Released on = January 23, 2006, 4:41 am

Press Release Author = La Merie Business Intelligence

Industry = Biotech

Press Release Summary = A plethora of SGLT inhibitors in the patent literature and
seven compounds in early clinical development indicate an abundance of interest in
the therapeutic use of SGLT inhibitors for the treatment of type 2 diabetes.

Press Release Body = A plethora of SGLT inhibitors in the patent literature and
seven compounds in early clinical development indicate an abundance of interest in
the therapeutic use of SGLT inhibitors for the treatment of type 2 diabetes. SGLT
inhibitors do not intervene with glucose metabolism, thus being complementary to
mainstream approaches to glucose regulation, i.e. PPAR agonists, DPP-IV antagonists
and GLP-1 analogues. While SGLT-2 inhibitors block the reabsorption of glucose from
the renal filtrate, SGLT1 inhibitors suppress absorption of glucose from the gut.
Most of the known SGLT inhibitors are selective for SGLT2, but there are also mixed
type inhibitors and SGLT1 inhibitors. Among the leading companies with clinical
stage SGLT inhibitors are Sanofi-Aventis (AVE2268), GlaxoSmithKline (869682) and
Bristol-Myers Squibb. These results were found in a search conducted by La Merie
Business Intelligence. The results were published in the January 23 issue of R&D
Pipeline News , edited by La Merie Business Intelligence.

SGLT2 is a molecular target to directly induce glucose excretion and to safely
normalise plasma glucose in the treatment of type 2 diabetes. Chemically, most of
the SGLT2 inhibitors are derived from the prototype phlorizin and structurally are
glycosides. Exceptions are the second generation antisense approach from ISIS
Pharmaceuticals and SGLT peptide antagonists from Theratech, both in preclinical
stages. Japanese companies have pioneered the SGLT inhibitor arena (Tanabe Seiyaku
with T-1095) and are still dominating the patent application field. SGLT2 inhibitors
are also promising for other therapeutic uses such as obesity as they cause the net
loss of calories from the body in form of glucose. In fact, GSK's lead compound
869682 is under clinical investigation in obesity.

So far, little is known about the therapeutic efficacy of SGLT inhibitors due to the
early development stage in the clinic. Theoretical safety concerns about increased
glucosuria by SGLT2 inhibtion do not appear to be relevant as patients with familial
renal glucosuria by an inherited defective form of SGLT2 have normal kidney
function, are not hypoglycemic and have no pathology caused by the transporter
defect.

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Contact Details = Jorge Márquez
La Merie S.L.
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Tel +34-93-342 91 97

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