Ambrisentan

Ambrisentan

Clinical data
Pregnancy category	US: X (Contraindicated) May cause harm to fetus
Routes of administration	Oral
ATC code	C02KX02 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	Undetermined
Protein binding	99%
Elimination half-life	15 hours (terminal)
Identifiers
IUPAC name 2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy- 3,3-diphenyl-propanoic acid
CAS Number	177036-94-1
PubChem CID	197712
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C22H22N2O4
Molar mass	378.421 g/mol
3D model (JSmol)	Interactive image
SMILES COC(C(Oc1nc(C)cc(C)n1)C(O)=O)(c2ccccc2)c3ccccc3

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

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Overview

Ambrisentan (U.S. trade name Letairis) is a drug being researched 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).

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. The Marketing Authorisation Application is under review by the European Medicines Agency. Ambrisentan had previously been designated an orphan drug by both the FDA and the European Commission, in August 2004 and May 2005 respectively.

References

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