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Kosan's Motilin Receptor Agonist, Licensed to Pfizer, Enters Phase 1 Clinical Trial in Gastroesophageal Reflux Disease
Date:8/19/2007

motilin receptor found on smooth muscle cells of the GI tract and elements of the enteric nervous system. The clinical observation that the macrolide antibiotic erythromycin, a motilin receptor agonist, accelerates gastric emptying in patients with diabetic gastroparesis (impaired gastric emptying) has resulted in efforts to develop non-antibiotic macrolides (motilides) as prokinetic agents. PF-04548043 is a potent, selective motilin receptor agonist that is chemically stable and orally bioavailable and lacks antibiotic activity. In preclinical studies, PF-04548043 showed an improved safety profile relative to erythromycin and accelerated gastric emptying, suggesting that it may provide symptom relief in several GI diseases.

About GERD

Although the pathophysiology underlying GERD is not fully understood, it is clear that GERD is not due to acid hyper-secretion, but rather, is due to a combination of disordered upper GI tract motility, resulting in increased ingress of gastric contents into the lower esophagus, together with impairments in esophageal clearance and protection mechanisms. Increased exposure to gastric contents, coupled with reduced ability to clear the bolus, appears to precipitate reflux symptoms. Despite adequate control of intra-gastric acidity with proton pump inhibitors, a proportion of GERD patients continues to have residual symptoms. Through improvement of GI motility and increases in the rate of gastric emptying, PF-04548043 has the potential to reduce the exposure of the esophagus to acidic and weakly acidic reflux and this may improve the symptoms of GERD.

About Kosan

Kosan Biosciences is a biotechnology company advancing two new classes of anticancer agents through clinical development -- Hsp90 (heat shock protein 90) inhibitors and epothilones. Kosan is leveraging its proprietary discovery platform to generate a pipeline of potentially significant product candidates, primarily in the area of oncology.

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SOURCE Kosan Biosciences Incorporated

Copyright©2007 PR Newswire.

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