Synergy Pharmaceuticals, Inc. a developer of new drugs to treat gastrointestinal (GI) disorders and diseases, announced that it has successfully completed preclinical in vitro research demonstrating the inhibition of bile acid uptake by GC-C agonists and that it plans to commence animal studies shortly. Synergy believes this is the first time that GC-C agonists have been shown to potentially lower cholesterol.

Synergy has filed a patent application covering the use of proprietary GC-C agonists as drug candidates for prevention and treatment of cholesterol lowering, heart stroke, atherosclerois, diabetes type II, coronary heart disease, gallstones, hypertension, obesity and other cardiovascular diseases. In addition, GC-C agonists may also be used in combination with statins to produce synergistic effect to reduce the dose of statins such as Lipitor, Zocor and Crestor to lower cholesterol.

“We are pleased to announce expansion of our GC-C agonist technology to lower cholesterol and are planning to develop a drug candidate for this indication,” said Dr Gary S Jacob, CEO of Synergy.

“We believe that the use of GC-C agonists to inhibit re-absorption of bile acids represents a novel avenue to develop a new class of safe and oral drugs for treatment of hypercholesterolemia and other cardiovascular diseases,” said Dr Kunwar Shailubhai, chief scientific officer of Synergy. “It is well documented that dietary or pharmacological manipulation of the enterohepatic circulation of either cholesterol or bile acids can potentially cause marked changes in plasma cholesterol levels.”

GC-C agonists are a new class of non-systemic drugs currently being developed to treat chronic constipation, constipation-predominant-Irritable Bowel Syndrome (IBS-C) and other functional GI disorders. Plecanatide, Synergy’s lead GC-C agonist in clinical development, is a synthetic analogue of uroguanylin, a natriuretic hormone that regulates ion and fluid transport in the GI tract.

Orally-administered plecanatide binds to and activates GC-C expressed on epithelial cells lining the GI mucosa, resulting in activation of the cystic fibrosis transmembrane conductance regulator, and leading to augmented flow of chloride and water into the lumen of the gut, facilitating bowel movement. In animal models, oral administration of plecanatide promotes intestinal secretion as well as ameliorating gastrointestinal inflammation.

Synergy is a biopharmaceutical company focused on the development of new drugs to treat gastrointestinal disorders and diseases.