"Advancing APD791 into Phase 1 expands our emerging clinical pipeline of novel therapeutics and further validates our research and development capabilities," said Jack Lief, Arena's President and Chief Executive Officer. "Like Arena's other proprietary and internally discovered drug candidates being clinically evaluated, lorcaserin for obesity and APD125 for insomnia, APD791 may provide significant advantages over current therapies. We anticipate announcing data from this program around the end of this year."
This Phase 1 trial is a randomized, placebo-controlled, double-blind, single-ascending dose trial in healthy male and female volunteers between the ages of 19 and 45 years old. The trial will include up to eight cohorts of nine volunteers each. In each cohort, three volunteers will be assigned to receive placebo and six volunteers will be assigned to receive APD791 in an ascending dose fashion. In addition to evaluating APD791's safety and tolerability profile, the trial will also evaluate the pharmacokinetics and pharmacodynamics of single oral doses of APD791. Pharmacodynamics will be evaluated by measuring ex vivo inhibition of platelet aggregation.
A second Phase 1 trial is planned to start after the first trial is completed. The second trial is primarily intended to evaluate the safety and tolerability of multiple ascending doses of APD791. It will also evaluate the pharmacokinetics and pharmacodynamics of multiple oral doses of APD791.
About APD791
APD791 is a novel, orally available and selective inverse agonist, or inhibitor, of the 5-HT2A serotonin receptor. Serotonin activation of the 5- HT2A receptor on platelets and vascular smooth muscle is thought to play an important role in the events leading to thrombosis, and elevated serotonin levels have been associated with increased cardiovascular risk. Normally, when a platelet is activated by one of a number of factors, such as thrombin or collagen, the platelet releases serotonin, which in preclinical studies promotes platelet aggregation, vasoconstriction and intimal hyperplasia (or thickening of the vessel wall). By blocking activation of the 5-HT2A receptor on platelets and other cardiovascular tissues, APD791 may curb these serotonin mediated effects in the clinical setting, thereby reducing the risk of thrombosis. APD791 demonstrated improved coronary artery flow in a preclinical study using the Folts model, an established model of acute coronary syndrome.
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About Thrombosis
Thrombosis is the formation of a clot, or thrombus, inside a blood vessel that restricts the flow of blood. The formation of a thrombus is often caused by an injury to the wall of a blood vessel. The injury to the blood vessel activates platelets, which then aggregate and adhere to one another as they start to release certain factors, including serotonin, that facilitate thrombosis. Thrombi that form in diseased atherosclerotic arteries of the heart may cause acute coronary syndrome or myocardial infarction, and thrombi that form in the vessels of the brain may cause stroke.
The American Heart Association estimates that in the United States over 13.6 million people alive in 2004 had survived either a myocardial infarction or a stroke. To reduce the risk of future events, many patients receive daily anti-thrombotic therapy.
About Arena Pharmaceuticals
Arena is a clinical-stage biopharmaceutical company focused on discovering, developing and commercializing oral drugs in four major therapeutic areas: cardiovascular, central nervous system, inflammatory and metabolic diseases. Arena's most advanced product candidate, lorcaserin, is being investigated in a Phase 3 clinical trial program for the treatment of obesity. Arena's broad pipeline of novel compounds targeting G protein-coupled receptors, an important class of validated drug targets, includes compounds being evaluated independently and with its partners, Merck & Co., Inc. and Ortho-McNeil Pharmaceutical, Inc.
Arena Pharmaceuticals(R) and Arena(R) are registered service marks of the company. "APD" is an abbreviation for Arena Pharmaceuticals Development.
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 timing, protocol, design, scope and other aspects of the Phase 1 clinical trials of APD791, the potential safety, efficacy and tolerability of APD791, the role of serotonin in thrombosis and in increasing cardiovascular risk, Arena's pipeline of compounds, and other statements about Arena's strategy, preclinical and internal and partnered clinical 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, Arena's planned clinical trials may not proceed at the time Arena expects or at all, the results of preclinical studies or clinical trials may not be predictive of future results, Arena's ability to partner lorcaserin, APD125, APD791 or other of its compounds or programs, the timing, success and cost of Arena's research, out-licensing endeavors and clinical trials, Arena's ability to obtain additional financing, Arena's ability to obtain and defend its patents, and the timing and receipt of payments and fees, if any, from Arena's collaborators. 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.
Arena Pharmaceuticals, Inc.
http://www.arenapharm.com |
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