Arena Pharmaceuticals Granted Patent for Drug Screening Methods Related to Ortho McNeil, Inc. Collaboration
Arena Pharmaceuticals, Inc. announced that it was granted patent number 1133559, entitled "HUMAN ORPHAN G PROTEIN-COUPLED RECEPTOR RUP3," by the European Patent Office. The patent relates to certain drug screening methods utilizing the 19AJ receptor, an orphan G protein-coupled receptor, or GPCR, which was discovered by Arena and is active in regulating blood glucose levels in a glucose-dependent manner. The invention set forth in the patent was utilized to identify the orally bioavailable compounds that Ortho-McNeil, Inc., a Johnson & Johnson company, and Arena are developing to treat diabetes as part of the collaboration they initiated in December 2004.
"This patent highlights the value of Arena's approach to the discovery and development of potential drugs that target orphan GPCRs, where the natural ligand is unknown," commented Jack Lief, Arena's President and Chief Executive Officer. "In partnership with Ortho-McNeil, Inc., the 19AJ program is making good progress towards its goal of developing an orally bioavailable drug that can effectively regulate blood glucose levels in a glucose-dependent manner, avoiding the potential for hypoglycemia."
19AJ is an orphan GPCR preferentially expressed in beta cells, the cells in the pancreas responsible for producing insulin in response to increases in blood glucose. Preclinical results indicate that stimulating the 19AJ receptor allows beta cells to produce insulin more efficiently in response to changes in blood glucose levels. In addition, stimulation of the 19AJ receptor has been found to increase levels and activity of intracellular factors thought to be involved in the preservation of beta cells.
Unlike the GLP-1 receptor, another beta-cell receptor responsible for secreting insulin in a glucose-dependent manner, the 19AJ receptor is amenable to small molecule, orally bioavailable drug development. Arena has discovered potent, selective and orally available small molecule agonists of the 19AJ receptor that improve glucose tolerance and lower blood glucose levels in animal models of diabetes. The 19AJ mechanism is glucose dependent: in animal studies, 19AJ agonists only lowered blood glucose when it rose above normal levels, such as after a meal. Therefore, unlike the glucose-insensitive sulphonylureas, 19AJ agonists neither lowered normal fasting blood glucose nor caused hypoglycemia.
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