The kidney is a key organ for promoting the excretion of drugs and drug metabolites. One of the mechanisms by which the kidney promotes excretion is via active secretion. Secretion of drugs and their metabolites from blood to luminal fluid in the nephron is a protein-mediated process that normally involves either the direct or indirect expenditure of energy. Renal transporters for organic anions are located in the proximal tubule segment of the nephron. The primary transporters of organic anions on the basolateral membrane (BLM) of proximal tubule cells are members of the organic anion transporter (OAT) family (mainly OAT1 and OAT3). The sulfate-anion antiporter 1 (SAT-1; hsat-1) may also contribute to organic anion transport at the basolateral membrane. On the apical membrane, the multi-drug resistance-associated protein 2 (MRP2) is an important transport protein to complete the secretion process. However, there are several transport proteins on the basolateral and apical membranes of proximal tubule cells in human kidneys that have not been fully characterized and whose role in the secretion of organic anions remains to be determined. This review will primarily focus on the human renal basolateral and apical membrane transporters for organic anions that may play a role in the excretion of drugs and drug metabolites.