Dosing convenience is mandatory to keep pace in the pipeline race of GLP-1 analogs for type 2 diabetes

BARCELONA, Spain | The Business Intelligence firm La Merie S.L. reported today that major diabetes companies are trying to keep pace with Eli Lilly and Amylin Pharmaceutical in the field of GLP-1 analogs to treat type 2 diabetes. Lilly’s and Amylin’s first-in-class, but twice-daily product exenatide posted 2006 sales of US$ 430.2 mln in the first full market year and gained FDA approval for expanded combination use. A once-daily GLP-1 analog as the closest follow-up product from competitor Novo Nordisk may not be sufficiently convenient as Lilly and at least four others are developing once-a-week products in clinical trials. Pfizer’s recent acquisition of Biorexis with its long-acting GLP-1 fusion protein further spurs the race in the second generation GLP-1 analog field. Nasal spray and oral formulations of GLP-1 analogs as a non-invasive alternative to injections may be a third generation follow-up approach. 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

Both enzymatic cleavage and renal clearance contribute to a very short circulating half-life of several minutes for native GLP-1 which is a 30-amino acid gut peptide produced in enteroendocrine cells located in the distal ileum and colon. Thus, GLP-1 analogs have been constructed with resistance to enzymatic cleavage. These GLP-1 mimetics bind to GLP-1 receptors with similar affinity and produce biological actions identical to those of native GLP-1 which controls blood glucose via multiple actions including stimulation of insulin secretion and inhibition of both glucagon secretion and gastric emptying. Preclinical data suggest that GLP-1 analogs engage signaling pathways in the islet beta-cell that lead to stimulation of beta-cell replication and inhibition of beta-cell apoptosis. However, it remains to be proven clinically whether GLP1 analogs may reverse the decline in beta-cell mass of the pancreas that is characteristic of the natural history of type 2 diabetes.

Exenatide from Lilly is approved for use in patients with type 2 diabetes who exhibit unaceptable glycemic control while using meformin and/or sulfonylurea. The label of exenatide recently has been extended by FDA approval as an add-on therapy to improve glucose control in type 2 diabetes patients with inadequate control on a thiazolidinedione. GLP-1 analog therapy clinically has shown the advantage of reducing body weight, but is associated with nausea and vomiting as the most common adverse effects which might be reduced with optimized dosing regimens.

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SOURCE: La Merie Business Intelligence