Released on = January 11, 2007, 6:34 am

Press Release Author = La Merie Business Intelligence

Industry = Biotech

Press Release Summary = A strongly growing market of now more than US$ 6 bln in 2006
for only tow PPAR gamma agonists founds the basis for a heavily researched field of
next generation mono, dual or triple PPAR agonists with fine-tuned subtype
combinations

Press Release Body = BARCELONA, Spain | Jan 11, 2007 | The commercial success of the
two peroxisome proliferator-activated receptor (PPAR) gamma agonists pioglitazone
and rosiglitazone from Takeda & Lilly and GlaxoSmithKline approved for treatment of
type 2 diabetes with 2005 global sales of more than US$ 5 bln fuels the R&D of next
generation PPAR agonists. Safety concerns and regulatory impediments caused Big
Pharma companies to discontinue their first generation, close to market dual PPAR
alpha and gamma agonists. The next generation fine-tuned dual PPAR alpha/gamma
agonists prefer agonists with full alpha and partial gamma activity with
Sanofi-Aventis and AstraZeneca as protagonists. Research is shifting into the field
of novel PPAR delta agonists and combinations of PPAR delta with PPAR gamma (dual)
or with PPAR gamma and delta (Pan PPAR agonists). GSK leads this field which has
already ten projects in clinical development. These results were found in a
Competitor Analysis conducted by La Merie Business Intelligence. The report can be
found at www.pipelinereview.com , La Merie's News Center and Online Store.

Sales of the two approved PPAR gamma agonists in 2006 are further growing at double
digit rates stimulated by the growing number of patients and by label extensions and
fixed dose combinations with metformin and glimepiride. The use of insulin
sensitizing, first generation PPAR gamma agonists is associated with an increased
incidence of edema and weight gain. Clinical data with improved modulators of PPAR
gamma from Metabolex indicate that this side effect can be avoided. At least six
clinical programs with next generation PPAR gamma modulators are on the way followed
by new non-TZD partial PPAAR gamma ligands with preferential recruitment of PPAR
gamma co-activator.

Major pharma companies BMS & Merck, AstraZeneca, Takeda, Eisai and Eli Lilly
discontinued their first generation dual PPAR alpha and gamma agonist projects for
the treatment of type 2 diabetics with dyslipidemia due to regulatory requests of
long term preclinical and clinical safety data. The next generation of dual PPAR
alpha/gamma agonists shows a fine-tuned agonist profile with preference on PPAR
alpha and little PPAR gamma activity. At least eight clinical programs are running
in this field. The impact of FDA's requests on the pipeline of PPAR alpha agonists
with fenofibrate-like actions on triglycerides and HDL cholesterol is not evident as
there are at least nine clinical stage projects ongoing.

GlaxoSmithKline leads the field of companies with interest in PPAR delta agonism
which affects cholesterol transport. PPAR delta mono-agonists as well as triple PPAR
alpha, delta and gamma agonists are in clinical development with at least ten
clinical stage development projects.


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SOURCE: La Merie Business Intelligence


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