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NVP-DPP728 is a **potent, selective, orally active small-molecule inhibitor** of **dipeptidyl peptidase IV (DPP-IV; also known as DPP-4)**, with a \(K_i\) of 11 nM and high selectivity over DPP-II and related proline-cleaving enzymes[1][3][7]. It **acts by reversibly inhibiting DPP-IV**, thereby preventing the degradation of incretin hormones such as **glucagon-like peptide-1 (GLP-1)**, which leads to increased insulin secretion in response to meals and improved glucose tolerance[1][3]. NVP-DPP728 demonstrated significant **antidiabetic effects in animal models** and in **early clinical trials for type 2 diabetes,** improving glycemic control with good tolerability[2][4][6]. The development of NVP-DPP728 was pivotal as it provided clinical proof-of-concept for DPP-4 inhibition as a therapeutic approach for type 2 diabetes[6].
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