ArticleBasic & clinical pharmacology & toxicology2016
Association of Oseltamivir Activation with Gender and Carboxylesterase 1 Genetic Polymorphisms.
Article in Basic & clinical pharmacology & toxicology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 43 citations in OpenAlex.
- Impact of carboxylesterase 1 genetic polymorphism on trandolapril activation in human liver and the pharmacokinetics and pharmacodynamics in healthy volunteers.Clinical and translational science · 2021Trial
- Sex-related differences in blood concentrations and emergence profiles following total intravenous anesthesia with remimazolam and remifentanil.Scientific reports · 2026Observational
- Biological sex differences in pharmacokinetics and adverse drug reactions.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Sex differences in hepatic enzymes and transporters involved in pharmacokinetics.Liver research (Beijing, China) · 2025Review
- Characterization of hydrolase activity in ocular tissues of humans and preclinical species.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Oseltamivir-induced hepatotoxicity: A retrospective analysis of the FDA adverse event reporting system.PloS one · 2025Article
- Pharmacogenetic study of CES1 gene and enalapril efficacy.Journal of applied genetics · 2024Review
- The influence of sex on the dosage of remimazolam co-administered with remifentanil for loss of consciousness in adult patients: an up-and-down sequential allocation trial.BMC anesthesiology · 2024Article
- The Comparative Metabolism of a Novel Hepatocellular Carcinoma Therapeutic Agent, 2,3-Diamino-Metabolites · 2024Article
- Regulation of carboxylesterases and its impact on pharmacokinetics and pharmacodynamics: an up-to-date review.Expert opinion on drug metabolism & toxicology · 2024Review
- Characterisation of AMB-FUBINACA metabolism and CBForensic toxicology · 2023Article
- The Influence of Structural Variants of theGenes · 2022Article
- Influenza antivirals and animal models.FEBS open bio · 2022Review
- The Influence of theJournal of personalized medicine · 2022Article
- Contributions of Cathepsin A and Carboxylesterase 1 to the Hydrolysis of Tenofovir Alafenamide in the Human Liver, and the Effect of CES1 Genetic Variation on Tenofovir Alafenamide Hydrolysis.Drug metabolism and disposition: the biological fate of chemicals · 2022Article
- Transcriptional Regulation of Carboxylesterase 1 in Human Liver: Role of the Nuclear Receptor Subfamily 1 Group H Member 3 and Its Splice Isoforms.Drug metabolism and disposition: the biological fate of chemicals · 2022Article
- Pharmacogenomics Informs Cardiovascular Pharmacotherapy.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Just a Reflection: Does Drug Repurposing Perpetuate Sex-Gender Bias in the Safety Profile?Pharmaceuticals (Basel, Switzerland) · 2021Review
- Pharmacogenomics and COVID-19: clinical implications of human genome interactions with repurposed drugs.The pharmacogenomics journal · 2021Review
- Macrophage imaging and subset analysis using single-cell RNA sequencing.Nanotheranostics · 2021Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
Oseltamivir, an inactive anti-influenza virus prodrug, is activated (hydrolysed) in vivo by carboxylesterase 1 (CES1) to its active metabolite oseltamivir carboxylate. CES1 functions are significantly associated with certain CES1 genetic variants and some non-genetic factors. The purpose of this study was to investigate the effect of gender and several CES1 genetic polymorphisms on oseltamivir activation using a large set of individual human liver samples. CES1-mediated oseltamivir hydrolysis and CES1 genotypes, including the G143E (rs71647871), rs2244613, rs8192935, the -816A>C (rs3785161) and the CES1P1/CES1P1VAR, were determined in 104 individual human livers. The results showed that hepatic CES1 protein expression in females was 17.3% higher than that in males (p = 0.039), while oseltamivir activation rate in the livers from female donors was 27.8% higher than that from males (p = 0.076). As for CES1 genetic polymorphisms, neither CES1 protein expression nor CES1 activity on oseltamivir activation was significantly associated with the rs2244613, rs8192935, -816A>C or CES1P1/CES1P1VAR genotypes. However, oseltamivir hydrolysis in the livers with the genotype 143G/E was approximately 40% of that with the 143G/G genotype (0.7 ± 0.2 versus 1.8 ± 1.1 nmole/mg protein/min, p = 0.005). In summary, the results suggest that hepatic oseltamivir activation appears to be more efficient in females than that in males, and the activation can be impaired by functional CES1 variants, such as the G143E. However, clinical implication of CES1 gender differences and pharmacogenetics in oseltamivir pharmacotherapy warrants further investigations.
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