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Sep 27, 2006

Ortho-McNeil Extends GDIR Agreement with Arena Pharmaceuticals

  • Ortho-McNeil Pharmaceutical its research agreement with Arena Pharmaceuticals by one year. This is compliant with provisions of the partnership between the two companies to develop compounds targeting the glucose-dependent insulinotropic receptor (GDIR).

    By extending the research term, Ortho-McNeil is committed to provide research funding to Arena worth $2.4 million.

    Arena discovered the GDIR receptor, which has the potential to stimulate insulin production in response to increases in blood glucose. The GDIR is an orphan G protein-coupled receptor expressed in beta cells.

    APD668 is a GDIR agonist intended to more efficiently stimulate insulin release by beta cells in response to elevated blood glucose levels and to avoid hypoglycemia. Unlike the GLP-1 receptor, the GDIR is amenable to small molecule, orally active drug development. Arena says it has discovered potent, selective, and orally available small molecule agonists of the GDIR that improve glucose tolerance and lower blood glucose levels in preclinical models of diabetes.

    In preclinical studies, GDIR agonists only lowered blood glucose when it rose above normal levels, such as after a meal. Therefore, unlike the glucose-insensitive sulfonylureas, Arena’s GDIR agonists are not expected to lower normal fasting blood glucose levels or cause hypoglycemia. In addition, GDIR stimulation has been found to increase the levels and activity of intracellular factors thought to be involved in the preservation of beta cells.


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