Type 2 diabetes mellitus (T2DM) is a worldwide public health problem. The fact that the existing treatments have limitations either because of their side effects as hypoglycaemia and weight gain or their other complications necessitate the need for development of new therapies for glycemic control. The therapeutic approachs represented by the incretin-based therapies, namely the dipeptidyl peptidase-4 (DPP-4) inhibitors and glucagon like peptide-1 (GLP-1) analogues/mimetics, offer a new therapeutic means for treatment of T2DM, in addition to other several even newer therapies in development. A great attention has been focused by many researchers on a number of potential molecular targets in fat cells or adipocytes, as the adipokines. In this article we will review the development of the possible molecular targets for the currently available antidiabetic agents with particular emphasis on incretin-based therapeutic targets as well as molecular targets in adipocytes and other future therapies.