Released on = February 6, 2006, 7:09 am

Press Release Author = La Merie Business Intelligence

Industry = Biotech

Press Release Summary = Twice-daily injection is the benchmark set by exenatide, the
first GLP-1 analog launched in the US by Lilly in June 2005 and half-year sales of
US$ 74.6 mln, which now faces competition by GLP-1 analog treatment modalities with
less frequent dosing.

Press Release Body = Barcelona, Spain | Feb 6, 2006 | The Business Intelligence firm
La Merie S.L. reported today that twice-daily injection is the benchmark set by
exenatide, the first GLP-1 analog launched in the US by Lilly in June 2005 and
half-year sales of US$ 74.6 mln, which now faces competition by GLP-1 analog
treatment modalities with less frequent dosing. More convenience is brought to
patients with once-daily dosing from the closest competitor (Novo Nordisk) which
Lilly counters with a once-a-week injectable drug delivery. Other competitors follow
with sustained release formulations of GLP-1 analogs or develop a nasal spray GLP-1
analog as a non-invasive alternative to injections. Another, yet IND or preclinical
stage approach is the development of fusion proteins of GLP-1 with large carrier
proteins such as albumin or transferrin leading to even longer half-lives, thus
potentially allowing dosing every 2 or 3 weeks. These results were found in a search
conducted by La Merie Business Intelligence published in the February 6 issue of R&D
Pipeline News, edited by La Merie, and can be acquired as a Project Pipeline List at
www.pipelinereview.com.

Both enzymatic cleavage and renal clearance contribute to a very short circulating
half-life of several minutes for native GLP-1 which is a 30-amino acid gut peptide
produced in enteroendocrine cells located in the distal ileum and colon. Thus, GLP-1
analogs have been constructed with resistance to enzymatic cleavage. These GLP-1
mimetics bind to GLP-1 receptors with similar affinity and produce biological
actions identical to those of native GLP-1 which controls blood glucose via multiple
actions including stimulation of insulin secretion and inhibition of both glucagon
secretion and gastric emptying. Preclinical data suggest that GLP-1 analogs engage
signaling pathways in the islet beta-cell that lead to stimulation of beta-cell
replication and inhibition of beta-cell apoptosis. However, it remains to be proven
clinically whether GLP1 analogs may reverse the decline in beta-cell mass of the
pancreas that is characteristic of the natural history of type 2 diabetes.

Exenatide from Lilly is approved for use in patients with type 2 diabetes who
exhibit unaceptable glycemic control whil using meformin and/or sulfonylurea. GLP-1
analog therapy clinically has shown the advantage of reducing body weight, but is
associated with nausea and vomiting as the most common adverse effects which might
be reduced with optimized dosing regimens.

Apart from use of GLP-1 analogs in the treatment of diabetes, its usefulness
currently is being investigated in clinical studies of irritable bowel syndrome and
functional dyspepsia. Further studies explore the effects of natural GLP-1 and of
AC2592 from Amylin Pharmaceuticals administered by continuous infusion in patients
with congestive heart failure.


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information visit www.lamerie.com.



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Web Site = http://www.lamerie.com

Contact Details = Jorge Márquez
C/Casp 33 B 4º 2ª.
08010 Barcelona
Tel + 34 93 342 91 97
Fax + 93 342 91 98
eMail: jorge.marquez@lamerie.com
http://www.lamerie.com