An update on the status of endothelin receptor antagonists for hypertension.
Endothelin receptor antagonists (ETRA) are actively developed by the pharmaceutical industry for several cardiovascular indications. In the context of hypertension, preclinical studies are increasingly focused on prevention or regression of end-organ damage and drug combination than on control of arterial pressure in monotherapy, as most experimental models have already been studied. In general, the antihypertensive effect of ETRA is limited but the overwhelming efficacy of this class of drugs to prevent several end-organ damages warrants judicious combination. However, the few studies looking at regression of hypertension-induced cardiovascular alterations proved less successful, suggesting that ETRA should be used early in the treatment of hypertension to obtain full benefit. Judging from the progression of ongoing trials and the development of new trials patients suffering from pulmonary hypertension and heart failure may be the first to benefit from this new class of drugs. However, it is expected that once on the market, responsive subsets of hypertensive patients will be identified and will benefit from end-organ protection.
Moreau
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Laboratory of Vascualar Pharmacology, Faculty of Pharmacy, Université de Montréal, P.O. Box 6128, Stn 'Centre-ville,' Montréal, Quebec, H3C 3J7, Canada. Pierre.Moreau@umontreal.ca
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D000818:Animals; D000959:Antihypertensive Agents / Q000627:therapeutic use*; D004359:Drug Therapy, Combination; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000502:physiology; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology
D000959:Antihypertensive Agents; D065128:Endothelin Receptor Antagonists; D016232:Endothelins