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Research Article

Unique/Major Human Metabolites: Why, How, and When to Test for Safety in Animals

Pages 447-463 | Published online: 09 Oct 2008

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Ivanna Hrynchak, Emília Sousa, Madalena Pinto & Vera Marisa Costa. (2017) The importance of drug metabolites synthesis: the case-study of cardiotoxic anticancer drugs. Drug Metabolism Reviews 49:2, pages 158-196.
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Mario Pellegatti. (2014) The debate on animal ADME studies in drug development: an update. Expert Opinion on Drug Metabolism & Toxicology 10:12, pages 1615-1620.
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Debra Luffer-Atlas. (2012) The early estimation of circulating drug metabolites in humans. Expert Opinion on Drug Metabolism & Toxicology 8:8, pages 985-997.
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Mario Pellegatti. (2012) Preclinical in vivo ADME studies in drug development: a critical review. Expert Opinion on Drug Metabolism & Toxicology 8:2, pages 161-172.
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Articles from other publishers (27)

Jennifer Lang, Ludwig Vincent, Marylore Chenel, Kayode Ogungbenro & Aleksandra Galetin. (2020) Simultaneous Ivabradine Parent-Metabolite PBPK/PD Modelling Using a Bayesian Estimation Method. The AAPS Journal 22:6.
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Andreu Bofill, Xavier Jalencas, Tudor I. Oprea & Jordi Mestres. (2019) The human endogenous metabolome as a pharmacology baseline for drug discovery. Drug Discovery Today 24:9, pages 1806-1820.
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Thomas A. Baillie. 2015. New Horizons in Predictive Drug Metabolism and Pharmacokinetics. New Horizons in Predictive Drug Metabolism and Pharmacokinetics 202 226 .
Jan Kiebist, Wolfgang Holla, Johannes Heidrich, Marzena Poraj-Kobielska, Martin Sandvoss, Reiner Simonis, Glenn Gröbe, Jens Atzrodt, Martin Hofrichter & Katrin Scheibner. (2015) One-pot synthesis of human metabolites of SAR548304 by fungal peroxygenases. Bioorganic & Medicinal Chemistry 23:15, pages 4324-4332.
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Raman Sharma, John Litchfield, Karen Atkinson, Heather Eng, Neeta B. Amin, William S. Denney, John C. Pettersen, Theunis C. Goosen, Li Di, Esther Lee, Jeffrey A. Pfefferkorn, Deepak K. Dalvie & Amit S. Kalgutkar. (2014) Metabolites in Safety Testing Assessment in Early Clinical Development: A Case Study with a Glucokinase Activator. Drug Metabolism and Disposition 42:11, pages 1926-1939.
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Natalie D. Glube & Guus Duchateau. 2014. Drug Metabolism Prediction. Drug Metabolism Prediction 413 440 .
Ann Aurell Holmberg, Anja Ekdahl & Lars Weidolf. (2014) Systemic Exposure to the Metabolites of Lesogaberan in Humans and Animals: A Case Study of Metabolites in Safety Testing. Drug Metabolism and Disposition 42:6, pages 1016-1021.
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Marzena Poraj-Kobielska, Jens Atzrodt, Wolfgang Holla, Martin Sandvoss, Glenn Gröbe, Katrin Scheibner & Martin Hofrichter. (2013) Preparation of labeled human drug metabolites and drug-drug interaction-probes with fungal peroxygenases. Journal of Labelled Compounds and Radiopharmaceuticals 56:9-10, pages 513-519.
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Angela Dudda & Gert Ulrich Kuerzel. 2013. Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays. Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays 1053 1094 .
Hongying Gao & R. Scott Obach. (2012) A Simple Liquid Chromatography-Tandem Mass Spectrometry Method to Determine Relative Plasma Exposures of Drug Metabolites across Species for Metabolite Safety Assessments (Metabolites in Safety Testing). II. Application to Unstable Metabolites. Drug Metabolism and Disposition 40:7, pages 1290-1296.
