur also in liver, placenta, and brain. OATs interact with endogenous metabolic end products such as urate and acidic neutrotransmitter metabolites, as well as with a multitude of widely used drugs, including antibiotics, antihypertensives, antivirals, anti-inflammatory drugs, diuretics and uricosurics. Thereby, OATs play an important role in renal drug elimination and have an impact on pharmacokinetics. In this review we focus on the interaction of human OATs with drugs. We report the affinities of human OATs for drug classes and compare the putative importance of individual OATs for renal drug excretion. The role of OATs as sites of drug-drug interaction and mediators cell toxicity, their gender-dependent regulation in health and diseased states, and the possible impact of single nucleotide polymorphisms are also dealt with.