Search Results - "Webborn, Peter J. H"
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Mass Spectrometry Imaging in Drug Development
Published in Analytical chemistry (Washington) (03-02-2015)Get full text
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Mass Spectrometry Imaging of Cassette-Dosed Drugs for Higher Throughput Pharmacokinetic and Biodistribution Analysis
Published in Analytical chemistry (Washington) (19-08-2014)“…Cassette dosing of compounds for preclinical drug plasma pharmacokinetic analysis has been shown to be a powerful strategy within the pharmaceutical industry…”
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Actives from MMV Open Access Boxes? A suggested way forward
Published in PLoS pathogens (01-04-2021)“…It is estimated that more than 1 billion people across the world are affected by a neglected tropical disease (NTD) that requires medical intervention. These…”
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Mapping Drug Distribution in Brain Tissue Using Liquid Extraction Surface Analysis Mass Spectrometry Imaging
Published in Analytical chemistry (Washington) (06-10-2015)“…Liquid extraction surface analysis mass spectrometry (LESA-MS) is a surface sampling technique that incorporates liquid extraction from the surface of tissue…”
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Use of Hepatocytes to Assess the Contribution of Hepatic Uptake to Clearance in Vivo
Published in Drug metabolism and disposition (01-06-2007)“…The wealth of information that has emerged in recent years detailing the substrate specificity of hepatic transporters necessitates an investigation into their…”
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Prediction of the Pharmacokinetics of Atorvastatin, Cerivastatin, and Indomethacin Using Kinetic Models Applied to Isolated Rat Hepatocytes
Published in Drug metabolism and disposition (01-07-2008)“…The disposition of atorvastatin, cerivastatin, and indomethacin, established substrates of rat hepatic basolateral uptake transporters, has been evaluated in…”
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Impact of Hepatic Uptake Transporters on Pharmacokinetics and Drug−Drug Interactions: Use of Assays and Models for Decision Making in the Pharmaceutical Industry
Published in Molecular pharmaceutics (07-12-2009)“…The ability to predict hepatic metabolic clearance is a key component in the design and selection of small molecule drug candidates within the pharmaceutical…”
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Hepatic Uptake in the Dog: Comparison of Uptake in Hepatocytes and Human Embryonic Kidney Cells Expressing Dog Organic Anion-Transporting Polypeptide 1B4
Published in Drug metabolism and disposition (01-12-2011)“…Although the dog is frequently used in pharmacological, pharmacokinetic, and drug safety studies, little is known about canine drug transporters. Dog organic…”
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AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis
Published in Proceedings of the National Academy of Sciences - PNAS (22-01-2019)“…Onchocerciasis and lymphatic filariasis are two neglected tropical diseases that together affect ∼157 million people and inflict severe disability. Both…”
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Functional Consequences of Active Hepatic Uptake on Cytochrome P450 Inhibition in Rat and Human Hepatocytes
Published in Drug metabolism and disposition (01-08-2008)“…A series of cytochrome P450 (P450) inhibition experiments were conducted with four hepatic uptake substrates (AZ3, AZ25, atorvastatin, and pitavastatin) using…”
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Spatial Quantitation of Drugs in tissues using Liquid Extraction Surface Analysis Mass Spectrometry Imaging
Published in Scientific reports (24-11-2016)“…Liquid extraction surface analysis mass spectrometry imaging (LESA-MSI) has been shown to be an effective tissue profiling and imaging technique, producing…”
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Design of Helicobacter pylori glutamate racemase inhibitors as selective antibacterial agents: A novel pro-drug approach to increase exposure
Published in Bioorganic & medicinal chemistry (15-08-2008)“…To achieve high bioavailability towards the design of Helicobacter pylori antibacterial drugs, a pro-drug approach was implemented wherein a sulfoxide moiety…”
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Development of Pyrazolopyrimidine Anti-Wolbachia Agents for the Treatment of Filariasis
Published in ACS medicinal chemistry letters (09-09-2021)“…Anti-Wolbachia therapy has been identified as a viable treatment for combating filarial diseases. Phenotypic screening revealed a series of pyrazolopyrimidine…”
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The right compound in the right assay at the right time: an integrated discovery DMPK strategy
Published in Drug metabolism reviews (01-08-2012)“…The high rate of attrition during drug development and its associated high research and development (R&D) cost have put pressure on pharmaceutical companies to…”
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Future directions of imaging MS in pharmaceutical R&D
Published in Bioanalysis (01-01-2015)“…MS imaging has rapidly evolved over the last decade, finding roles in all aspects of pharmaceutical research and development. This article discusses possible…”
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From ATP to AZD6140 : The discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis
Published in Bioorganic & medicinal chemistry letters (01-11-2007)“…Starting from adenosine triphosphate (ATP), the identification of a novel series of P2Y(12) receptor antagonists and exploitation of their SAR is described…”
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The role of pharmacokinetic studies in drug discovery: where are we now, how did we get here and where are we going?
Published in Future medicinal chemistry (01-07-2014)Get more information
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Robust Assessment of Statistical Significance in the Use of Unbound/Intrinsic Pharmacokinetic Parameters in Quantitative StructureâPharmacokinetic Relationships with Lipophilicity
Published in Drug metabolism and disposition (01-02-2000)“…The optimization of pharmacokinetic properties remains one of the most challenging aspects of drug design. Key parameters, clearance and volume of…”
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Drug-phospholipid interactions. 2. Predicting the sites of drug distribution using n-octanol/water and membrane/water distribution coefficients
Published in Journal of pharmaceutical sciences (01-09-1997)“…The in vivo tissue distribution of seventeen drugs has been modeled by using estimated n-octanol/water and membrane/water distribution coefficients. In this…”
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