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| Trade names | Letairis, Volibris, Pulmonext |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a612023 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Protein binding | 99% |
| Eliminationhalf-life | 15 hours (terminal) |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.184.855 |
| Chemical and physical data | |
| Formula | C22H22N2O4 |
| Molar mass | 378.428 g·mol−1 |
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Ambrisentan, sold under the brand nameLetairis among others, is a drug used for the treatment ofpulmonary hypertension.[2][4] It is an endothelin receptor antagonist.[2]
The peptideendothelin constricts muscles in blood vessels, increasing blood pressure. Ambrisentan, which relaxes those muscles, is anendothelin receptor antagonist, and is selective for the type Aendothelin receptor (ETA).[5] Ambrisentan significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 and ARIES-2).[6] 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 forteratogenic effects on the fetus.[7]
Ambrisentan was approved by the USFood and Drug Administration (FDA) and theEuropean Medicines Agency (EMA), and designated anorphan drug, for the treatment of pulmonary hypertension.[8][3][9][10]
Ambrisentan isindicated for the treatment of pulmonary arterial hypertension (WHO Group 1) in people with WHO class II or III symptoms to improve exercise capacity and delay clinical worsening.[2][3]
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Ambrisentan is a drug that blocks endothelin, an endogenous hormone found in higher quantities in patients with pulmonary arterial hypertension. Endothelin binds to two receptors, ETA and ETB. ETA is responsible for cell growth in the vessels as well asvasoconstriction, while ETB plays a role invasodilation,endothelin 1 clearance, and antiproliferation of cells.
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Endothelin receptor activation mediates strong pulmonaryvasoconstriction and positiveinotropic effect on the heart. These physiologic effects are vital for the development of the fetal cardiopulmonary (heart and lung) system. In addition to this, endothelin receptors are also known to play a role inneural crest cell migration, growth, anddifferentiation. As such, endothelin receptor antagonists such as ambrisentan are known to beteratogenic.
Ambrisentan is sold under the brand name Letairis,[2] Volibris,[3] and Pulmonext.[citation needed]
 | This section needs to beupdated. Please help update this article to reflect recent events or newly available information.(April 2020) |
Last updated 9/2/2015 | |
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| 8/15/2015 Reprod. Toxicol. | Endothelin receptor activation mediates strong pulmonary vasoconstriction and positiveinotropic effect on the heart. These physiologic effects are vital for the development of the fetal cardiopulmonary system. As such,endothelin receptor antagonists such as ambrisentan areteratogenic.[11] |
| 8/27/2015 NEJM | Ambrisentan when used in combination therapy withtadalafil was found to be more efficacious in treatingtreatment naive patients withWHO class II or III pulmonary arterial hypertension than monotherapy using either drug.[12] |
