LCZ696 is a first-in-class dual inhibitor of the angiotensin II receptor(AT II receptor) and neprilysin; a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio).

Racecadotril (acetorphan), a potent enkephalinase inhibitor (IC50= 4.5 uM), protects endogenous enkephalins from degradation.

SCH-42354 is a potent, orally active neutral endopeptidase (NEP) inhibitor, is the pharmacologically active form of the prodrug SCH-42495. SCH-42354 inhibits the hydrolysis of NEP to enhance the activity of atrial natriuretic peptide (ANP). SCH-42354 inhibits hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. SCH-42354 has antihypertensive activity.

Thiorphan (DL-3-Mercapto-2-benzylpropanoylglycine) is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. It is also a potent inhibitor of enkephalinase, with antinociceptive activity.