Arena Pharmaceuticals has announced that it was issued US patent number 6,953,787, entitled "5-HT2C Receptor Modulators," by the United States Patent and Trademark Office.
The patent relates to novel compounds that modulate the 5-HT2C serotonin receptor, which helps regulate food intake and may also influence metabolic rate. These modulators could be useful in pharmaceutical compositions for the treatment of obesity. APD356, discovered by Arena, is a selective and orally available 5-HT2C receptor modulator covered by the patent. A 12-week, randomized, double-blind, dose-ranging Phase 2b clinical trial studying APD356 in obese patients is currently ongoing.
"This patent, along with a similar patent granted by the European Patent Office earlier this year, provides important protection for our lead drug candidate, APD356," commented Jack Lief, Arena's President and Chief Executive Officer. "We are looking forward to announcing top-line, longer term safety and efficacy data from our Phase 2b clinical trial of APD356 around the end of the year."
APD356 stimulates the 5-HT2C serotonin receptor, a G protein-coupled receptor located in the part of the brain called the hypothalamus, which helps regulate food intake and may also influence metabolic rate. 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 agents. In addition, APD356 has approximately 15-fold selectivity in vitro for the 5-HT2C receptor versus the 5-HT2A receptor, a central nervous system (CNS) receptor thought to be responsible for many of the CNS adverse effects of non-selective serotonergic agents. Arena believes that the selectivity of APD356 for the 5-HT2C receptor will 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.