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TBC3711

Pfizer Inc.

Drug Names(s): TBC3711

Description: TBC3711 is a second generation endothelin A antagonist, which Encysive believes is more selective and potent than its first drug, Thelin.

Endothelin is a small peptide hormone that is believed to play a critical role in the control of blood flow and cell growth. Elevated endothelin blood levels are associated with several cardiovascular disease conditions, including pulmonary arterial hypertension, chronic kidney disease, hypertension, chronic heart failure, stroke and restenosis of arteries after balloon angioplasty or stent implantation. There are two classes of endothelin receptors, ETA and ETB, which play significantly different roles in regulating blood vessel diameter. The binding of endothelin to ETA receptors located on smooth muscle cells causes vasoconstriction, or narrowing of the blood vessels. However, the binding of endothelin to ETB receptors located on the vascular endothelium causes vasodilation through the production of nitric oxide. The activity of the ETB receptor is thought to be counter-regulatory, protecting against excessive vasoconstriction.

Deal Structure: TBC3711 was originally developed by Texas Biotechnology Corporation (TBC).

In May 2003, Texas Biotechnology Corporation announced, following approval by its shareholders, the change of its corporate name to Encysive Pharmaceuticals.

In April 2008, Encysive became a wholly-owned subsidiary of Pfizer.


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