| Summary: | Variants in the <i>CES1</i> gene encoding carboxylesterase 1 may affect the metabolism of enalapril to the active metabolite enalaprilat. It was shown that the A allele of rs71647871 and the C allele of rs2244613 led to a decrease in plasma enalaprilat concentrations. This study aimed to estimate the effect of structural haplotypes of <i>CES1</i> containing the pseudogene <i>CES1P1,</i> or a hybrid of the gene and the pseudogene <i>CES1A2,</i> on the pharmacokinetics of enalapril. We included 286 Caucasian patients with arterial hypertension treated with enalapril. Genotyping was performed using real-time PCR and long-range PCR. Peak and trough plasma enalaprilat concentrations were lower in carriers of <i>CES1A2</i>. The studied haplotypes were in linkage disequilibrium with rs2244613: generally, the A allele was in the haplotype containing the <i>CES1P1</i>, and the C allele was in the haplotype with the <i>CES1A2</i>. Thus, carriers of <i>CES1A2</i> have reduced CES1 activity against enalapril. Linkage disequilibrium of the haplotype containing the <i>CES1P1</i> or <i>CES1A2</i> with rs2244613 should be taken into account when genotyping the <i>CES1</i> gene.
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