GENAERA PRESENTS DATA ON OBESITY DRUG CANDIDATE

Genaera has presented preclinical data supporting the mechanism of action of trodusquemine, the company's centrally acting small-molecule appetite suppressant, at the Keystone Symposia Obesity Meeting.

The presentation described a multifactorial mechanism of action through which trodusquemine suppresses appetite, induces loss of body weight and normalizes blood glucose and blood cholesterol levels. This includes the selective inhibition of protein tyrosine phosphatase 1B (PTP1B), the inhibition of neurotransmitter reuptake transporters (dopamine and norepinephrine) and the downregulation of orexigenic hormone expression (AgRP and NPY) to decrease appetite and induce fat loss.

"These data confirm that trodusquemine is active against several critical molecular targets involved in the regulation of appetite, body weight and insulin sensitivity that may give it broad utility in treating obesity and related conditions," Jack Armstrong, president and CEO of Genaera, said. "We expect to begin exploring the potential of trodusquemine in humans with a Phase I clinical trial in the first half of 2007."

Genaera has conducted studies in a number of mouse models of obesity (including diet-induced obese mice, agouti mice, and leptin-deficient and leptin-receptor-deficient mouse strains). This preclinical activity of trodusquemine reduces food intake by appetite suppression and is reversible. The ability of trodusquemine to induce weight loss without associated toxicities in several animal models (rodent, rabbit, dog and monkey) supports selection of this compound as a candidate for evaluation in clinical studies.