Which of the following is a Neprilysin inhibitor?
Correct Answer: Sacubitril
Description: Sacubitril is a prodrug Neprilysin inhibitor approved for the treatment of hea failure in conjunction with the Angiotensin Receptor Blockade, Valsaan(Sacubitril/Valsaan). Sacubitril is also undergoing clinical testing for its role in the treatment of hypeension. Neprilysin (NEP) is an endopeptidase that metabolizes different vasoactive peptides especially natriuretic peptides including Atrial and Brain Natriuretic peptides thereby promoting diuresis, natriuresis and vasodilation. Sacubitril is a prodrug that once activated inhibits the enzyme Neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide. Sacubitril/Valsaan: Angiotensin Receptor blocker-Neprilysin Inhibitor (ARNI) combination: Sacubitril/Valsaan is a first-in-class medicine that contains a Neprilysin (NEP) inhibitor (Sacubitril) and an Angiotensin II (Ang-II) receptor blocker (Valsaan) Neprilysin(NEP) is an endopeptidase that metabolize different vasoactive peptides including natriuretic peptides, bradykinin and Ang-II. NEP substrates may have biological opposing action and the total effect of the inhibition depends on the net effect of the individual metabolized substrates. Neprilysin inhibition not only increases the levels of both, natriuretic peptides (promoting diuresis, natriuresis and vasodilatation) but also increases the level of Ang-II (producing an opposite action of vasoconstriction and aldosterone release) The benefits of increasing the Natriuretic peptides (NP) system may thus be lost by increasing Ang-II, therefore a simultaneous suppression of the RAAS is necessary. Addition of Valsaan (angiotensin receptor blocker) blocks the undesirable effects of Ang-II (thereby reducing the undesirable effects of vasoconstriction and aldosterone release) Consequently, the ARNI is expected to promote the beneficial effects natriuresis, diuresis and vasodilatation of aerial and venous blood vessels and to inhibit thrombosis, fibrosis, cardiac myocyte hyperophy, and renin release. Ref: Goodman and Gilman 13th edition Pgno: 485
Category:
Pharmacology
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