Ambrisentan

drugbox
IUPAC_name = (2"S")-2- [(4,6-dimethylpyrimidin-2-yl)oxy] -3-methoxy- 3,3-diphenylpropanoic acid

---

CAS_number = 177036-94-1
ATC_prefix = C02
ATC_suffix = KX02
PubChem = 197712
DrugBank =
smiles = COC(C(Oc1nc(C)cc(C)n1)C(O)=O)(c2ccccc2)c3ccccc3
C = 22 | H = 22 | N = 2 | O = 4
molecular_weight = 378.421 g/mol
bioavailability = Undetermined
protein_bound = 99%
metabolism =
elimination_half-life = 15 hours (terminal)
excretion =
pregnancy_AU =
pregnancy_US = X
pregnancy_category= May cause harm to fetus
legal_AU =
legal_CA =
legal_UK = POM
legal_US = Rx-only
legal_status =
routes_of_administration = Oral
licence_EU = Volibris
licence_US = Ambrisentan

Ambrisentan (U.S. trade name Letairis; E.U. trade name Volibris) 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 (ET_A). [cite journal |author=Vatter H, Seifert V |title=Ambrisentan, a non-peptide endothelin receptor antagonist |journal=Cardiovasc Drug Rev |volume=24 |issue=1 |pages=63–76 |year=2006 |pmid=16939634 |doi=10.1111/j.1527-3466.2006.00063.x]

Ambrisentan was approved for sale by the U.S. Food and Drug Administration (FDA) on June 15 2007 for the once-daily treatment of pulmonary arterial hypertension. [cite news
last = Pollack
first = Andrew
title = Gilead’s Drug Is Approved to Treat a Rare Disease
work = New York Times
date = 2007-06-16
url = http://www.nytimes.com/2007/06/16/business/16gilead.html
accessdate = 2007-05-25] [cite press release
title = U.S. Food and Drug Administration Approves Gilead's Letairis Treatment of Pulmonary Arterial Hypertension
publisher = Gilead Sciences
date = 2007-06-15
url = http://www.gilead.com/wt/sec/pr_1016053
accessdate = 2007-06-16] [cite press release
title = FDA Approves New Orphan Drug for Treatment of Pulmonary Arterial Hypertension
publisher = Food and Drug Administration
date = 2007-06-15
url = http://www.fda.gov/bbs/topics/NEWS/2007/NEW01653.html
accessdate = 2007-06-22] It was later approved by the European Medicines Agency for use in the EU on April 2008. [cite press release
title = GlaxoSmithKline's Volibris (ambrisentan) receives authorisation from the European Commission for the treatment of Functional Class II and III Pulmonary Arterial Hypertension
publisher = GlaxoSmithKline
date = 2008-04-25
url = http://www.gsk.com/media/pressreleases/2008/2008_pressrelease_10033.htm
accessdate = 2008-04-29] Ambrisentan had previously been designated an orphan drug by both the FDA and the European Commission, in August 2004 and May 2005 respectively. [cite web
last = Waknine
first = Yael
title = International Approvals: Ambrisentan, Oral-lyn, Risperdal
publisher = Medscape
date = 2005-05-09
url = http://www.medscape.com/viewarticle/504469
accessdate = 2007-06-16]

Clinical uses

Ambrisentan is indicated for the treatment of pulmonary arterial hypertension (WHO Group 1) inpatients with WHO class II or III symptoms to improve exercise capacity and delay clinical worsening.

The LETAIRIS Education and Access Program

The LETAIRIS Education and Access Program (LEAP) is is a program to help physicians and patients learn about the risks of LETAIRIS, including the serious risks of liver injury and birth defects.

LEAP works by:

* Providing information to prescribers on the risks of LETAIRIS
* Providing comprehensive education to patients and assistance with obtaining LETAIRIS
* Requiring enrollment of both prescriber and patient in LEAP
* Controlling dispensing through a specialized distribution network (specialty pharmacies)

External links

* [http://www.letairis.com/ Letairis website] run by Gilead Sciences
* [http://www.letairis.com/downloads/LETAIRIS_prescribing_information.pdf Prescribing information]
* [http://www.letairis.com/how_to_get_letairis.html Information on the LETAIRIS Education and Access Program (LEAP)]

References