Abstract: Prodrugs comprising a lipophilic drug linked to a transport moiety that can be taken up by a fatty acid transporter are provided. The transport moiety comprises a lipid chain connected to a hydrophilic group (e.g. a carboxylic acid, a phosphate, or a sphingosine-like moiety). Due to the presence of the transport moiety, the prodrugs are substrates for endogenous fatty acid transporter systems. The transport moiety thus serves as a carrier or targeting moiety to facilitate uptake of the entire prodrug complex by endogenous fatty acid transporter systems, thereby moving the prodrug into cells and tissues where drug distribution and effects are desired. Hydrolysis of the chemical linkage between the lipid-like moiety and the lipophilic drug releases the drug in an active form within the cells or tissues.