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Arena Pharmaceuticals Expands GPR119 Patent Portfolio for Type 2 Diabetes

Thursday, March 10, 2011

San Diego, CA -- Arena Pharmaceuticals, Inc. (Nasdaq: ARNA) announced today that it was issued United States Reissue Patent No. RE42,190 with claims to methods of identifying compounds that modulate the activity of the GPR119 receptor. This invention stems from the discovery by Arena's scientists of the GPR119 receptor, a target for identifying small molecules for the treatment of diabetes.

"Targeting GPR119 with small molecules represents a promising new approach for the treatment of type 2 diabetes," statedDominic P. Behan, Ph.D., Arena's Senior Vice President and Chief Scientific Officer. "Our growing GPR119 patent portfolio covers technologies and tools that are useful in identifying orally active drug candidates. We are pursuing exclusive partnering opportunities for our internally discovered GPR119 agonists, including APD597 and next-generation compounds, and non-exclusive licensing opportunities for our portfolio of patents and patent applications related to the discovery and development of GPR119 receptor agonists."

Arena recently had additional GPR119 patent successes: United States Patent No. 7,893,235 issued with claims to isolated GPR119 nucleic acid sequences as well as vectors, plasmids and host cells containing those sequences; and United States Patent No. 7,816,492 issued with claims to isolated and recombinant GPR119 amino acid sequences. In addition, Arena holds patents on related GPR119 subject matter issued by patent offices of foreign jurisdictions, including the European Patent Office (EP 1133559, EP 1584683 and EP 1849866) as well as the patent offices of Canada, Australia, South Korea, Mexico, Hong Kong and New Zealand.

The technologies covered by Arena's patents and patent applications are related to the discovery and development of GPR119 receptor agonists, including materials and methods that may be used to identify and determine the activity of molecules that modulate the GPR119 receptor, methods that measure the incretin response to GPR119 agonists and pharmaceutical compositions containing both GPR119 agonists and DPP-4 inhibitors.

About GPR119

GPR119 is expressed in beta cells, which are located in the pancreas and responsible for secreting 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 agonists have stimulated the release of GLP-1, GIP and PYY, incretins that play important roles in insulin regulation and other metabolic pathways.

About APD597

APD597, Arena's internally discovered GPR119 agonist intended for the treatment of type 2 diabetes, was evaluated by Ortho-McNeil-Janssen Pharmaceuticals, Inc., under a former collaboration between Arena and Ortho-McNeil-Janssen, in a Phase 1 program that included single and multi-ascending dose studies in healthy volunteers and in subjects with type 2 diabetes. Arena believes APD597 may have utility alone and in combination with a DPP-4 inhibitor for the treatment of type 2 diabetes.

About Diabetes

According to the Centers for Disease Control and Prevention, diabetes affects approximately 26 million of the US population, and type 2 diabetes accounts for 90-95% of the diabetes prevalence. Type 2 diabetes is characterized by dysregulation of insulin sensitivity, insulin secretion and hepatic glucose production. Therapies for type 2 diabetes act by improving insulin release, enhancing insulin sensitivity, increasing insulin levels, modifying glucose absorption from the gut, or modifying hepatic glucose production. Current oral medications for type 2 diabetes may have side effects that include hypoglycemia, weight gain, edema or possible increases in cardiovascular mortality, prompting continuing efforts to develop therapeutics to improve the treatment of diabetes.

About Arena Pharmaceuticals

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 is lorcaserin, which is intended for weight management. Arena's wholly owned subsidiary, Arena Pharmaceuticals GmbH, has granted Eisai Inc. exclusive rights to market and distribute lorcaserin in the United States following FDA approval of the New Drug Application (NDA) for lorcaserin.

Arena Pharmaceuticals(R) and Arena(R) are registered service marks of the company.

Forward-Looking Statements

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 therapeutic indication and use, mechanism of action and potential of APD597 alone and in combination; the potential of GPR119, GPR119 agonists and related patent coverage; the potential value, growth and other aspects of Arena's GPR119 patent portfolio; potential partnering, licensing and other opportunities; potential therapeutic indication and use, FDA approval and commercialization of lorcaserin; the Eisai collaboration and potential activities thereunder; and Arena's focus, goals, strategy, research and development programs, and ability to develop compounds and commercialize drugs. For such statements, Arena claims the protection of the Private Securities Litigation Reform Act of 1995. Actual events or results may differ materially from Arena's expectations. Factors that could cause actual results to differ materially from the forward-looking statements include, but are not limited to, the following: Arena may not be successful in partnering GPR119 agonists or licensing its patents, patent applications and other technologies; the risk that APD597 or GPR119 agonists as a class may not realize their potential or ever receive marketing approval; there is no assurance that any of Arena's GPR119-related patent applications will issue, that any of Arena's patents will be enforceable or will cover a drug or other commercially significant technology or method, or that the patents will be held to be valid for their expected terms; Arena's activities in the GPR119 field, or those of its licensors or collaborators, could be impacted by conflicting positions that may exist between any overlapping chemical, receptor or pharmacology based information that are or have been generated by other organizations, companies or individuals and considered by them to be proprietary; the risk that regulatory authorities may not find data and other information related to Arena's clinical trials and other studies meet safety or efficacy requirements or are otherwise sufficient for regulatory approval; the timing of regulatory review and approval is uncertain; Arena's response to the complete response letter for the lorcaserin NDA may not be submitted when anticipated or the information provided in such response may not satisfy the FDA; the FDA may request other information prior to or after Arena resubmits the lorcaserin NDA or approval of the lorcaserin NDA; unexpected or unfavorable new data; risks related to commercializing new products; Arena's ability to obtain and defend its patents; the timing, success and cost of Arena's research and development programs; results of clinical trials and other studies are subject to different interpretations and may not be predictive of future results; clinical trials and other studies may not proceed at the time or in the manner Arena or others expect or at all; Arena's ability to obtain adequate funds; risks related to relying on collaborative agreements; the timing and receipt of payments and fees, if any, from collaborators; and satisfactory resolution of pending and any future litigation or other disagreements with others. Additional factors that could cause actual results to differ materially from those stated or implied by Arena's forward-looking statements are disclosed in Arena's filings with the Securities and Exchange Commission. These forward-looking statements represent Arena's judgment as of the time of this release. Arena disclaims any intent or obligation to update these forward-looking statements, other than as may be required under applicable law.

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