Type 2 diabetes is a complex metabolic disease of epidemic proportions, and is more prevalent in People with a Western life-style. Present treatments consist mainly of insulin secretagogues, metformin and insulin sensitizers. This review will focus on the therapeutic potential of carnitine palmitoyltransferase (CPT) inhibitors, which act on long-chain fatty acids transport into the mitochondria. Particular attention will be devoted to the group of structurally related carnitine inhibitors, where a new selective molecule has now entered clinical development. In the past, a number of compounds have shown interesting characteristics without producing, for several reasons, a clinically available drug.