Title : Effect of CES1 genetic variation on enalapril steady-state pharmacokinetics and pharmacodynamics in healthy subjects.

Pub. Date : 2021 Dec

PMID : 33963573






6 Functional Relationships(s)
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1 Effect of CES1 genetic variation on enalapril steady-state pharmacokinetics and pharmacodynamics in healthy subjects. Enalapril carboxylesterase 1 Homo sapiens
2 BACKGROUND AND OBJECTIVE: Enalapril is a prodrug and needs to be activated by carboxylesterase 1 (CES1). Enalapril carboxylesterase 1 Homo sapiens
3 BACKGROUND AND OBJECTIVE: Enalapril is a prodrug and needs to be activated by carboxylesterase 1 (CES1). Enalapril carboxylesterase 1 Homo sapiens
4 A previous in vitro study demonstrated the CES1 genetic variant, G143E (rs71647871), significantly impaired enalapril activation. Enalapril carboxylesterase 1 Homo sapiens
5 A prospective, multi-dose, pharmacokinetics, and pharmacodynamics (PK/PD) study was conducted to determine the impact of the CES1 G143E variant on enalapril steady-state PK and PD in healthy volunteers. Enalapril carboxylesterase 1 Homo sapiens
6 CONCLUSIONS: The CES1 loss-of-function G143E variant significantly impaired enalapril activation and its systolic blood pressure-lowering effect in healthy volunteers. Enalapril carboxylesterase 1 Homo sapiens