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  • Title: Metabolism of the influenza neuraminidase inhibitor prodrug oseltamivir in the rat.
    Author: Sweeny DJ, Lynch G, Bidgood AM, Lew W, Wang KY, Cundy KC.
    Journal: Drug Metab Dispos; 2000 Jul; 28(7):737-41. PubMed ID: 10859145.
    Abstract:
    The metabolism of [2-acetyl-(14)C]oseltamivir (GS4104, Ro 64-0796), the prodrug of the novel influenza neuraminidase inhibitor GS4071 (Ro 64-0802), was examined in rats after oral dosing. Intact oseltamivir was observed only in lung and urine, accounting for 37 and 15% of the total radioactivity in these samples, respectively. GS4071 was the major metabolite in plasma, tissues, and urine, and accounted for 32 to 56% of the radioactivity present in these samples. The second most abundant peak in these samples (13-24% of radioactivity) was a novel metabolite (M3). This metabolite was purified from urine of rats dosed orally with oseltamivir and was identified by liquid chromatography-mass spectrometry and NMR as the (R)-omega-carboxylic acid metabolite of oseltamivir. The omega-carboxylic acid metabolite of oseltamivir could not be produced in vitro. However, omega-hydroxylated products of oseltamivir were produced by rat liver microsomes. Both the (R)- and (S)-omega-hydroxylated products were observed, but formation of the (R)-isomer predominated. These data indicated that in the rat, oseltamivir was primarily metabolized to the active influenza neuraminidase inhibitor GS4071 and, to a lesser extent, to an (R)-omega-carboxylic acid metabolite.
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