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- W2157155858 abstract "1. The disposition etamicastat was evaluated in the Cynomolgus monkey after intravenous and oral administration of [14C]-etamicastat. The pharmacokinetics of etamicastat and its N-acetylated metabolite BIA 5-961 were also evaluated in monkeys and dogs.2. In the monkey, 7 days after intravenous and oral administration of [14C]-etamicastat, 76.6–91.1% of the etamicastat-related radioactivity had been excreted mainly in urine. The radioactivity peaked in plasma between 4- and 8-h post-dosing followed by a quick decline and a slow terminal phase (half-life of 68.7 h). The calculated oral bioavailability for etamicastat was 46.1%. Etamicastat was quickly absorbed in monkeys and dogs with a half-life ranging from 5.2 to 9.9 h in monkeys and 6.9 to 11.4 h in dogs over.3. The N-acetylated metabolite of etamicastat, represented 4–7% of the extent of exposure of etamicastat in the monkey, but was not found detectable in dogs. Gender did not influence etamicastat exposure and the concentration versus time curves fitted a dose-dependent pharmacokinetics in the dog, but not in the monkey.4. In conclusion, etamicastat is rapidly absorbed and primarily excreted via urine in monkeys. Similarly, to humans, monkeys, unlike dogs, N-acetylate etamicastat and evidence that etamicastat pharmacokinetics is less than dose proportional." @default.
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- W2157155858 date "2015-04-14" @default.
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- W2157155858 title "Distribution and pharmacokinetics of etamicastat and itsN-acetylated metabolite (BIA 5-961) in dog and monkey" @default.
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- W2157155858 doi "https://doi.org/10.3109/00498254.2015.1024780" @default.
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