HAYWARD, Calif., Dec. 18 /PRNewswire/ -- Arete Therapeutics Inc. today announced positive top line Phase I results for AR9281, an orally-administered soluble epoxide hydrolase (s-EH) inhibitor for the treatment of metabolic syndrome. The results of the multi-dose study demonstrate that AR9281 was safe and well tolerated in healthy volunteers.
"We are extremely pleased with the results of this trial, which show that AR9281, a first-in-class s-EH inhibitor, produces a dose-dependent inhibition of blood s-EH activity, and is safe and well-tolerated in healthy volunteers," said James Sabry, M.D., Ph.D., President and Chief Executive Officer of Arete Therapeutics. "In the first quarter of 2009, we will initiate a Phase IIa clinical trial with AR9281, a compound we believe has the potential to become a new alternative for patients with metabolic syndrome."
The Phase I single-center, multiple ascending dose study tested the safety, tolerance and pharmacodynamics of AR9281 in 24 healthy male and female volunteers. Participants were enrolled in three cohorts, evaluating doses up to 1200 mg/day of AR9281 for seven consecutive days. All doses of the drug were well tolerated and no dose-related adverse events were observed. As part of the pharmacodynamic assessment, levels of s-EH activity were measured after day one of the trial and confirmed 100% inhibition of the target in all subjects receiving 1200 mg of AR9281.
Randy Whitcomb, M.D., Chief Medical Officer of Arete commented, "We are particularly pleased that the diagnostic biomarker used in the trial confirmed that AR9281 fully inhibits s-EH enzyme production in humans safely, suggesting that we can now explore the effects of this level of inhibition on glucose metabolism in our planned Phase IIa clinical trial."
AR9281 is a first-in-class, orally-administered compound which inhibits s-EH. Operating within the third branch of the arachidonic acid pathway, s-EH is critical to the metabolism of this important signaling molecule. As such, it is thought to play a role in diseases such as metabolic syndrome, hypertension and several inflammatory disorders. AR9281 has shown activity in multiple animal models of diabetes, hypertension and inflammation. In addition, AR9281 has been evaluated in various published and proprietary in vitro and in vivo assays for potency, selectivity, efficacy, ADME, toxicity and safety, with very favorable results.
About Arete Therapeutics Inc.
Arete Therapeutics is a privately-held biotechnology company dedicated to the discovery and development of novel drugs to treat metabolic, inflammatory and cardiovascular disease. It is the world's leading company focused on s-EH, an important enzyme for the metabolism of arachidonic acid that plays an essential role in metabolic, inflammatory and cardiovascular physiology. The Company was founded by Dr. Bruce Hammock, a Professor at the University of California, Davis, who discovered s-EH. The company has raised a total of over $51 million in Series A financing led by Frazier Healthcare Ventures, Alta Partners, Three Arch Partners, Burrill & Company and Altitude Life Science Ventures. For more information on Arete Therapeutics, please visit http://www.aretetherapeutics.com.