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Neprilysin inhibitors block a zinc endopeptidase that inactivates natriuretic and opioid peptides. Neprilysin (NEP), also called neutral endopeptidase, was purified in 1974 from rabbit kidney brush border membranes. In 1978 a high-affinity enkephalin-degrading peptidase was described in brain, and the activity became known as enkephalinase. Further NEP substrates include atrial natriuretic peptide, bradykinin, substance P and amyloid-β peptides. Sacubitril calcium and candoxatril are prodrugs, and sacubitrilat is the active form of sacubitril. Racecadotril is a prodrug of an enkephalinase inhibitor, and phosphoramidon disodium salt is a microbial metalloendopeptidase inhibitor. Omapatrilat blocks both NEP and angiotensin-converting enzyme (ACE), while Sacubitril/Valsartan combines NEP inhibition with angiotensin receptor blockade.
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.
