The early estimation of circulating drug metabolites in humans

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Expert Opinion on Drug Metabolism & Toxicology

• Publication date

  2012-07-18

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1517/17425255.2012.693159PMID 22681256
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Radiolabelled mass-balance excretion and metabolism studies in laboratory animals: are they still necessary?

  2012cited by this paper
• Why do metabolites circulate?

  2012cited by this paper
• Use of relative 12C/14C isotope ratios to estimate metabolite concentrations in the absence of authentic standards.

  2012cited by this paper
• From definition to implementation: a cross-industry perspective of past, current and future MIST strategies

  2011cited by this paper
• Humanized mice with ectopic artificial liver tissues

  2011cited by this paper
• Validation of Isolated Metabolites from Drug Metabolism Studies as Analytical Standards by Quantitative NMR

  2011cited by this paper
• Managing the challenge of chemically reactive metabolites in drug development

  2011cited by this paper
• Workshop/conference report on EMA draft guideline on validation of bioanalytical methods.

  2011cited by this paper
• Approaches for the rapid identification of drug metabolites in early clinical studies.

  2011cited by this paper
• The use of accelerator MS in support of MIST.

  2011cited by this paper
• Looking back through the MIST: a perspective of evolving strategies and key focus areas for metabolite safety analysis.

  2010cited by this paper
• A radiocalibration method with pseudo internal standard to estimate circulating metabolite concentrations.

  2010cited by this paper
• Assessment of a Micropatterned Hepatocyte Coculture System to Generate Major Human Excretory and Circulating Drug Metabolites

  2010cited by this paper
• Determination of exposure multiples of human metabolites for MIST assessment in preclinical safety species without using reference standards or radiolabeled compounds.

  2010cited by this paper
• A Simple Liquid Chromatography-Tandem Mass Spectrometry Method to Determine Relative Plasma Exposures of Drug Metabolites across Species for Metabolite Safety Assessments

  2010cited by this paper
• Metabolites in Safety Testing: “MIST” for the Clinical Pharmacologist

  2010cited by this paper
• Quantifying the Metabolic Activation of Nevirapine in Patients by Integrated Applications of NMR and Mass Spectrometries

  2010cited by this paper
• Metabolites: have we MIST out the importance of structure and physicochemistry?

  2010cited by this paper
• Autoradiography, MALDI-MS, and SIMS-MS Imaging in Pharmaceutical Discovery and Development

  2010cited by this paper
• Overview of metabolite safety testing from an industry perspective.

  2010cited by this paper
• Best practices in a tiered approach to metabolite quantification: views and recommendations of the European Bioanalysis Forum.

  2010cited by this paper
• Challenges and solutions to metabolites in safety testing: impact of the International Conference on Harmonization M3(R2) guidance

  2010cited by this paper
• Bioanalytical method validation: notable points in the 2009 draft EMA Guideline and differences with the 2001 FDA Guidance.

  2010cited by this paper
• Clearing the MIST (metabolites in safety testing) of time: The impact of duration of administration on drug metabolite toxicity.

  2009cited by this paper
• Metabolite quantitation: detector technology and MIST implications.

  2009cited by this paper
• Nuclear magnetic resonance spectroscopy as a quantitative tool to determine the concentrations of biologically produced metabolites: implications in metabolites in safety testing.

  2009cited by this paper
• Biotransformation profiling of [(14)C]ixabepilone in human plasma, urine and feces samples using accelerator mass spectrometry (AMS).

  2009cited by this paper
• Safety testing of metabolites: Expectations and outcomes.

  2009cited by this paper
• Interpretation and considerations on the safety evaluation of human drug metabolites.

  2009cited by this paper
• An accurate-mass-based spectral-averaging isotope-pattern-filtering algorithm for extraction of drug metabolites possessing a distinct isotope pattern from LC-MS data.

  2009cited by this paper
• Metabolites in safety testing (MIST): considerations of mechanisms of toxicity with dose, abundance, and duration of treatment.

  2009cited by this paper
• Issues in the safety testing of metabolites.

  2009cited by this paper
• Metabolites in safety testing.

  2009cited by this paper
• A holistic strategy for characterizing the safety of metabolites through drug discovery and development.

  2009cited by this paper
• Safety assessment of drug metabolites: implications of regulatory guidance and potential application of genetically engineered mouse models that express human P450s.

  2009cited by this paper
• Which human metabolites have we MIST? Retrospective analysis, practical aspects, and perspectives for metabolite identification and quantification in pharmaceutical development.

  2009cited by this paper
• Approaches to the assessment of stable and chemically reactive drug metabolites in early clinical trials.

  2009cited by this paper
• Predicting circulating human metabolites: how good are we?

