Search Results - "MURRAY, Bernard"
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Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat
Published in Kidney international (01-08-2014)“…Many xenobiotics including the pharmacoenhancer cobicistat increase serum creatinine by inhibiting its renal active tubular secretion without affecting the…”
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Assessing Pleiotropic Effects of a Mixed-Mode Perpetrator Drug, Rifampicin, by Multiple Endogenous Biomarkers in Dogs
Published in Drug metabolism and disposition (14-02-2024)“…Rifampicin (RIF) is a mixed-mode perpetrator that produces pleiotropic effects on liver cytochrome P450 enzymes and drug transporters. To assess the complex…”
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Key Metabolic Enzymes Involved in Remdesivir Activation in Human Lung Cells
Published in Antimicrobial agents and chemotherapy (17-08-2021)“…Remdesivir (RDV; GS-5734, Veklury), the first FDA-approved antiviral to treat COVID-19, is a single-diastereomer monophosphoramidate prodrug of an adenosine…”
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Regional proteomic quantification of clinically relevant non-cytochrome P450 enzymes along the human small intestine
Published in Drug metabolism and disposition (01-07-2020)“…Current challenges in accurately predicting intestinal metabolism arise from the complex nature of the intestine, leading to limited applicability of available…”
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Comparison of Tissue Abundance of Non-Cytochrome P450 Drug-Metabolizing Enzymes by Quantitative Proteomics between Humans and Laboratory Animal Species
Published in Drug metabolism and disposition (01-03-2022)“…The use of animal pharmacokinetic models as surrogates for humans relies on the assumption that the drug disposition mechanisms are similar between preclinical…”
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Characterization of Differential Tissue Abundance of Major Non-CYP Enzymes in Human
Published in Molecular pharmaceutics (02-11-2020)“…The availability of assays that predict the contribution of cytochrome P450 (CYP) metabolism allows for the design of new chemical entities (NCEs) with minimal…”
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Lenacapavir Exhibits Atropisomerism-Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway
Published in The Journal of pharmacology and experimental therapeutics (18-09-2024)“…Lenacapavir (LEN), a long-acting injectable, is the first approved human immunodeficiency virus type 1 capsid inhibitor and one of a few Food and Drug…”
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Cobicistat Boosts the Intestinal Absorption of Transport Substrates, Including HIV Protease Inhibitors and GS-7340, In Vitro
Published in Antimicrobial Agents and Chemotherapy (01-10-2012)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs
Published in Drug metabolism and disposition (01-10-2023)“…We investigated the effect of variability and instability in aldehyde oxidase (AO) content and activity on the scaling of in vitro metabolism data. AO content…”
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Ontogeny of Human Liver Aldehyde Oxidase: Developmental Changes and Implications for Drug Metabolism
Published in Molecular pharmaceutics (08-05-2024)“…Despite the increasing importance of aldehyde oxidase (AO) in the drug metabolism of clinical candidates, ontogeny data for AO are limited. The objective of…”
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Pharmacokinetics and Disposition of Momelotinib Revealed a Disproportionate Human Metabolite-Resolution for Clinical Development
Published in Drug metabolism and disposition (01-03-2018)“…Momelotinib (MMB), a small-molecule inhibitor of Janus kinase (JAK)1/2 and of activin A receptor type 1 (ACVR1), is in clinical development for the treatment…”
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Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer
Published in ACS medicinal chemistry letters (12-08-2010)“…Cobicistat (3, GS-9350) is a newly discovered, potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes. In contrast to ritonavir, 3 is…”
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Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis
Published in Thrombosis research (01-10-2018)“…Spleen tyrosine kinase (SYK) mediates signal transduction in multiple hematopoietic cells, including platelets. SYK signals downstream of immunoreceptors and…”
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Structure–activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)
Published in Bioorganic & medicinal chemistry letters (01-02-2014)“…A series of novel 1,4-diamine-based CYP3A inhibitors were designed and evaluated. A potent and selective inhibitor of CYP3A, cobicistat (35, GS-9350) was…”
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The Drug–Drug Interaction Profile of Presatovir
Published in Journal of clinical pharmacology (01-06-2018)“…Respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infections in young children. Presatovir (previously GS‐5806) is a novel, orally…”
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Preclinical Characterization of GS-9669, a Thumb Site II Inhibitor of the Hepatitis C Virus NS5B Polymerase
Published in Antimicrobial Agents and Chemotherapy (01-02-2013)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Structure–activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: Core region
Published in Bioorganic & medicinal chemistry letters (01-02-2014)“…The synthesis and evaluation of analogs with extensive modifications of the 1,4-diamine core along with the structure activity relationships with respect to…”
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Discovery of GS-9669, a Thumb Site II Non-Nucleoside Inhibitor of NS5B for the Treatment of Genotype 1 Chronic Hepatitis C Infection
Published in Journal of medicinal chemistry (13-03-2014)“…Investigation of thiophene-2-carboxylic acid HCV NS5B site II inhibitors, guided by measurement of cell culture medium binding, revealed the structure–activity…”
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Identification and characterization of erlotinib as a potent mechanism-based inactivator of human aldehyde oxidase
Published in Drug metabolism and pharmacokinetics (01-04-2024)Get full text
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