Product Description
Pharmaceutical
Raw Materials and Intermediates
AI Product Description
*The following content is generated by AI and is for reference only.
LCZ696, known by the developmental code AHU-377 during its clinical trials, is a novel fixed-dose combination medication comprising two active pharmaceutical ingredients: sacubitril and valsartan. Sacubitril acts as a prodrug that converts to sacubitrilat in vivo, functioning as a neprilysin inhibitor. This mechanism prevents the breakdown of natriuretic peptides, bradykinin, and adrenomedullin, thereby promoting vasodilation, natriuresis, and diuresis. Valsartan is an angiotensin II receptor blocker (ARB) that antagonizes the renin-angiotensin-aldosterone system (RAAS), inhibiting vasoconstriction and aldosterone secretion. The synergistic action of these dual mechanisms offers superior hemodynamic benefits compared to traditional ACE inhibitors alone.
The molecular formula for LCZ696 represents the combination of its components rather than a single unified structure, as it is a salt formed between sodium sacubitrilat and valsartan. Specifically, sacubitrilat has the formula C25H28N4O5Na, while valsartan is C24H29N5O6. The combined therapeutic entity does not possess a singular CAS number; instead, sacubitril carries CAS 1060660-60-3, valsartan is assigned CAS 137862-53-4, and the specific combination drug LCZ696 is often associated with CAS 1212073-33-8 in regulatory contexts.
Clinically, LCZ696 is primarily indicated for the treatment of heart failure with reduced ejection fraction (HFrEF) in adults to reduce cardiovascular death and hospitalization risk. It was developed based on the landmark PARADIGM-HF trial, which demonstrated significant mortality benefits over enalapril. Beyond heart failure, research is ongoing to evaluate its efficacy in chronic kidney disease and hypertension management due to its unique ability to modulate multiple neurohormonal pathways simultaneously. By blocking both the degradation of beneficial peptides and the activation of harmful angiotensin II receptors, this agent provides a comprehensive approach to managing complex cardiovascular pathologies, marking a significant advancement in pharmacotherapy for patients with compromised cardiac function.