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Endothelin Receptor Antagonist
An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: * selective ETA receptor antagonists ( sitaxentan, ambrisentan, atrasentan, BQ-123, zibotentan, edonentan), which affect endothelin A receptors. * dual antagonists (bosentan, macitentan, tezosentan), which affect both endothelin A and B receptors. * selective ETB receptor antagonists (BQ-788 and A192621) which affect endothelin B receptors 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 is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal b ... drug. References {{cardiova ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Medication
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and relies on the science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are classified in multiple ways. One of the key divisions is by level of control, which distinguishes prescription drugs (those that a pharmacist dispenses only on the order of a physician, physician assistant, or qualified nurse) from over-the-counter drugs (those that consumers can order for themselves). Another key distinction is between traditional small molecule drugs, usually derived from chemical synthesis, and biopharmaceuticals, which include recombinant proteins, vaccines, blood products used therapeutically (such as IVIG), gene therapy, monoclonal antibodies and cell therapy (for instance, stem cell therapies) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endothelin Receptor
There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose activation result in elevation of intracellular-free calcium, which constricts the smooth muscles of the blood vessels, raising blood pressure, or relaxes the smooth muscles of the blood vessels, lowering blood pressure, among other functions. Physiological functions *ETA is a subtype for vasoconstriction These receptors are found in the smooth muscle tissue of blood vessels, and binding of endothelin to ETA increases vasoconstriction (contraction of the blood vessel walls) and the retention of sodium, leading to increased blood pressure. *ETB1 mediates vasodilation, When endothelin binds to ETB1 receptors, this leads to the release of nitric oxide (also called endothelium-derived relaxing factor), natriuresis and diuresis (the production and elimination of urine) and mechanisms that lower blood pressure. *ETB2 mediates vasoconstriction *ETC has yet no c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sitaxentan
Sitaxentan sodium (TBC-11251) is a medication for the treatment of pulmonary arterial hypertension (PAH). It was marketed as Thelin by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market due to concerns about liver toxicity.Citing liver damage, Pfizer withdraws Thelin Associated Press, December 12, 2010 Mechanism of action Sitaxentan is a that blocks the action of |
Ambrisentan
Ambrisentan (U.S. trade name Letairis; E.U. trade name Volibris; India trade name Pulmonext by MSN labs) is a drug indicated for use in the treatment of pulmonary hypertension. The peptide endothelin constricts muscles in blood vessels, increasing blood pressure. Ambrisentan, which relaxes those muscles, is an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA). Ambrisentan significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 and ARIES-2). Like all endothelin receptor antagonists, Ambrisentan is contraindicated in pregnant women as well as those who are trying to become pregnant, due to the potential for teratogenic effects on the fetus. Patients who are on the Ambrisentan must enroll in the Ambrisentan (Letairis) REMS Program. Ambrisentan was approved by the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA), and designated ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atrasentan
Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is also being investigated as a therapy for diabetic kidney disease. Atrasentan failed a phase 3 trial for prostate cancer in patients unresponsive to hormone therapy. A second trial confirmed this finding. It is an endothelin receptor antagonist selective for subtype A (ETA). While other drugs of this type ( sitaxentan, ambrisentan) exploit the vasoconstrictive Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vessel ... properties of endothelin and are mainly used for the treatment of pulmonary arterial hypertension, atrasentan blocks endothelin induced cell proliferation. In April 2014, de Zeeuw et al. showed that 0.75 mg and 1.25 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BQ-123
BQ-123, also known as cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu-), is a cyclic pentapeptide that was first isolated from a fermentation broth of '' Streptomyces misakiensis'' in 1991. NMR studies indicate that the polypeptide backbone consists of a type II beta turn and an inverse gamma turn. The side-chains adopt different orientations depending on the solvent used. The proline carbonyl oxygen atom located at the onset of a beta turn is a sodium ion binding site. It has a high affinity for sodium ions and can coordinate up to three of them. Studies have shown that BQ123 is effective in reversing Ischemia-induced acute renal failure, and it has been suggested that this might be because BQ123 increases reabsorption of sodium ions in the proximal tubule cells. BQ-123 is a selective ETA endothelin receptor antagonist. As such, it is used as a biochemical tool in the study of endothelin receptor There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zibotentan
Zibotentan (INN; development code ZD4054) is an experimental anti-cancer drug candidate in development by AstraZeneca. It is an endothelin receptor antagonist. Zibotentan was granted fast track status for the treatment of prostate cancer by the FDA. It failed a phase III clinical trial for prostate cancer, but other trials are planned. Tolerability of zibotentan plus docetaxel has been evaluated. Zibotentan has also been studied in clinical trials for treatment of breast cancer, colorectal cancer, non-small cell lung cancer, ovarian cancer Ovarian cancer is a cancerous tumor of an ovary. It may originate from the ovary itself or more commonly from communicating nearby structures such as fallopian tubes or the inner lining of the abdomen. The ovary is made up of three different c ..., scleroderma-related renal disease, bone metastasis, and heart failure. References {{reflist External links Zibotentan Experimental cancer drugs Oxadiazoles Pyridines Sulfonamides Pyr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endothelin Receptor Type A
Endothelin 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. See also * Endothelin receptor There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose activation result in elevation of intracellular-free calcium, which constricts the smooth muscles of the blood vessels ... References External links * Further reading * * * * * * * * * * * * * * * * * * * * * * G protein-coupled receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bosentan
Bosentan, sold under the brand name Tracleer and Safebo among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery hypertension (PAH). Bosentan is available as film-coated tablets (62.5 mg or 125 mg) or as dispersable tablets for oral suspension (32 mg). Medical uses Bosentan is used to treat people with moderate pulmonary arterial hypertension and to reduce the number of digital ulcers — open wounds on especially on fingertips and less commonly the knuckles — in people with systemic scleroderma. Bosentan causes harm to fetuses and pregnant women must not take it, and women must not become pregnant while taking it (Pregnancy Category X). It may render hormonal contraceptives ineffective so other forms of birth control must be used. In the US it is only available from doctors who follow an FDA-mandated risk evaluation and mitigation strategy (REMS) with respect to risks to fetuses and its risks of causing liv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Macitentan
Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist (ERA) developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). The other two ERAs marketed as of 2014 are bosentan and ambrisentan. Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype. The drug received approval from the U.S. Food and Drug Administration (FDA) on October 13, 2013. Macitentan is available as a generic medication in the United States as of April 2021. Adverse effects The FDA has issued a black box warning for macitentan for embryo-fetal toxicity. It is only available to females in the U.S through a risk evaluation and mitigation strategy (REMS) program. Mechanism of action Endothelin and endothelin receptors Endothelin (ET) is an extremely potent blood vessel constr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tezosentan
Tezosentan is a non-selective ETA and ETB receptor antagonist. It acts as a vasodilator and was designed by Actelion as a therapy for patients with acute heart failure. However, studies showed that tezosentan did not improve dyspnea Shortness of breath (SOB), also medically known as dyspnea (in AmE) or dyspnoea (in BrE), is an uncomfortable feeling of not being able to breathe well enough. The American Thoracic Society defines it as "a subjective experience of breathing di ... or reduce the risk of fatal or nonfatal cardiovascular events. References Vasodilators Tetrazoles Pyridines Pyrimidines Phenol ethers Sulfonamides Alcohols Endothelin receptor antagonists Isopropyl compounds Diaryl ethers {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
