Review
Nature Reviews Drug Discovery 1, 986-1001 (December 2002) | doi:10.1038/nrd962
New therapeutics that antagonize endothelin: promises and frustrations
Giuseppe Remuzzi1,2, Norberto Perico1 & Ariela Benigni1 About the authors
Abstract
The discovery of endothelin — a highly potent endogenous vasoconstrictor — in 1988 has led to considerable efforts to develop antagonists of endothelin receptors that could have therapeutic potential in disorders including hypertension, heart failure and renal diseases. However, in general, the results of trials in humans have not mirrored the highly promising effects in animal disease models. Here, we discuss preclinical and clinical results with endothelin antagonists, and consider possible approaches to fully realizing the potential of endothelin antagonism.
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Author affiliations
- Mario Negri Institute for Pharmacological Research, Via Gavazzeni 11, 24125 Bergamo, Italy.
- Department of Medicine and Transplantation, Ospedali Riuniti Bergamo, Largo Barozzi 1, 24128 Bergamo, Italy.
Correspondence to: Giuseppe Remuzzi1,2 Email: gremuzzi@marionegri.it
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