Sacubitril/Valsartan Treats Patients With Essential Hypertension and Type 2 Diabetic Nephropathy

Sacubitril/Valsartan is a novel antihypertensive medication composed of an angiotensin II receptor blocker (ARB) Valsartan and a neprilysin inhibitor Sacubitril in a 1:1 molar co-crystal form. Sacubitril is a prodrug that, once ingested, is metabolized by esterases into its active form, which inhibits neprilysin activity. Neprilysin has various substrates, including natriuretic peptides and angiotensin II (Ang II). By inhibiting neprilysin, the levels of natriuretic peptides that have antihypertensive and organ-protective effects are increased. The other component, Valsartan, effectively inhibits the Ang II type 1 receptor (AT1R), providing additional antihypertensive and organ-protective effects. The co-crystal structure ensures that Sacubitril and Valsartan have similar absorption and elimination rates, thereby synchronizing their pharmacological effects.

Valsartan, effectively inhibits the Ang II type 1 receptor (AT1R), providing both antihypertensive and organ-protective effects.