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March 22, 2007

Patient Enrollment Initiated for Phase II Study With New Endothelin Receptor Antagonist For Resistant Hypertension

Topics: Medicine

Encysive Pharmaceuticals Inc. announced yesterday that the first patient has been enrolled into its Phase II dose-ranging study of oral TBC3711, the Company's next-generation, highly selective endothelin receptor antagonist, in resistant hypertension. The 12-week, multi-center, randomized, double-blind, placebo-controlled study will evaluate four once-daily oral doses of TBC3711 in approximately 150 patients with diagnosed resistant hypertension:

TBC3711 is a small molecule that blocks the action of endothelin, a potent mediator of blood vessel constriction and growth of smooth muscle in vascular walls. TBC3711 is a next-generation endothelin A antagonist which possesses high oral bioavailability and is more selective and potent than THELIN(tm) (sitaxsentan sodium) Encysive's oral treatment for pulmonary arterial hypertension. TBC3711 is greater than 100,000-fold selective in the targeting of the endothelin A receptor versus the endothelin B receptor.

Many individuals can successfully lower blood pressure through lifestyle modifications and/or treatment with one or more approved hypertension drugs. Resistant hypertension is defined as the failure to reach goal blood pressure (less than 140/90 mmHg) in patients who are adhering to a regimen of full doses of three anti-hypertensive drugs, including a diuretic. A direct relationship exists between increased blood pressure and risk of heart attack, stroke, kidney disease and heart failure.

Endothelin (ET)-1 is an endothelium-derived peptide (endothelium is a layer of cells which line the heart and blood vessels) with potent vasoconstrictor and proliferative properties (constricts blood vessels and elevates blood pressure). Endothelin receptor antagonists are a new class of drugs for the treatment of a number of major diseases, including pulmonary arterial hypertension.

More here...

Cross posted from New Hope Blog

Posted by Richard at March 22, 2007 7:52 AM

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