Human mass balance, pharmacokinetics and metabolism of rovatirelin and identification of its metabolic enzymes in vitro
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DOI: 10.1080/00498254.2019.1580796
Abstract: Abstract The mass balance, pharmacokinetics and metabolism of rovatirelin were characterised in healthy male subjects after a single oral dose of [14C]rovatirelin. [14C]Rovatirelin was steadily absorbed, and the peak concentrations of radioactivity and rovatirelin were… read more here.
Keywords: balance pharmacokinetics; rovatirelin; mass balance; metabolic enzymes ... See more keywords
Pharmacokinetics and metabolism of brexpiprazole, a novel serotonin-dopamine activity modulator and its main metabolite in rat, monkey and human
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DOI: 10.1080/00498254.2021.1890275
Abstract: Abstract The pharmacokinetics of brexpiprazole were investigated in the in vitro and in vivo. The total body clearance of brexpiprazole in rat and monkey was 2.32 and 0.326 L/h/kg, respectively, after intravenous administration, and oral availability… read more here.
Keywords: metabolism; rat monkey; main metabolite; pharmacokinetics metabolism ... See more keywords
Pharmacokinetics, metabolism and off-target effects in the rat of 8-[(1H- benzotriazol-1-yl)amino]octanoic acid, a selective inhibitor of human cytochrome P450 4Z1: β-oxidation as a potential augmenting pathway for inhibition
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DOI: 10.1080/00498254.2021.1930281
Abstract: Abstract 8‐[(1H‐1,2,3‐benzotriazol‐1‐yl)amino]octanoic acid (8-BOA) was recently identified as a selective and potent mechanism-based inactivator (MBI) of breast cancer-associated CYP4Z1 and exhibited favourable inhibitory activity in vitro, thus meriting in vivo characterization. The pharmacokinetics and metabolism… read more here.
Keywords: metabolism; amino octanoic; target; benzotriazol amino ... See more keywords
Pharmacokinetics and metabolism of mirogabalin, a novel α2δ ligand, in rats and monkeys
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DOI: 10.1080/00498254.2022.2049396
Abstract: Abstract The purpose of this study was to investigate the pharmacokinetic behaviour of mirogabalin in rats and monkeys. Pharmacokinetic parameters of mirogabalin after its oral and intravenous administration were determined. Distribution study, mass balance study,… read more here.
Keywords: rats monkeys; mirogabalin; metabolism mirogabalin; oral administration ... See more keywords
Pharmacokinetics, metabolism and excretion of radiolabeled fostemsavir administered with or without ritonavir in healthy male subjects
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DOI: 10.1080/00498254.2022.2119179
Abstract: Abstract The pharmacokinetics, elimination, and metabolism of fostemsavir (FTR), a prodrug of the HIV-1 attachment inhibitor temsavir (TMR), were investigated in healthy volunteers. FTR was administered with and without ritonavir (RTV), a protease inhibitor previously… read more here.
Keywords: metabolism; administered without; tmr; without ritonavir ... See more keywords