Omapatrilat

Omapatrilat
Systematic (IUPAC) name
(4S,7S,10aS)-5-oxo-4-{[(2S)-3-phenyl-2- sulfanylpropanoyl]amino}-2,3,4,7,8,9,10,10a-octahydropyrido[6,1-b] [1,3]thiazepine-7-carboxylic acid
Identifiers
CAS Number 167305-00-2 YesY
ATC code none
PubChem CID 656629
ChemSpider 570983 N
UNII 36NLI90E7T N
ChEMBL CHEMBL289556 N
Chemical data
Formula C19H24N2O4S2
Molar mass 408.534 g/mol
 NYesY (what is this?)  (verify)

Omapatrilat (INN) is a novel antihypertensive agent that inhibits both neutral endopeptidase (NEP) and angiotensin converting enzyme. NEP inhibition results in elevated natriuretic peptide levels, promoting natriuresis, diuresis, vasodilation, and reductions in preload and ventricular remodeling.

This drug from Bristol-Myers Squibb was not approved by the U.S. Food and Drug Administration due to angioedema safety concerns.[1]

Omapatrilat angioedema was attributed to its dual mechanism of action, inhibiting both angiotensin converting enzyme (ACE), and neutral endopeptidase, both of these enzymes are responsible for the metabolism of bradykinin which causes vasodilation, angioedema, and airway obstruction.

Clinical uses

The drug was promoted for possible uses in congestive heart failure.

See also

References

  1. Joshi Venugopal. (2003) Pharmacological modulation of the natriuretic peptide system. Expert Opinion on Therapeutic Patents 13:9, 1389



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