The right balance drives the field of PPAR agonist R&D

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 Related Report: PPAR Agonists

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 , 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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