Metabolism and disposition of lesinurad, a uric acid reabsorption inhibitor, in humans
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DOI: 10.1080/00498254.2018.1504257
Abstract: Abstract The objectives of this study were to determine the absolute bioavailability of lesinurad and to characterized its disposition in humans. The oral bioavailability assessment was performed using a clinical design of simultaneous dosing of… read more here.
Keywords: disposition; lesinurad uric; metabolism disposition; disposition lesinurad ... See more keywords
An in vivo evaluation of the ontogeny of stereoselective fluoxetine metabolism and disposition in lambs from birth to one year of age
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DOI: 10.1080/00498254.2018.1563922
Abstract: Abstract 1. The objective was to determine the ontogeny of stereoselective fluoxetine (FX) disposition in postnatal sheep from newborn to adulthood. 2. Catheters were implanted in a carotid artery and jugular vein. FX was administered… read more here.
Keywords: disposition; metabolism; metabolism disposition; stereoselective fluoxetine ... See more keywords
Metabolism and disposition of the SGLT2 inhibitor bexagliflozin in rats, monkeys and humans
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DOI: 10.1080/00498254.2019.1654634
Abstract: Abstract Bexagliflozin is a C-aryl glucoside inhibitor of human sodium-glucose linked transporter 2 (SGLT2) that undergoes oxidation and glucuronidation to form six principal metabolites in humans. In vitro metabolism by human liver microsomes and recombinant… read more here.
Keywords: monkeys humans; inhibitor; metabolism; bexagliflozin ... See more keywords
Metabolism and disposition in rats, dogs, and humans of erdafitinib, an orally administered potent pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor
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DOI: 10.1080/00498254.2020.1821123
Abstract: Abstract This article describes in vivo biotransformation and disposition of erdafitinib following single oral dose of 3H-erdafitinib and 14C-erdafitinib to intact and bile duct-cannulated (BC) rats (4 mg/kg), 3H-erdafitinib to intact dogs (0.25 mg/kg), and 14C-erdafitinib to… read more here.
Keywords: disposition rats; erdafitinib major; metabolism disposition; rats dogs ... See more keywords
Preclinical pharmacokinetics, metabolism, and disposition of NXE0041178, a novel orally bioavailable agonist of the GPR52 receptor with potential for treatment of schizophrenia and related psychiatric disorders
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DOI: 10.1080/00498254.2025.2501593
Abstract: Abstract The physico-chemical properties, protein binding, metabolism, permeability, transporter interactions, chemical toxicity, and drug-drug interaction potential of the novel GPR52 agonist NXE0041178 were characterised. NXE0041178 demonstrated high cellular permeability, little interaction with efflux transporters P-gp… read more here.
Keywords: pharmacokinetics metabolism; preclinical pharmacokinetics; metabolism; agonist ... See more keywords
The Metabolism and Disposition of Brepocitinib in Humans and Characterization of the Formation Mechanism of an Aminopyridine Metabolite
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DOI: 10.1124/dmd.124.001750
Abstract: Brepocitinib is an oral once-daily Janus kinase 1 and Tyrosine kinase 2 selective inhibitor currently in development for the treatment of several autoimmune disorders. Mass balance and metabolic profiles were determined using accelerator mass spectrometry… read more here.
Keywords: dose; brepocitinib; metabolism; formation ... See more keywords
An integrated approach for studying exposure, metabolism, and disposition of traditional Chinese medicine using PATBS and MDRB tools: a case study of semen Armeniacae Amarum
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DOI: 10.1186/s13020-024-01031-8
Abstract: Deciphering the in vivo processes of traditional Chinese medicine (TCM) is crucial for identifying new pharmacodynamic substances and new drugs. Due to the complexity and diversity of components, investigating the exposure, metabolism, and disposition remains… read more here.
Keywords: exposure metabolism; vivo; medicine; chinese medicine ... See more keywords