Incretin mimetics and DPP-IV inhibitors for the treatment of type 2 diabetes

2005 ◽  
Vol 10 (10) ◽  
pp. 703-710 ◽  
Author(s):  
Loretta L. Nielsen
2006 ◽  
Vol 19 (6) ◽  
pp. 612-620 ◽  
Author(s):  
D. Hinnen ◽  
L. L. Nielsen ◽  
A. Waninger ◽  
P. Kushner

2010 ◽  
Vol 89 (3) ◽  
pp. e49-e52 ◽  
Author(s):  
Seung Jin Han ◽  
Hae Jin Kim ◽  
Sung-E Choi ◽  
Yup Kang ◽  
Kwan Woo Lee ◽  
...  

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Thiquynhnga Nguyen ◽  
Min Gong ◽  
Song Wen ◽  
Xinlu Yuan ◽  
Chaoxun Wang ◽  
...  

Incretin-based therapy is now a prevalent treatment option for patients with type 2 diabetes mellitus (T2DM). It has been associated with considerably good results in the management of hyperglycemia with cardiac or nephron-benefits. For this reason, it is recommended for individuals with cardiovascular diseases in many clinical guidelines. As an incretin hormone, glucagon-like peptide-1 (GLP-1) possesses multiple metabolic benefits such as optimizing energy usage, maintaining body weight, β cell preservation, and suppressing neurodegeneration. However, recent studies indicate that oral antidiabetic medications interact with endogenous or exogenous GLP-1. Since these drugs are transported to distal intestine portions, there are concerns whether these oral drugs directly stimulate intestinal L cells which release GLP-1, or whether they do so via indirect inhibition of the activity of dipeptidyl peptidase-IV (DPP-IV). In this review, we discuss the metabolic relationships between oral antihyperglycemic drugs from the aspect of gut, microbiota, hormones, β cell function, central nervous system, and other cellular mechanisms.


2008 ◽  
Vol 4 (2) ◽  
pp. 101-109 ◽  
Author(s):  
Anthony Stonehouse ◽  
Ted Okerson ◽  
David Kendall ◽  
David Maggs

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Nalinee Poolsup ◽  
Naeti Suksomboon ◽  
Wanwaree Setwiwattanakul

Background and Aim. Diabetes mellitus is a chronic disease that has a great impact on patients and society. Metformin monotherapy is capable of maintaining a target glycemic control only for a short term. The aim of this study was to determine the efficacy of combination therapy of metformin with any antidiabetic agents in type 2 diabetes mellitus (T2DM) patients. Methods. Reports of randomized controlled trials (RCTs) of combination therapy of metformin with various antidiabetic agents in T2DM failing metformin alone were identified. Results. Eight studies were identified in our paper. Thiazolidinediones (TZDs) were as effective as dipeptidyl peptidase IV inhibitors (DPP IV inhs) in reducing HbA1c value (pooled mean difference −0.03%; 95% CI −0.16 to 0.10%). In comparison between TZDs and sulphonylureas (SUs), TZDs reduced fasting plasma insulin (FPI) more effectively than SUs (pool mean difference −5.72 μU/mL; 95% CI −8.21 to −3.22 μU/mL, ), but no significant differences were detected in the effects on HbA1c and fasting plasma glucose (FPG) (pooled mean difference −2.19 mg/dL; 95% CI −11.32 to 6.94 mg/dL, ). Conclusions. Our study showed that TZDs reduced FPG better than did DPP IV inhs and decreased FPI more than did SUs.


2015 ◽  
Vol 93 (7) ◽  
pp. 721-729
Author(s):  
R. Abu Khalaf ◽  
Z. Jarekji ◽  
T. Al-Qirim ◽  
D. Sabbah ◽  
G. Shattat

Inhibition of dipeptidyl peptidase-IV (DPP-IV) prevents the inactivation of gastric inhibitory polypeptide (GIP) and glucagon-like peptide–1 (GLP-1). This increases circulating levels of active GLP-1 and GIP and stimulates insulin secretion, which results in lowering of glucose levels and improvement of the glycemic control in patients with type 2 diabetes. In this study, pharmacophore modeling and docking experiments were carried out and a series of eight novel 2-ethoxy-6,9-disubstituted acridines (13, 15, and 17a–17f) have been designed and synthesized. Then, these compounds were evaluated for their ability to inhibit DPP-IV. Most of the synthesized compounds were proven to have anti-DPP-IV activity where compound 17b displayed the best activity of 43.8% inhibition at 30 μmol/L concentration. Results of this work might be helpful for further optimization to develop more potent DPP-IV inhibitors.


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