What is the active metabolite of the prodrug Sacubitril?

The active metabolite of the prodrug Sacubitril is LBQ657. Sacubitril itself is converted into this active form through metabolism in the body. LBQ657 functions as a neprilysin inhibitor, which plays a crucial role in promoting vasodilation and enhancing the effects of natriuretic peptides. This mechanism is significant in the management of heart failure, as it helps to reduce strain on the heart and improve outcomes for patients.

Understanding this relationship is important, as the pharmacological effects of Sacubitril are largely dependent on the actions of LBQ657. By inhibiting neprilysin, LBQ657 increases the levels of natriuretic peptides, which contribute to fluid balance and vasoregulation. The premature termination of Sacubitril’s effects without this conversion underscores the importance of recognizing LBQ657 as the key active metabolite that mediates the intended therapeutic effects in clinical practice.