Endothelin receptor antagonist
Encyclopedia
A endothelin receptor antagonist (ERA) is a drug
that blocks endothelin
receptors.
Three main kinds of ERAs exist:
Sitaxentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension, while atrasentan is an experimental anti-cancer
drug.
Medication
A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...
that blocks endothelin
Endothelin
Endothelins are proteins that constrict blood vessels and raise blood pressure. They are normally kept in balance by other mechanisms, but when they are over-expressed, they contribute to high blood pressure and heart disease....
receptors.
Three main kinds of ERAs exist:
- selective ETA receptor antagonists (sitaxentan, ambrisentanAmbrisentanAmbrisentan is a drug indicated for use in the treatment of pulmonary hypertension.It functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor ....
, atrasentanAtrasentanAtrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer.It is an endothelin receptor antagonist selective for subtype A...
, BQ-123BQ-123BQ-123 is a cyclic peptide consisting of five amino acids. The amino acid sequence is D-tryptamine-D-aspartic acid-L-proline-D-valine-L-leucine....
, zibotentanZibotentanZibotentan is an anti-cancer candidate. It is a endothelin receptor antagonist.It failed a phase III clinical trial for prostate cancer but other trials are planned. Tolerability of zibotentan plus docetaxel has been evaluated....
), which affect endothelin A receptorsEndothelin receptor type AEndothelin receptor type A, also known as ETA, is a human G protein-coupled receptor.-Interactions:Endothelin receptor type A has been shown to interact with HDAC7A and HTATIP.-Further reading:...
. - dual antagonists (bosentanBosentanBosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension . It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.-Mechanism of action:Bosentan is...
, tezosentanTezosentanTezosentan is a non-selective ETA and ETB receptor antagonist. It acts as a vasodilator and was designed as a therapy for patients with acute heart failure. Recent studies have shown however, that tezosentan does not improve dyspnea or reduce the risk of fatal or nonfatal cardiovascular events....
), which affect both endothelin A and B receptorsEndothelin receptor type BEndothelin receptor type B, also known as ETB is a protein that in humans is encoded by the EDNRB gene.- Function :Endothelin receptor type B is a G protein-coupled receptor which activates a phosphatidylinositol-calcium second messenger system. Its ligand, endothelin, consists of a family of three...
. - selective ETB receptor antagonists (BQ-788) which affect endothelin B receptorsEndothelin receptor type BEndothelin receptor type B, also known as ETB is a protein that in humans is encoded by the EDNRB gene.- Function :Endothelin receptor type B is a G protein-coupled receptor which activates a phosphatidylinositol-calcium second messenger system. Its ligand, endothelin, consists of a family of three...
are used in research but have not yet reached the clinical trial stage.
Sitaxentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension, while atrasentan is an experimental anti-cancer
Cancer
Cancer , known medically as a malignant neoplasm, is a large group of different diseases, all involving unregulated cell growth. In cancer, cells divide and grow uncontrollably, forming malignant tumors, and invade nearby parts of the body. The cancer may also spread to more distant parts of the...
drug.