Endothelin antagonists are drug candidates that acts against endothelin receptors and generate pharmacological actions such as blocking the vasoconstriction and mediate vasodilatation. Endothelin-1 is a peptide which is comprised of 21 amino acids and formed by vascular endothelium.
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The biological molecule is a potent vasoconstrictor that binds to endothelin receptors A and B. This further leads to the activation of IP3 DA pathway that causes efflux of calcium ions from the endoplasmic reticulum and produce vasoconstriction in the smooth muscles. The endothelin receptor B release nitric oxide that produce vasodilation effect in erectile muscles. The endothelin-1 releases calcium in heart, resulting in the increment of cardiac rate. The endothelin receptor antagonist is having powerful vasodilation properties as they have been shown to improve the hemodynamic and decrease the mortality rate in the mouse models of heart failure.
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AbbVie Inc. is in the process of developing ABT-627 as an endothelin receptor antagonist for the treatment of diabetic nephropathy in type 2 diabetes. Idorsia Pharmaceuticals Ltd. is developing ACT-132577 as an endothelin receptor antagonist for the treatment of resistant hypertension. Moreover, Retrophin Inc. is also developing sparsentan as an endothelin receptor antagonist for the treatment of focal segmental glomerulosclerosis. Ligand Pharmaceuticals Inc., and ENB Therapeutics LLC are some other companies having pipeline of endothelin receptor antagonist.
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The report provides a comprehensive understanding of the pipeline activities covering all drug candidates under various stages of development, with the detailed analysis of pipeline and clinical trials. Pipeline analysis of drugs by phases includes product description and development activities including information about clinical results, designations, collaborations, licensing, grants, technology, and others.