Search Results - "WONG, Simon G"
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Prediction of drug-drug interactions arising from mechanism-based inactivation: key input parameters and impact on risk assessment
Published in Current drug metabolism (01-11-2011)“…As the prevalence of polypharmacy increases with our aging population, the propensity for adverse drug-drug interactions arising from the altered metabolism of…”
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An Inhibitory Metabolite Leads to Dose- and Time-Dependent Pharmacokinetics of (R)-N-{1-[3-(4-Ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in Human Subjects After Multiple Dosing
Published in Drug metabolism and disposition (01-03-2009)“…( R )- N -{1-[3-(4-Ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3- d ]-pyrimidin-2-yl]-ethyl}- N -pyridin-3-yl-methyl-2-(4-trifluoromethoxyphenyl)-acetamide (AMG…”
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Considerations from the Innovation and Quality Induction Working Group in Response to Drug-Drug Interaction Guidance from Regulatory Agencies: Guidelines on Model Fitting and Recommendations on Time Course for In Vitro Cytochrome P450 Induction Studies Including Impact on Drug Interaction Risk Assessment
Published in Drug metabolism and disposition (01-01-2021)“…Translational and ADME Sciences Leadership Group Induction Working Group (IWG) presents an analysis on the time course for cytochrome P450 induction in primary…”
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Development of a mass spectrometry-based tryptophan 2, 3-dioxygenase assay using liver cytosol from multiple species
Published in Analytical biochemistry (01-09-2018)“…A novel and rapid method to determine the potency of inhibitors for tryptophan 2, 3-dioxygenase (TDO2) activities in human and preclinical species was…”
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Discovery and in Vivo Evaluation of Macrocyclic Mcl‑1 Inhibitors Featuring an α‑Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere
Published in Journal of medicinal chemistry (27-11-2019)“…Overexpression of the antiapoptotic protein Mcl-1 provides a survival advantage to some cancer cells, making inhibition of this protein an attractive…”
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Single concentration loss of activity assay provides an improved assessment of drug-drug interaction risk compared to IC50-shift
Published in Xenobiotica (01-11-2016)“…1. The utility of two abbreviated, higher-throughput assays [IC50-shift and the loss of activity (LOA) assay] to evaluate time-dependent inhibition (TDI) of 24…”
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Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme
Published in Drug metabolism and disposition (01-07-2012)“…CYP3A4-mediated biotransformation of…”
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Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP
Published in Bioorganic & medicinal chemistry letters (01-07-2014)“…Based on their structural similarity to previously described compound AMG 009, indole-phenyl acetic acids were proposed to be potent dual inhibitors of…”
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Bioactivation of a Novel 2-Methylindole-Containing Dual Chemoattractant Receptor-Homologous Molecule Expressed on T-Helper Type-2 Cells/D-Prostanoid Receptor Antagonist Leads to Mechanism-Based CYP3A Inactivation: Glutathione Adduct Characterization and Prediction of In Vivo Drug-Drug Interaction
Published in Drug metabolism and disposition (01-05-2010)“…The 2-methyl substituted indole, 2MI [2-(4-(4-(2,4-dichlorophenylsulfonamido)-2-methyl-1H-indol-5-yloxy)-3-methoxyphenyl)acetic acid] is a potent dual…”
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Isolation of regioisomers of N-alkylprotoporphyrin IX from chick embryo liver after treatment with porphyrinogenic xenobiotics
Published in Canadian journal of physiology and pharmacology (01-09-2001)“…Several porphyrinogenic xenobiotics cause mechanism-based inactivation of cytochrome P450 (P450) isozymes with concomitant formation of a mixture of four…”
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Use of recombinant human ferrochelatase as a sensitive bioassay for N-alkylprotoporphyrin IX formed after interaction of porphyrinogenic xenobiotics with rat liver microsomes
Published in Canadian journal of physiology and pharmacology (01-07-2000)“…Several porphyrinogenic xenobiotics elicit mechanism-based inactivation of cytochrome P450 (CYP) isozymes, leading to the formation of N-alkylprotoporphyrin IX…”
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An Inhibitory Metabolite Leads to Dose-and Time-Dependent Pharmacokinetics of (R)-A/-{1-[3-(4-Ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in Human Subjects After Multiple Dosing
Published in Drug metabolism and disposition (2009)Get full text
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Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD sub(2) receptors CRTH2 and DP
Published in Bioorganic & medicinal chemistry letters (01-07-2014)“…Based on their structural similarity to previously described compound AMG 009, indole-phenyl acetic acids were proposed to be potent dual inhibitors of…”
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14
The role of mitochondrial injury in bromobenzene and furosemide induced hepatotoxicity
Published in Toxicology letters (16-08-2000)“…Bromobenzene (BB) and furosemide (FS) are two hepatotoxicants whose bioactivation to reactive intermediates is crucial to the development of liver injury…”
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Cytochrome CYP Sources of N-Alkylprotoporphyrin IX after Administration of Porphyrinogenic Xenobiotics to Rats
Published in Drug metabolism and disposition (01-09-1999)“…Cytochrome P-450 (CYP) 3A2 and CYP2C11 are sources of 70 and 30%, respectively, of N- vinylprotoporphyrin IX ( N -vinylPP) formation after administration of…”
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Neutron Reflection from 2,4-Bis(4-(N-methyl-N-octylamino)phenyl)squaraine at the Air−Water Interface and the Linear and Nonlinear Optical Properties of Its Langmuir−Blodgett and Spun-Coated Films
Published in Langmuir (19-03-1997)“…Neutron specular reflection has been used to probe the structure of monolayer films of an anilino squaraine, 2,4-bis(4-(N-methyl-N-octylamino)phenyl)squaraine,…”
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