Tezosentan in the management of decompensated heart failure.

Decompensated heart failure continues to significantly impact the economics of our healthcare system. In recent years, the focus on management of decompensated heart failure has changed from solely improving hemodynamics to modifying neurohormones. Endothelin (ET) is one of the important mediators in heart failure. This article reviews the clinical pharmacology, clinical efficacy, and tolerability of tezosentan, a dual-action ET-1 receptor antagonist. Using the search term tezosentan, a literature review was conducted to identify peer-reviewed articles and abstracts in MEDLINE (1966 to April 2004) and Current Content (1966 to April 2004) databases. Citations from available articles were also reviewed for additional references. When given as an intravenous infusion, tezosentan achieves steady-state concentration within the first 6 hours. Tezosentan is excreted almost entirely through the bile (>95%) and has a terminal elimination half-life of 3 hours. The side effects of tezosentan include headache, nausea, and hypotension. Clinical studies demonstrated mixed results for tezosentan regarding its efficacy and tolerability in the management of decompensated heart failure. The role or tezosentan in treating heart failure is yet to be defined.