Key result
Endothelin-receptor antagonists are clinically used for pulmonary arterial hypertension and are under investigation for cancer and fibrogenic diseases, though liver toxicity remains a major side effect.
Endothelin-receptor antagonists are established therapies for pulmonary arterial hypertension but require monitoring for liver toxicity and fluid retention, while their utility in cancer and fibrosis remains under investigation.
Endothelin-receptor antagonists require liver monitoring in pulmonary arterial hypertension; leaves open expanded roles in cancer and fibrosis.
The endothelin axis and in particular the two endothelin receptors, ETA and ETB, are targets for therapeutic intervention in human diseases. Endothelin-receptor antagonists are in clinical use to treat pulmonary arterial hypertension and have been under clinical investigation for the treatment of several other diseases, such as systemic hypertension, cancer, vasospasm, and fibrogenic diseases. In this Perspective, we review the molecules that have been evaluated in human clinical trials for the treatment of pulmonary arterial hypertension, as well as other cardiovascular diseases, cancer, and fibrosis. We will also discuss the therapeutic consequences of receptor selectivity with regard to ETA-selective, ETB-selective, or dual ETA/ETB antagonists. We will also consider which chemical characteristics are relevant to clinical use and the properties of molecules necessary for efficacy in treating diseases against which known molecules displayed suboptimal efficacy.
No takes yet. Share an insight, caveat, or question.
Aubert et al. (2016) conducted a review in Pulmonary arterial hypertension, cancer, and fibrosis. Endothelin-receptor antagonists was evaluated. Endothelin-receptor antagonists are clinically used for pulmonary arterial hypertension and are under investigation for cancer and fibrogenic diseases, though liver toxicity remains a major side effect.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: