Genaera Corp. announced May 7th that it has begun enrolling patients in a Phase 1 clinical trial of the obesity and diabetes drug trodusquemine (MSI-1436).

Trodusquemine is a centrally and peripherally-acting appetite suppressant and a highly selective inhibitor of protein tyrosine phosphatase 1B (PTP1B), an enzyme target for the treatment of diabetes and obesity.

Another compound, ertiprotafib, was developed by Wyeth several years ago to selectively inhibit PTP1B, but was abandoned after Phase II trials found it was not very effective and also gave rise to concerns about side-effects.

Genaera said trodusquermine produced consistent, sustainable weight loss in a variety of animal models and appeared to overcome metabolic readjustment, which often limits sustained weight loss during caloric restriction.

“We are pleased that FDA has given Genaera the green light to begin testing trodusquemine in humans and that we were able to efficiently execute our clinical program and proceed into the clinic,” said Jack Armstrong, President and Chief Executive Officer of Genaera.

“While the primary endpoint of this first phase 1 study is safety and tolerability, we will be looking for evidence supporting our pre-clinical observations that trodusquemine induces appetite suppression and weight loss while normalizing glucose metabolism and insulin sensitivity.”