Arena Pharmaceuticals Provides Update on GPR119 Portfolio for Type 2 Diabetes
The Phase 1 program evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of APD597, and included single and multi-ascending studies in healthy volunteers and in subjects with type 2 diabetes. APD597 was well tolerated and showed dose-proportional pharmacokinetics with a half-life of six to seven hours in solution and approximately 13 hours in suspension in healthy volunteers. The Phase 1 program also provided evidence for incretin stimulation (GLP-1, GIP and PYY) and reductions in post-meal glucose increases with APD597 treatment in both overweight and obese non-diabetic volunteers and in subjects with type 2 diabetes. In general, reductions in post-meal glucose increases were greater with APD597 in combination with sitagliptin, a DPP-4 inhibitor, compared to sitagliptin alone.
"Results of the Phase 1 program suggest that APD597 may have utility both alone and in combination with a DPP-4 inhibitor for the treatment of type 2 diabetes," said Jack Lief, Arena's President and Chief Executive Officer. "With our existing GPR119 patent portfolio, internally discovered next generation compounds and return of rights under the collaboration, including to APD597, we look forward to pursuing additional opportunities in this area."
Upon termination of the collaboration, all rights under licenses granted by Arena to Ortho-McNeil-Janssen under the agreement will terminate and revert to Arena, including rights relating to APD597. Ortho-McNeil-Janssen will also be required to deliver and assign to Arena rights and information relating to regulatory filings, including the Investigational New Drug Application (IND) relating to APD597, as well as certain other technology that may be useful to the development of GPR119 agonists that were subject to the collaboration. In addition, Ortho-McNeil-Janssen will cease reimbursing Arena for the cost of prosecuting Arena's GPR119 patent portfolio.
Arena owns a broad array of internally discovered, oral GPR119 agonists, including next generation compounds that Arena discovered after the research portion of its collaboration with Ortho-McNeil-Janssen ended in
Arena believes GPR119 represents a novel pharmaceutical mechanism for discovering oral small molecule agonists for the treatment of diabetes. GPR119 is expressed in beta cells, which are located in the pancreas and responsible for producing insulin in response to increases in blood glucose. Stimulation of GPR119 has been shown to promote insulin release by beta cells in response to elevated blood glucose levels. In addition, GPR119 is expressed in cells other than pancreatic beta cells, such as endocrine cells in the gastrointestinal tract. In preclinical studies and clinical trials, GPR119 has been shown to stimulate the release of GLP-1, GIP and PYY, incretins that play important roles in insulin regulation and metabolism.
A significant portion of type 2 diabetics fail oral medication and require injectable agents. Current oral medications for type 2 diabetes have a number of side effects, including hypoglycemia, weight gain, edema, and possibly an increase in cardiovascular mortality, prompting continued efforts to develop therapeutics to improve the treatment of diabetes.
Arena is a clinical-stage biopharmaceutical company focused on discovering, developing and commercializing oral drugs that target G protein-coupled receptors, an important class of validated drug targets, in four major therapeutic areas: cardiovascular, central nervous system, inflammatory and metabolic diseases. Arena's most advanced drug candidate, lorcaserin, is intended for weight management. Arena's wholly owned subsidiary,
Certain statements in this press release are forward-looking statements that involve a number of risks and uncertainties. Such forward-looking statements include statements about the termination of Arena's collaboration with Ortho-McNeil-Janssen and related expectations and future activities; the therapeutic indication and use, safety, efficacy, tolerability, mechanism of action and potential of APD597 alone and in combination; the potential of GPR119; Arena's GPR119 patent portfolio and program and potential opportunities; the potential therapeutic indication and use,
Contact: Arena Pharmaceuticals, Inc.
Media Contact: Russo Partners
David Schull, President
President and CEO
Manager, IR and Corporate Communications
Anthony J. Russo, Ph.D., CEO
858.453.7200, ext. 1479
News Provided by Acquire Media