Latest research on Vildagliptin

Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions.

Latest findings

All the gliptins took to dedicated CV safety trials except Vildagliptin. [source, 2016]
He was treated with Metformin + Vildagliptin 850/50 mg, Enalapril 20 mg, Atorvastatin 10 mg, rivaroxaban 20 mg, Amlodipine 5 mg, Fluvoxamine 50 mg, and Gliclazide 30 mg. [source, 2016]
In accordance with this hypothesis, studies conducted in Japan with the DPP-4 inhibitor Vildagliptin reported greater reductions in glycated hemoglobin (HbA1c) from lower HbA1c baselines2 than those reported from non-Japanese studies, wherein the majority of the patients are Caucasians of European descent.3,4 [source, 2016]
This pooled analysis aimed to compare the efficacy levels of Vildagliptin action in Japanese and Caucasian patients. [source, 2016]
To directly compare the efficacy of the DPP-4 inhibitor Vildagliptin (50 mg twice daily [bid]) in Japanese and Caucasian populations, we pooled data from all the randomized Vildagliptin monotherapy studies (total of 19 studies) conducted in drug-naïve patients with T2DM, wherein HbA1c was assessed at 12 weeks. [source, 2016]
The data from this pooled analysis support the conclusion that, on average, Japanese physicians initiate treatment at lower levels of glucose, resulting in more Japanese than Caucasian patients reaching HbA1c goals with Vildagliptin. [source, 2016]
Similar reductions from baseline in HbA1c from a lower baseline HbA1c also suggest better efficacy of Vildagliptin in Japanese patients when compared with the results obtained in Caucasians. [source, 2016]
Vildagliptin is known to work by improving β- and α-cell function, as well as through various extrapancreatic actions, which could together yield similar levels of glycemic control. [source, 2016]
Where indicated, cells were washed (1 or 2 x 1h) with Krebs-HEPES buffer (20 mM HEPES, 118 mM NaCl, 4.7 mM KCl, 1.2 mM MgSO4, 5 mM NaHCO3, 1.2 mM KH2PO4, 2.5 mM CaCl2, 5.5 mM glucose, 0.2% BSA (w/v), pH 7.2) containing Vildagliptin (300 μM) prior to addition of test compounds in the same buffer. [source, 2016]
Vildagliptin and other DPP4 inhibitors were shown to be atheroprotective in non‐diabetic and diabetic ApoE‐deficient mice through the activation of both incretin hormones (GLP‐1 and GIP) and restoring insulin production 83. [source, 2015]