Incretin levels approach normal physiological values following treatment with dipeptidyl peptidase (DPP)-IV inhibitors. This is in contrast to incretin levels resulting from the exogenous administration of glucagon-like peptide (GLP)-1 and its analogs, which can reach super-physiological values. This review describes the role of DPP-IV inhibitors as incretin enhancers in the regulation of glucose homeostasis in type 2 diabetic patients. The roles of incretins and the effect of DPP-IV on their actions are described, as are new therapeutic interventions based on the restoration of impaired incretin secretion in type 2 diabetic patients and obese individuals. In addition, the relevance of DPP-IV inhibition for weight control, its potential influence on beta-cell mass, and possible new indications are discussed, as are the implications of the currently available clinical data.
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