In recent years, a new type of organic cation transporter has been found to transport organic cation drugs like pyrilamine, diphenhydramine and oxycodone in brain capillary endothelial cells, Caco-2 cells and other cells. Its transport activity can not be inhibited by typical organic cation transporter substrates or inhibitors, and its transport characteristics are different from those reported for the organic cation transporters, such as organic cation transporters (OCTs), organic cation/carnitine transporters (OCTNs), multidrug and toxin extrusion transporters (MATE) and the plasma membrane monoamine transporter (PMAT). It is a novel organic cation transporter, called pyrilamine-sensitive H(+)/OC antiporter. This review will present a comprehensive summary to elaborate the transport characteristics, structure of the substrates, tissue expression and the differences with other organic cation transporters.