March 22, 2007
Patient Enrollment Initiated for Phase II Study With New Endothelin Receptor Antagonist For Resistant HypertensionTopics: 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.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.
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.
Cross posted from New Hope Blog
Posted by Richard at March 22, 2007 7:52 AM
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