Released on = January 17, 2006, 4:30 am

Press Release Author = La Merie Business Intelligence

Industry = Biotech

Press Release Summary = 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.

Press Release Body = 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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