  2009cited by this paper
• The State of Innovation in Drug Development

  2008cited by this paper
• Fractional mass filtering as a means to assess circulating metabolites in early human clinical studies.

  2008cited by this paper
• Evaluation of preparative high performance liquid chromatography and cryoprobe-nuclear magnetic resonance spectroscopy for the early quantitative estimation of drug metabolites in human plasma.

  2008cited by this paper
• Humanized Mouse Lines and Their Application for Prediction of Human Drug Metabolism and Toxicological Risk Assessment

  2008cited by this paper
• Unique/major human metabolites: why, how, and when to test for safety in animals.

  2008cited by this paper
• Biomedical accelerator mass spectrometry: recent applications in metabolism and pharmacokinetics

  2008cited by this paper
• Unique/Major Human Metabolites: Why, How, and When to Test for Safety in Animals

  2008cited by this paper
• Application of liquid chromatography-accelerator mass spectrometry (LC-AMS) to evaluate the metabolic profiles of a drug candidate in human urine and plasma.

  2007cited by this paper
• What is the Objective of the Mass Balance Study? A Retrospective Analysis of Data in Animal and Human Excretion Studies Employing Radiolabeled Drugs

  2007cited by this paper
• Robust expansion of human hepatocytes in Fah−/−/Rag2−/−/Il2rg−/− mice

  2007cited by this paper
• Humanized mice in translational biomedical research

  2007cited by this paper
• LC-MS/MS-based approach for obtaining exposure estimates of metabolites in early clinical trials using radioactive metabolites as reference standards.

  2007cited by this paper
• Current opinion: safety evaluation of drug metabolites in development of pharmaceuticals.

  2007cited by this paper
• A rapid method for quantitatively estimating metabolites in human plasma in the absence of synthetic standards using a combination of liquid chromatography/mass spectrometry and radiometric detection.

  2007cited by this paper
• Metabolites and safety: What are the concerns, and how should we address them?

  2006cited by this paper
• Safety assessment of drug metabolites: Characterization of chemically stable metabolites.

  2006cited by this paper
• A regulatory perspective on issues and approaches in characterizing human metabolites.

  2006cited by this paper
• Complicating factors in safety testing of drug metabolites: kinetic differences between generated and preformed metabolites.

  2006cited by this paper
• Functional expression of human cytochrome P450 enzymes in Escherichia coli.

  2006cited by this paper
• Safety Assessment of Stable Drug Metabolites

  2006cited by this paper
• Near completely humanized liver in mice shows human-type metabolic responses to drugs.

  2004cited by this paper
• The use of radiolabeled compounds for ADME studies in discovery and exploratory development.

  2004cited by this paper
• Drug metabolites in safety testing.

  2002cited by this paper
• Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver.

  1998cited by this paper
• Identification and quantification of fluorine-containing metabolites of 1-chloro-2,2,2-trifluoroethane (HCFC133A) in the rat by 19F-NMR spectroscopy.

  1995cited by this paper
• Application of Liquid Chromatography ‐ Mass Spectrometry.

  1994cited by this paper
• An unexpected life in research.

  1988cited by this paper
• History of drug metabolism: the first half of the 20th century.

  1985cited by this paper
• Determination of mean valproic acid serum level by assay of a single pooled sample

  1981cited by this paper
• Enzymatic metabolism of drugs and other foreign compounds.

  1958cited by this paper

• A MIST conception: what has been learned from twenty years of human metabolite safety assessment?

  2023cites this paper
• A decade of drug metabolite safety testing: industry and regulatory shared learning

  2017cites this paper
• Standard-Free Bioanalytical Approach for Absolute Quantitation of Drug Metabolites Utilizing Biosynthesis of Reciprocal Radio and Stable Isotopologues and Its Application.

  2017cites this paper
• Metabolism and Bioactivation of Fluorochloridone, a Novel Selective Herbicide, in Vivo and in Vitro.

  2016cites this paper
• Database extraction of metabolite information of drug candidates: Analysis of 27 AstraZeneca compounds with human ADME data

  2016cites this paper
• A Pharmacokinetic Modeling Approach to Predict the Contribution of Active Metabolites to Human Efficacious Dose

  2016cites this paper
• Database Extraction of Metabolite Information of Drug Candidates: Analysis of 27 AstraZeneca Compounds with Human Absorption, Distribution, Metabolism, and Excretion Data

  2016cites this paper
• Pragmatic approaches to determine the exposures of drug metabolites in preclinical and clinical subjects in the MIST evaluation of the clinical development phase.

  2014cites this paper
• The debate on animal ADME studies in drug development: an update

  2014cites this paper
• Systemic Exposure to the Metabolites of Lesogaberan in Humans and Animals: A Case Study of Metabolites in Safety Testing

  2014influential citation