Ambrisentan
Chemical compound / From Wikipedia, the free encyclopedia
Dear Wikiwand AI, let's keep it short by simply answering these key questions:
Can you list the top facts and stats about Ambrisentan?
Summarize this article for a 10 year old
Ambrisentan, sold under the brand name Letairis among others, is a drug used for the treatment of pulmonary hypertension.[3][5] It is an endothelin receptor antagonist.[3]
This article needs additional citations for verification. (October 2021) |
Clinical data | |
---|---|
Trade names | Letairis, Volibris, Pulmonext |
AHFS/Drugs.com | Monograph |
MedlinePlus | a612023 |
License data |
|
Pregnancy category |
|
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Protein binding | 99% |
Elimination half-life | 15 hours (terminal) |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank |
|
ChemSpider |
|
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.184.855 |
Chemical and physical data | |
Formula | C22H22N2O4 |
Molar mass | 378.428 g·mol−1 |
3D model (JSmol) | |
| |
| |
(verify) |
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).[6] Ambrisentan significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 and ARIES-2).[7] 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.[8]
Ambrisentan was approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA), and designated an orphan drug, for the treatment of pulmonary hypertension.[9][4][10][11]