Drug intelligence / Profile preview

NVP-DPP728

Development stage
Discontinued
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

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].

Other names
UNII-HCX5M1YIOMUNII-HCX-5M1YIOMUNII-HCX 5M1YIOM(2S)-1-(2-((2-((5-Cyano-2-pyridyl)amino)ethyl)amino)acetyl)pyrrolidine-2-carbonitrile1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)-pyrrolidine(S)-6-((2-((2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl)amino)ethyl)amino)nicotinonitrile3-Pyridinecarbonitrile, 6-((2
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)

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