Disposition and metabolism of [(14)C] Sacubitril/Valsartan (formerly LCZ696) an angiotensin receptor neprilysin inhibitor, in healthy subjects.

@article{Flarakos2016DispositionAM,
  title={Disposition and metabolism of [(14)C] Sacubitril/Valsartan (formerly LCZ696) an angiotensin receptor neprilysin inhibitor, in healthy subjects.},
  author={Jimmy Flarakos and Yancy Du and Timothy Bedman and Qusai Al-Share and Pierre J. Jordaan and Priya Chandra and Diego Albrecht and Lai Mun Wang and Helen Gu and Heidi J. Einolf and S W Huskey and James B. Mangold},
  journal={Xenobiotica; the fate of foreign compounds in biological systems},
  year={2016},
  volume={46 11},
  pages={986-1000}
}
1. Sacubitril/valsartan (LCZ696) is an angiotensin receptor neprilysin inhibitor (ARNI) providing simultaneous inhibition of neprilysin (neutral endopeptidase 24.11; NEP) and blockade of the angiotensin II type-1 (AT1) receptor. 2. Following oral administration, [(14)C]LCZ696 delivers systemic exposure to valsartan and AHU377 (sacubitril), which is rapidly metabolized to LBQ657 (M1), the biologically active neprilysin inhibitor. Peak sacubitril plasma concentrations were reached within 0.5-1 h… CONTINUE READING

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