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Rajinder Bhardwaj & Gamini Chandrasena. 2012. ADME‐Enabling Technologies in Drug Design and Development. ADME‐Enabling Technologies in Drug Design and Development 15 28 .
Alexander V. LyubimovShelby Anderson, Debra Luffer‐Atlas & Mary Pat Knadler. 2011. Encyclopedia of Drug Metabolism and Interactions. Encyclopedia of Drug Metabolism and Interactions 1 27 .
Alexander V. LyubimovThomas A. Baillie. 2011. Encyclopedia of Drug Metabolism and Interactions. Encyclopedia of Drug Metabolism and Interactions 1 24 .
Gordon J Dear, Claire Beaumont, Andrew Roberts, Bianca Squillaci, Steve Thomas, Mike Nash & Donna Fraser. (2011) Approaches for the rapid identification of drug metabolites in early clinical studies. Bioanalysis 3:2, pages 197-213.
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Takashi Izumi. (2011) Assessment of Drug Metabolites. Drug Metabolism and Pharmacokinetics 26:2, pages 121-122.
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Ulrich Kuerzel, Volker Krone, Manfred Zimmer & Gareth Shackleton. 2011. Drug Discovery and Evaluation: Methods in Clinical Pharmacology. Drug Discovery and Evaluation: Methods in Clinical Pharmacology 73 103 .
J. Greg Slatter. 2010. Biotransformation and Metabolite Elucidation of Xenobiotics. Biotransformation and Metabolite Elucidation of Xenobiotics 295 312 .
Ping Yi & Debra Luffer-Atlas. (2010) A radiocalibration method with pseudo internal standard to estimate circulating metabolite concentrations. Bioanalysis 2:7, pages 1195-1210.
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Shelby Anderson, Mary Pat Knadler & Debra Luffer-Atlas. (2010) Overview of metabolite safety testing from an industry perspective. Bioanalysis 2:7, pages 1249-1261.
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Gerhard GrossIan Wilson. (2009) Issues in the safety testing of metabolites. Future Medicinal Chemistry 1:8, pages 1381-1390.
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Pat WrightZhuang MiaoBarclay Shilliday. (2009) Metabolite quantitation: detector technology and MIST implications. Bioanalysis 1:4, pages 831-845.
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Mingshe Zhu, Donglu Zhang, Haiying Zhang & Wen Chyi Shyu. (2009) Integrated strategies for assessment of metabolite exposure in humans during drug development: analytical challenges and clinical development considerations. Biopharmaceutics & Drug Disposition 30:4, pages 163-184.
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Thomas A. Baillie. (2009) Approaches to the Assessment of Stable and Chemically Reactive Drug Metabolites in Early Clinical Trials. Chemical Research in Toxicology 22:2, pages 263-266.
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Mark W. Powley, Clay B. Frederick, Frank D. Sistare & Joseph J. DeGeorge. (2009) Safety Assessment of Drug Metabolites: Implications of Regulatory Guidance and Potential Application of Genetically Engineered Mouse Models that Express Human P450s. Chemical Research in Toxicology 22:2, pages 257-262.
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Shelby Anderson, Debra Luffer-Atlas & Mary Pat Knadler. (2009) Predicting Circulating Human Metabolites: How Good Are We?. Chemical Research in Toxicology 22:2, pages 243-256.
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Thomas N. Thompson. 2009. Annual Reports in Medicinal Chemistry Volume 44. Annual Reports in Medicinal Chemistry Volume 44 459 474 .
G.J. Dear, A.D. Roberts, C. Beaumont & S.E. North. (2008) Evaluation of preparative high performance liquid chromatography and cryoprobe-nuclear magnetic resonance spectroscopy for the early quantitative estimation of drug metabolites in human plasma. Journal of Chromatography B 876:2, pages 182-190.
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