EPIX BEGINS TRIAL OF PRX-07034 IN OBESITY

Epix Pharmaceuticals has announced the initiation of a Phase I multiple-ascending-dose clinical trial to study the safety, tolerability, pharmacokinetics and pharmacodynamics of PRX-07034 administered once-daily for 28 days in a population of otherwise healthy obese adults with body mass indices between 30 and 42 kg/m2. PRX-07034 is a novel, highly selective 5-HT6 receptor antagonist being developed for the treatment of obesity, as well as for cognitive impairment associated with Alzheimer's disease and schizophrenia.

PRX-07034 is a novel, highly selective, small-molecule antagonist of a specific G-protein coupled receptor known as 5-HT6. Preliminary safety and tolerability data from a recently completed single-ascending-dose Phase I trial in healthy adult male and female volunteers indicated that single doses of PRX-07034 were well-tolerated up to 2,500 mg, the highest dose tested. In addition, PRX-07034 demonstrated adequate absorption, with drug exposures increasing with increasing doses and a half-life of 14 to 24 hours, making it suitable for once-daily dosing.

The drug has been shown to have cognitive-enhancing properties in preclinical animal models of memory impairment, as well as reducing both food intake and body weight in several preclinical animal models of obesity. Indications are that the human 5-HT6 receptor is found mainly in the central nervous system with little or no expression in peripheral tissues, which may result in greater drug selectivity with fewer side effects.