Drug intelligence / Profile preview

sacubitril + valsartan + sitagliptin

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

This is a theoretical combination of three active ingredients: sacubitril (a neprilysin inhibitor), valsartan (an angiotensin II receptor blocker), and sitagliptin (a dipeptidyl peptidase-4 inhibitor). The sacubitril/valsartan component (marketed as Entresto) is used to treat heart failure by simultaneously inhibiting neprilysin via LBQ657 (the active metabolite of sacubitril) and blocking the angiotensin II type-1 receptor via valsartan. This combination helps reduce the risk of cardiovascular death and hospitalization in patients with chronic heart failure. Sitagliptin is used for the management of type 2 diabetes mellitus by inhibiting DPP-4, which leads to glucose-dependent increases in insulin and decreases in glucagon to improve blood sugar control.

02

Targets

AGTR1 (Angiotensin II Type-1 receptor)DPP-4 (Dipeptidyl Peptidase-IV)NEP (Neutral Endopeptidase)

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