|Trade names||Letairis, Volibris, Pulmonext, others|
|Drug class||Endothelin receptor antagonist|
|Main uses||Pulmonary hypertension|
|Side effects||Swelling, palpitations, headache, constipation|
|Elimination half-life||15 hours (terminal)|
|Chemical and physical data|
|Molar mass||378.428 g·mol−1|
|3D model (JSmol)|
Ambrisentan, sold under the brand name Letairis among others, is a medication used for pulmonary hypertension. It improved the ability to exercise and slows worsening. It is not useful in those with pulmonary fibrosis. It is taken by mouth.
Common side effects include swelling, palpitations, headache, and constipation. Other side effects may include anemia, flushing, ringing in the ears, and liver problems. Use in pregnancy may harm the baby. It works by blocking the endothelin receptor, specifically the type A endothelin receptor (ETA).
Ambrisentan was approved for medical use in the United States in 2007 and Europe in 2008. In the United Kingdom it costs the NHS about £1,600 per month. In the United States this amount costs about 5,100 USD as of 2021.
Ambrisentan is used 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.
It is taken at a dose of 5 to 10 mg once per day.
Endothelin receptor activation mediates strong pulmonary vasoconstriction and positive inotropic effect on the heart. These physiologic effects are vital for the development of the fetal cardiopulmonary system. In addition to this, endothelin receptors are also known to play a role in neural crest cell migration, growth, and differentiation. As such, endothelin receptor antagonists such as Ambrisentan are known to be teratogenic.
Ambrisentan has a high risk of liver damage, and of birth defects if a woman becomes pregnant while taking it. In the U.S., doctors who prescribe it, and patients who take it, must enroll in a special program, the LETAIRIS Education and Access Program (LEAP), to learn about those risks. Ambrisentan is available only through specialty pharmacies.
Last Updated 9/2/2015
|8/15/2015 Reprod. Toxicol.||Endothelin receptor activation mediates strong pulmonary vasoconstriction and positive inotropic 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 are teratogenic.|
|8/27/2015 NEJM||Ambrisentan when used in combination therapy with tadalafil was found to be more efficacious in treating treatment naive patients with WHO class II or III Pulmonary Arterial Hypertension than monotherapy using either drug.|
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- Galiè, Nazzareno; Barberà, Joan A.; Frost, Adaani E.; Ghofrani, Hossein-Ardeschir; Hoeper, Marius M.; McLaughlin, Vallerie V.; Peacock, Andrew J.; Simonneau, Gérald; Vachiery, Jean-Luc; Grünig, Ekkehard; Oudiz, Ronald J.; Vonk-Noordegraaf, Anton; White, R. James; Blair, Christiana; Gillies, Hunter; Miller, Karen L.; Harris, Julia H.N.; Langley, Jonathan; Rubin, Lewis J. (2015). "Initial Use of Ambrisentan plus Tadalafil in Pulmonary Arterial Hypertension". New England Journal of Medicine. 373 (9): 834–44. doi:10.1056/NEJMoa1413687. hdl:2445/97236. PMID 26308684.