Entresto LCZ696 (Valsartan/sacubitril)

CAS No:
936623-90-4 Categories: , ,
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Product Details:

  • CAS No: 936623-90-4
  • AHFC code:
  • Synonyms: LCZ 696, LCZ-696, LCZ696, Sacubitril mixture with valsartan, Trisodium (3-(1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-3'-methyl-2'-(pentanoyl(2'-(tetrazol-5-ylate)biphenyl-4'-ylmethyl)amino)butyrate) hemipentahydrate, UNII-WB8FT61183, Valsartan mixture with AHU-377
  • ATC Code:
  • Chemical Formula: C24-H29-N5-O3.C24-H29-N-O5.5/2H2-O.3Na
  • Molecular Weight: 1916.007
  • Assay/Purity: Typically NLT 98%
  • DrugBank:
  • SMILES:
  • InChl:
  • PubChem:
  • IUPAC:

Additional Details

Indication:
LCZ696 (Entresto) is indicated for patients with chronic heart failure to combat cardiovascular hospitalizations and all-cause mortality.
Pharmacodynamics:
LCZ696 is an efficacious angiotensin receptor-neprilysin inhibitor. As a combination of Sacubitril, a first-in-class neprilysin inhibitor, and the angiotensin receptor antagonist Valsartan) works via augmentation of natriuretic peptides.
Mode of Action:
Entresto, or LCZ696 offers a unique mode of action as it effectively reduces strain and stress on the heart by harnessing the body's natural defense, or protective neurohormonal systems of the heart against heart failure. An enhancement of natriuretic levels and endogenous vasoactive peptides, as well as an inhibition of the renin-angiotensin-aldosterone system makes LCZ696 effectual.
Metabolism:
LCZ696 is associated with dose-dependent increases in plasma cGMP, angiotensin II and renin activity, which is consistent with this drug’s dual mechanism of action. A typical dosage of 200-400 milligrams of LCZ696 attains 90% of its maximal NEP inhibition metabolically.
Toxicity:
The toxicity of LCZ696 has not been determined to be concerning. Common side effects reported by patients in investigational studies include high potassium, dizziness, lower than normal blood pressure, cough and kidney problems.
General Reference:
Ito S, Satoh M, Tamaki Y, Gotou H, Charney A, Okino N, Akahori M, Zhang J. Safety and efficacy of LCZ696, a first-in-class angiotensin receptor neprilysin inhibitor, in Japanese patients with hypertension and renal dysfunction. Hypertens Res. 2015 Feb 19. http://www.egyreg.com/2015/06/entresto-sacubitril-valsartan-fda-2015.htmlMcMurray JJV et al. Angiotensin-Neprilysin Inhibition versus Enalapril in Heart Failure, N Engl J Med 2014.
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