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Post# of 252232
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Re: biotech jim post# 144801

Friday, 06/29/2012 4:02:01 PM

Friday, June 29, 2012 4:02:01 PM

Post# of 252232
GPR119 receptor agonist in T2DM

Looks like efficacy issues also with the GSK compound, as presented in a poster at ADA last year:

Following single doses of GSK1292263, there was a dose-dependent decrease in glucose AUC (0-3h) during the OGTT. After 14 days, GSK1292263 did not reduce AUCglucose (0-24h) when administered alone or when co-dosed with metformin or sitagliptin. There was an increase in circulating gut hormone levels during the prandial periods, especially for PYY. Combination with sitagliptin resulted in increased plasma active GLP-1 concentrations, but lower total GLP-1, GIP and PYY concentrations. Sitagliptin alone reduced AUCglucose (0-24h). This suggests that GPR119 agonism does not provide clinically meaningful glycemic improvement in T2DM patients, and efficacy is not increased when co-dosed with metformin or sitagliptin.

http://diabetes.diabetesjournals.org/content/60/Supplement_1/A235.full.pdf

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