Drug intelligence / Profile preview

tbc-3711

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

TBC-3711 is a next-generation, highly selective endothelin A receptor antagonist developed originally by Encysive Pharmaceuticals. It is a small molecule designed for oral and intravenous administration. The drug blocks the action of endothelin—a potent mediator of blood vessel constriction and smooth muscle growth in vascular walls—by selectively antagonizing the endothelin A receptor with over 100,000-fold selectivity versus the endothelin B receptor. This mechanism makes it more selective and potent than sitaxsentan sodium (THELIN), another drug from Encysive. TBC-3711 was investigated primarily for resistant hypertension and other cardiovascular disorders but development was discontinued after Phase II trials. Pfizer acquired Encysive Pharmaceuticals during its development[2][3][4][5].

Other names
Endothelin Mordulator 1
02

Targets

EDNRA (Endothelin receptor type A)

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