Arena obtains European patent relating to 5-HT2A agonists, which have potential use in insomnia drugs

By E. Janene Geiss

Philadelphia, Dec. 29 - Arena Pharmaceuticals, Inc. said Thursday that it received a European patent relating to its class of inverse agonists to the 5-HT2A serontonin receptor, which is thought to be involved in regulating sleep and could be used in drugs that treat insomnia.

Arena said it was granted patent number 1558582, entitled "Diaryl and Arylheteroaryl Urea Derivatives as Modulators of the 5-HT2A Serotonin Receptor Useful for the Prophylaxis and Treatment of Disorders Related Thereto," by the European Patent Office, according to a company news release.

The patent relates to a class of inverse agonists to the 5-HT2A serotonin receptor, which is thought to be involved in the regulation of sleep architecture and sleep maintenance. These inverse agonists may be useful in pharmaceutical compositions for the treatment of insomnia, officials said.

APD125, discovered by Arena, is an orally available 5-HT2A receptor modulator covered under the patent. Arena said it intends to validate the patent in 31 European jurisdictions, including Germany, France, Italy, United Kingdom and Spain.

On June 30, Arena announced top-line results from its phase 1 clinical trial program, which indicated that APD125 was well-tolerated at all doses investigated and demonstrated a robust 60%, and statistically significant, increase in the amount of deep, or slow wave, sleep in volunteers with normal sleep/wake patterns, officials said.

An ongoing evaluation of the phase 1 APD125 data has provided additional statistically significant signals that indicate improved sleep maintenance, including statistically significant increases in stage 3 and stage 4 sleep, reductions in stage 1 sleep, reductions in the number of awakenings and an increase in delta power during slow wave sleep, officials said.

The company said the ongoing evaluation also continues to support the encouraging preliminary safety and tolerability profile of APD125.

Arena said it intends to begin dosing chronic insomniacs in a phase 2 clinical trial of APD125 in early 2006 under an Investigational New Drug Application being reviewed by the FDA. Arena said it expects results from that trial in mid-2006.

"APD125 represents a promising new approach to the treatment of insomnia and we look forward to the phase 2 results," Jack Lief, Arena's president and chief executive officer, said in the release.

"APD125, like our obesity drug candidate APD356, was discovered by Arena. Also like APD356, it is unpartnered and directed at a major pharmaceutical market opportunity," he added.

Arena is a San Diego clinical-stage biopharmaceutical company focusing on development and commercialization of small molecule drugs in four major therapeutic areas including metabolic, cardiovascular, inflammatory and central nervous system diseases.

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