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Tight race to be the first in a new class of dipeptidyl peptidase IV (DPP-IV) inhibitors for the oral treatment of type 2 diabetes

Tight race to be the first in a new class of dipeptidyl peptidase IV (DPP-IV) inhibitors for the oral treatment of type 2 diabetes


The oral DPP-IV inhibitors vildagliptin (LAF237), sitaglitpin (MK-0431) and saxagliptin (BMS-477118) from Novartis, Merck & Co., and BMS are in advanced phase III development and compete to be “First in Class” of a new oral treatment modality for type 2 diabetes.
Last Updated: 27-Aug-2010

At least five phase II and six phase I DPP-IV inhibitors are closely following and more than 10 further companies are in advanced preclinical R&D. Available data show differences in duration of action and anticipated dosing frequency, whereas data to compare clinical efficacy and safety presently is not available. The high interest of the pharmaceutical industry reflects the market attractivity. The WHO estimates that globally over 170 mln people have diabetes, with type 2 diabetes accounting for 90 % to 95 %. By 2030, the prevalence of diabetes is predicted to double, driven by adverse lifestyle changes. These results were found in a search conducted by La Merie Business Intelligence. The results were published in the January 16 issue of R&D Pipeline News , edited by La Merie Business Intelligence.

Dipeptidyl peptidase IV is an enzyme that rapidly inactivates the insulinotropic hormone glucagon-like peptide-1 (GLP-1). Inhibition of dipeptidyl peptidase IV by DPP-IV inhibitors enhances the hormone activity of GLP-1 and other bioactive peptides (GIP, PACAP38 and GRP), thereby stimulating the release of insulin and reducing the secretion of glucagon. Both effects contribute to regulation of the elevated blood glucose levels in type 2 diabetic patients as measured by hemoglobin A1c (HbA1c).

Available data from clinical phase II data suggest that long term treatment with DPP-IV inhibitors was well tolerated and was not associated with weight gain. The DPP-IV inhibitors are being evaluated as both monotherapy and in combination with other standard antidiabetic drugs, e.g. metformin. Regulatory filings of the first DPP-IV inhibitors are expected in 2006. The major advantages of DPP-IV inhibitors are the ability to achieve sustainable reductions in HbA1c with an orally administered, well tolerated agent. Other classes of new antidiabetic medications include GLP-1 agonists and dual PPAR agonists. However, GLP-1 agonists require administration by injection and dual PPAR agonists are associated with safety concerns.

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