Carboxylesterase 1 Polymorphism Impairs Oseltamivir Bioactivation in Humans
Copyright policy )Carboxylesterase 1 Polymorphism Impairs Oseltamivir Bioactivation in Humans
Bioactivation of the antiviral agent oseltamivir to active oseltamivir carboxylate is catalyzed by carboxylesterase 1 (CES1). After the screening of 860 healthy Finnish volunteers for the CES1 c.428G>A (p.Gly143Glu, rs121912777) polymorphism, a pharmacokinetic study with 75 mg oseltamivir was carried out in c.428G>A carriers and noncarriers. Heterozygous c.428GA carriers (n = 9) had 18% larger values of oseltamivir area under the plasma concentration-time curve from 0 h to infinity (AUC(0-∞)) (P = 0.025) and 23% smaller carboxylate-to-oseltamivir AUC(0-∞) ratio (P = 0.006) than noncarriers (n = 12). This shows that the CES1 c.428G>A polymorphism impairs oseltamivir bioactivation in humans.
- University of Helsinki Finland
- Robert Bosch (Germany) Germany
- University of Tübingen Germany
- Helsinki University Hospital Finland
- EBERHARD KARLS UNIVERSITAET TUEBINGEN Germany
Adult, Male, Polymorphism, Genetic, Dose-Response Relationship, Drug, Genotype, 610, Antiviral Agents, Influenza B virus, Oseltamivir, Influenza A virus, Area Under Curve, Influenza, Human, Humans, Female, Prodrugs, Drug Monitoring, Carboxylic Ester Hydrolases
Adult, Male, Polymorphism, Genetic, Dose-Response Relationship, Drug, Genotype, 610, Antiviral Agents, Influenza B virus, Oseltamivir, Influenza A virus, Area Under Curve, Influenza, Human, Humans, Female, Prodrugs, Drug Monitoring, Carboxylic Ester Hydrolases
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