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Article

Sacubitril Is Selectively Activated by Carboxylesterase 1 (CES1) in the Liver and the Activation Is Affected by CES1 Genetic Variation.

Drug metabolism and disposition: the biological fate of chemicals - 1 Apr 2016

Shi Jian, Wang Xinwen, Nguyen Jenny, Wu Audrey H, Bleske Barry E, Zhu Hao-Jie

Abstract excerpt

Sacubitril was recently approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure with reduced ejection fraction. As a prodrug, sacubitril must be metabolized (hydrolyzed) to its active metabolite sacubitrilat (LBQ657) to exert its intended therapeutic effects. Thus, understanding the determinants of sacubitril activation will lead to the...

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Source

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Identifiers

PMID: 26817948
DOI: 10.1124/dmd.115.068536
PMCID: PMC4810765

Genes

CES1

Variants

rs71647871

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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