Investigated for use/treatment in congestive heart failure, hypertension, and pulmonary hypertension.
Mechanism of action
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. It 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.
Wu C, Decker ER, Blok N, Bui H, You TJ, Wang J, Bourgoyne AR, Knowles V, Berens KL, Holland GW, Brock TA, Dixon RA: Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2 -carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. J Med Chem. 2004 Apr 8;47(8):1969-86. [PubMed:15055997 ]