Arena initiates anti-obesity drug trials

Arena Pharmaceuticals, from San Diego, US, has initiated a Phase I clinical trial in the UK for APD356, its lead anti-obesity compound. This double-blind, placebo-controlled, single-dose, dose-escalation trial is planned to enroll 54 healthy, overweight volunteers. The study will evaluate the safety, tolerability and pharmacokinetic profile of APD356.

The single-dose protocol should be completed in the first half of this year and, if the results support further testing, Arena expects to begin a larger, multi-dose trial later this year to study the safety of multiple doses of APD356 and to examine weight loss in a double-blind, placebo-controlled trial in healthy, overweight volunteers. If the Phase I clinical trial is successful, the company anticipates launching a Phase II clinical trial in overweight and obese patients in 2005.

'I'm pleased to report that we began the first human testing of one of our internally developed drug candidates and I look forward to updating you on the progress of the clinical trial for this compound by mid-year,' stated Jack Lief, Arena's president and chief executive officer. 'This is an important milestone for us because it shows that we are making significant progress in leveraging our proprietary technologies and in-depth knowledge of G protein-coupled receptors to fuel our development pipeline. It also meets our announced goal to advance a product candidate into the clinic this year.'

Obesity and metabolic syndrome

Obesity and metabolic syndrome are afflictions that affect tens of millions of adults and children and pose a serious long-term threat to their health and welfare. APD356 is an orally-administered small molecule that is a selective 5HT2C serotonin receptor agonist. The 5HT2C receptor is located in an area of the brain known to be critical for regulating metabolism and food intake. APD356 reduced body weight and food intake in animal models of obesity, which, Arena believes, is due to the compound's ability to regulate satiety. Arena's in vivo experiments showed that APD356 selectively reduced fat mass in obese animals, while leaving lean body mass unchanged, a very desirable outcome. Further, these same animals evidenced a statistically significant decrease in total cholesterol, while their HDL, the so-called 'good' cholesterol, increased.