This talk will provide an overview of recent knowledge on the (patho)physiological and pharmacological functions of organic cation transporters in the lung. The organic cation transporters (OCT) 1, 2 and 3 and novel organic cation transporters (OCTN) 1 and 2 of the solute carrier 22 (SLC22) family are involved in the various cellular transport mechanisms of endogenous compounds such as neurotransmitters and l-carnitine and further play an important role in the interaction with inhaled drugs such as beta2-agonists and anticholinergic drugs. They may be associated with the development of chronic lung diseases such as asthma and chronic obstructive pulmonary disease (COPD). In particular OCTN2 may be a potential target to enhance the pulmonary delivery of inhaled drugs for better therapeutical responsiveness in patients. The talk will further elucidate this and discuss future options of OCT/N molecular targets for therapeutic approaches.