Article
Carboxylesterase 1 polymorphism impairs oseltamivir bioactivation in humans.
Clinical pharmacology and therapeutics - 1 Jul 2012
Tarkiainen E K, Backman J T, Neuvonen M, Neuvonen P J, Schwab M, Niemi M
Abstract excerpt
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...
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