SAN DIEGO, March 5 /PRNewswire-FirstCall/ -- Arena Pharmaceuticals, Inc. today announced that it initiated dosing in a Phase 2 clinical trial of APD125 in chronic insomnia patients. APD125 is an orally available drug candidate discovered by Arena with the potential to reduce insomnia symptoms and improve sleep maintenance and quality. The Phase 2 trial of APD125 is a randomized, double-blinded, placebo-controlled study evaluating the safety and efficacy of nighttime dosing in patients with chronic insomnia. This trial will evaluate standard measurements of sleep, such as wake after sleep onset (WASO), number of awakenings, total sleep time and latency to persistent sleep, and will enroll a total of approximately 100 male and female patients in about 25 clinical sites in the United States. This trial employs a cross-over design, meaning that every patient receives both active doses of APD125 (10 mg and 40 mg) and placebo in random order, for one week, separated by at least one week to allow for wash out of the study drug.
"Moving APD125 into a Phase 2 trial in patients with chronic insomnia is an opportunity to build upon the favorable Phase 1 clinical data demonstrating that APD125 has the potential to improve sleep maintenance and quality with an excellent tolerability profile," said Jack Lief, Arena's President and Chief Executive Officer. "We continue to advance our pipeline of novel, Arena discovered, orally available compounds: lorcaserin is in an ongoing Phase 3 trial for the treatment of obesity, APD125 is now in a Phase 2 trial for insomnia, and we expect soon to initiate a Phase 1 trial of APD791, our lead anti-thrombotic drug candidate. We also continue to work on our partnered diabetes program with Ortho-McNeil and our partnered cardiovascular disease program with Merck."
At the 20th Anniversary Meeting of the Associated Professional Sleep Societies in June 2006, Arena presented favorable results from Phase 1 clinical trials of APD125, which were designed to evaluate the single and multiple dose safety and pharmacokinetics, and single dose pharmacodynamics, of APD125 in normal volunteers. In the Phase 1 program, APD125 was very well tolerated at all doses investigated. APD125 also improved measurements associated with sleep maintenance, including statistically significant increases in the minutes of slow wave, or deep, sleep (p<0.0001 for treatment effect). The increases in slow wave sleep were not associated with changes in the percentage of time in REM sleep. Additional improvements included statistically significant decreases in the number of shifts between different stages of sleep (p<0.0001) and the number of awakenings during sleep (p<0.0001). Statistically significant decreases in the number of sleep bouts were also found (p<0.0001) and there was a trend towards a decrease in WASO at all three doses in these volunteers with normal sleep patterns. Fewer sleep stage shifts and fewer sleep bouts are additional factors that may be associated with improved sleep maintenance, reflecting fewer sleep cycle interruptions. APD125 was not associated with any limiting next-day cognitive or motor impairments.
About APD125
Discovered by Arena, APD125 is a novel and orally available, highly selective inverse agonist of the 5-HT2A serotonin receptor. The vast majority of approved drugs for insomnia activate the GABA-A receptor in the brain, triggering a general CNS-suppressive effect. These drugs are DEA-scheduled, controlled substances due to their potential for abuse. Common side effects of GABA activating drugs include the risk of developing tolerance to the drug, impaired functioning when the drug is at therapeutic levels, and the potential for causing a sensation of dullness and lethargy upon awakening, often referred to as the "hangover effect."
By selectively targeting the 5-HT2A receptor, APD125 acts through a different mechanism than currently marketed insomnia drugs and inhibits one of several CNS activating pathways. Because of the different mechanism of action, APD125 may not have the side effects or abuse potential generally associated with currently marketed GABA-A drugs. APD125 has the potential to reduce insomnia symptoms and improve sleep maintenance by decreasing the number of awakenings and the amount of wake time after initial sleep onset, and by increasing total sleep time.
About Insomnia
Insomnia is characterized by inadequate or poor sleep due to nonrefreshing sleep, frequent wakening with difficulty falling back to sleep, difficulty falling asleep or waking too early. Most insomnia complaints relate to sleep maintenance issues, such as waking frequently or awakening too early, as opposed to problems with sleep latency (i.e. falling asleep). About 30 to 40 percent of U.S. adults complain about some level of insomnia in the course of a year, and about 10 to 15 percent of U.S. adults indicate that their condition is severe or chronic. In these cases, the lack of restful sleep impairs the person's ability to carry out their daily responsibilities because they are too tired or have trouble concentrating.
Insomnia has a variety of causes. It is often a symptom of some other disease or condition (e.g. life stress, psychiatric and medical disorders, or use of certain medications), but it can also be a distinct disorder. The prevalence of insomnia increases with age and is more common in women. Common symptoms of acute insomnia are sleepiness, negative mood and impairment of performance. Chronic insomnia is often associated with fatigue, mood changes, difficulty concentrating and impaired daytime functioning.
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 2 clinical trial of APD125, the timing of a Phase 1 clinical trial of APD791, the tolerability, side effects, efficacy and potential of Arena's product candidates and compounds, the advancement and content of Arena's pipeline, Arena's collaborations with Ortho-McNeil and Merck, including expected activities thereunder, 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.
Contacts: Jack Lief E. Blair Schoeb President and CEO WeissComm Partners Media Relations David Walsey 760.365.1857 Director, Corporate Communications Arena Pharmaceuticals, Inc. 858.453.7200, ext. 1682 http://www.arenapharm.com
Arena Pharmaceuticals, Inc.CONTACT: Jack Lief, President and CEO, or, David Walsey, Director,Director, Corporate Communications, both of Arena Pharmaceuticals, Inc.,+1-858-453-7200 ext. 1682; or E. Blair Schoeb, Media Relations, WeissCommPartners, +1-760-365-1857
Web site: http://www.arenapharm.com/
