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Arena Pharmaceuticals Issued Patent for 5-HT2C Receptor Modulators By European Patent Office

Posted on: Wednesday, 4 May 2005, 18:00 CDT

SAN DIEGO, May 4 /PRNewswire-FirstCall/ -- Arena Pharmaceuticals, Inc. announced today that it was granted patent number 03 718 323, entitled "5-HT2C Receptor Modulators," by the European Patent Office. The patent relates to novel compounds that modulate the 5-HT2C serotonin receptor, which is thought to be involved in the regulation of food intake and may be useful in pharmaceutical compositions for the treatment of obesity. APD356, discovered by Arena, is an orally available 5-HT2C receptor modulator covered under the patent. Arena expects to complete a randomized, double-blind, multiple dose Phase 2 clinical trial studying APD356 in obese patients this quarter. Arena intends to validate the patent in 31 European jurisdictions, including Germany, France, Italy, the United Kingdom and Spain, as well as Hong Kong.

"Developing a strong intellectual property estate is fundamental to a biotechnology company. This patent provides protection for our lead drug candidate, APD356, and is an important addition to our intellectual property estate," commented Jack Lief, Arena's President and Chief Executive Officer.

APD356 stimulates the 5-HT2C serotonin receptor, a G protein-coupled receptor located in the part of the brain called the hypothalamus and thought to be involved in the regulation of food intake. APD356 has approximately 100-fold selectivity in vitro for the 5-HT2C receptor relative to the 5-HT2B receptor. Arena believes the 5-HT2B receptor is primarily implicated in the cardiac valvulopathy observed with non-selective serotonergic drugs. In addition, APD356 has approximately 15-fold selectivity in vitro for the 5-HT2C receptor versus the 5-HT2A receptor, the central nervous system (CNS) receptor thought to be primarily responsible for most of the CNS adverse effects of non-selective serotonergic agents. Arena believes that the selectivity of APD356 for the 5-HT2C receptor may allow the compound to be dosed at a well-tolerated level that will induce clinically relevant weight loss without the side effects observed with non-selective serotonergic agents.

About Obesity

Obesity and a related condition known as metabolic syndrome affect tens of millions of adults and children in the U.S. and pose a serious long-term threat to their health and welfare. The number of overweight and obese people has substantially increased over the past few decades. Approximately two-thirds of all adults in the U.S. are obese or overweight and 16% of children and adolescents ages 6 to 19 in the U.S. are overweight. Medical and related costs of obesity in the U.S. were more than $117 billion in 2000. Being obese or overweight is associated with a number of conditions, including heart disease, stroke, diabetes, cancer and osteoarthritis. Medical treatment options for obesity and metabolic syndrome are currently limited.

About Arena Pharmaceuticals

Arena is a clinical-stage biopharmaceutical company focusing on the discovery, development and commercialization of small molecule drugs in four major therapeutic areas: metabolic, cardiovascular, inflammatory and central nervous system diseases. Arena is developing a broad pipeline of compounds that act on an important class of drug targets called G protein-coupled receptors, or GPCRs, using its proprietary technologies, including CART(TM) (Constitutively Activated Receptor Technology) and Melanophore. Arena's most advanced clinical compound, APD356, a selective 5-HT2C serotonin receptor agonist for the treatment of obesity, is in a Phase 2 clinical trial. Arena is also conducting Phase 1 clinical trials on APD125, a compound with a novel mechanism of action (a selective 5-HT2A receptor antagonist) for the treatment of insomnia. Arena has active collaborations with two major pharmaceutical companies, Ortho-McNeil Pharmaceutical Inc., a Johnson & Johnson company, for the treatment of type 2 diabetes, and Merck & Co., Inc., for the treatment of atherosclerosis and related disorders.

Arena Pharmaceuticals(R) and Arena(R) are registered service marks of the company. CART(TM) is an unregistered service mark 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 APD356's safety profile, potency and pharmaceutical behavior, Arena's intention to validate the European patent covering APD356, the significance of, and the protection provided by, such patent, and the expected timing of Arena's clinical trial studying APD356 and other statements about Arena's strategy, technologies, preclinical and clinical programs, and ability to develop compounds. 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 timing, success and cost of Arena's research, out-licensing endeavors and clinical studies, Arena's ability to obtain additional financing, Arena's ability to obtain and defend its patents, Arena's patent protection, and the timing and receipt of payments and fees, if any, from Arena's collaborators, including Ortho-McNeil and Merck. 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.

Contacts: Jack Lief

President and CEO

David Walsey

Director, Corporate Communications

Arena Pharmaceuticals

(858) 453-7200

Susan Neath

Atkins + Associates

Media & Investor Relations

(858) 527-3486

http://www.arenapharm.com/

Arena Pharmaceuticals, Inc.

CONTACT: Jack Lief, President and CEO, or David Walsey, Director,Corporate Communications, both of Arena Pharmaceuticals, +1-858-453-7200; orSusan Neath, Media & Investor Relations of Atkins + Associates,+1-858-527-3486

Web site: http://www.arenapharm.com/

Source: PRNewswire-FirstCall

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