432
Views
10
CrossRef citations to date
0
Altmetric
Reviews

The early estimation of circulating drug metabolites in humans

, PhD
Pages 985-997 | Published online: 10 Jun 2012

Bibliography

  • The US FDA. Guidance for Industry: Guideline for the Format and Content of the Nonclinical Pharmacology/Toxicology Section of an Application. Available from: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM079234.pdf 1987
  • Dear GJ, Beaumont C, Roberts A, Approaches for the rapid identification of drug metabolites in early clinical studies. Bioanalysis 2011;3:197-213
  • Smith DA, Dalvie D. Why do metabolites circulate? Xenobiotica 2012;42:107-26
  • Ito K, Iwatsubo T, Kanamitsu S, Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver. Pharmacol Rev 1998;50:387-412
  • Baillie TA, Cayen MN, Fouda H, Drug metabolites in safety testing. Toxicol Appl Pharmacol 2002;182:188-96
  • The US FDA. Guidance for Industry: Safety Testing of Drug Metabolites. Available from: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm079266.pdf 2008
  • ICH M3(R2): Guidance on nonclinical safety studies for the conduct of human clinical trials and marketing authorization for pharmaceuticals. Available from: http://www.ich.org/LOB/media/MEDIA5544.pdf 2009
  • Robison TW, Jacobs A. Metabolites in safety testing. Bioanalysis 2009;1:1193-200
  • Humphreys WG, Unger SE. Safety assessment of drug metabolites: characterization of chemically stable metabolites. Chem Res Toxicol 2006;19:1564-9
  • Smith DA, Obach RS. Metabolites and safety: what are the concerns, and how should we address them? Chem Res Toxicol 2006;19:1570-9
  • Naito S, Furuta S, Yoshida T, Current Opinion: safety evaluation of drug metabolites in development of pharmaceuticals. J Toxicol Sci 2007;32:329-41
  • Leclercq L, Cuyckens F, Mannens GSJ, Which human metabolites have we MIST? Retrospective analysis, practical aspects, and perspectives for metabolite identification and quantification in pharmaceutical development. Chem Res Toxicol 2009;22:280-93
  • Smith DA, Obach RS, Williams DP, Park BK. Clearing the MIST of time: the impact of duration of administration on drug metabolite toxicity. Chem Biol Interact 2009;179:60-7
  • Smith DA, Obach RS. Metabolites in safety testing (MIST): considerations of mechanisms of toxicity with dose, abundance, and duration of treatment. Chem Res Toxicol 2009;22:267-79
  • Walker D, Brady J, Dalvie D, A holistic strategy for characterizing the safety of metabolites through drug discovery and development. Chem Res Toxicol 2009;22:1653-62
  • Gross G, Wilson I. Issues in the safety testing of metabolites. Future Med Chem 2009;1:1381-90
  • Yu H, Bischoff D, Tweedie D. Challenges and solutions to metabolites in safety testing: impact of the International Conference on Harmonization M3(R2) guidance. Expert Opin Drug Metab Toxicol 2010;6:1539-49
  • Anderson S, Knadler MP, Luffer-Atlas D. Overview of metabolite safety testing from an industry perspective. Bioanalysis 2010;2:1249-61
  • Nedderman AN, Wright P. Looking back through the MIST: a perspective of evolving strategies and key focus areas for metabolite safety analysis. Bioanalysis 2010;2:1235-48
  • Frederick CB, Obach RS. Metabolites in safety testing: “MIST” for the clinical pharmacologist. Clin Pharmacol Ther 2010;87:345-50
  • Smith DA, Obach RS. Metabolites: have we MIST out the importance of structure and physicochemistry. Bioanalysis 2010;2:1223-33
  • Nedderman AN, Dear GJ, North S, From definition to implementation: a cross-industry perspective of past, current and future MIST strategies. Xenobiotica 2011;41:605-22
  • Davis-Bruno KL, Atrakchi A. A regulatory perspective on issues and approaches in characterizing human metabolites. Chem Res Toxicol 2006;19:1561-3
  • Atrakchi AH. Interpretation and considerations on the safety evaluation of human drug metabolites. Chem Res Toxicol 2009;22:1217-20
  • Guengerich FP. Safety assessment of stable drug metabolites. Chem Res Toxicol 2006;19:1559-60
  • Baillie TA. Approaches to the safety assessment of stable and chemically reactive drug metabolites in early clinical trials. Chem Res Toxicol 2009;22:263-6
  • Pang KS. Safety testing of metabolites: expectations and outcomes. Chem Biol Interact 2009;179:45-59
  • Obach RS, Nedderman AN, Smith DA. Radiolabelled mass-balance excretion and metabolism studies in laboratory animals: are they still necessary? Xenobiotica 2012;42:46-56
  • Anderson S, Luffer-Atlas D, Knadler MP. Predicting circulating human metabolites: how good are we? Chem Res Toxicol 2009;22:243-56
  • Park KB, Boobis A, Clarke S, Managing the challenge of chemically reactive metabolites in drug development. Nature Reviews Drug Disc 2011;10:292-306
  • Luffer-Atlas D. Unique/major human metabolites: why, how, and when to test for safety in animals. Drug Metab Rev 2008;40:447-63
  • Brodie BB, Gillette JR, La Du BN. Enzymatic metabolism of drugs and other foreign compounds. Annu Rev Biochem 1958;27:427-54
  • Bachmann C, Bickel MH. History of drug metabolism: the first half of the 20th century. Drug Metab Rev 1985;6:185-253
  • Axelrod J. An unexpected life in research. Annu Rev Pharmacol Toxicol 1988;28:1-23
  • Wang WW, Khetani SR, Krzyzewski S, Assessment of a micropatterned hepatocyte coculture system to generate major human excretory and circulating drug metabolites. Drug Metab Dispos 2010;38:1900-5
  • Yun C-Ho, Yim S-K, Kim D-H, Ahn T. Functional expression of human cytochrome P450 enzymes in Escherichia coli. Curr Drug Metab 2006;7:411-29
  • Hamilton RA, Garnett WR, Kline BJ. Determination of mean valproic acid serum level by assay of a single pooled sample. Clin Pharmacol Ther 1981;29:408-13
  • Gao H, Deng S, Obach RS. A simple liquid chromatography-tandem mass spectrometry method to determine relative plasma exposures of drug metabolites across species for metabolite safety assessments. Drug Metab Dispos 2010;38:2147-56
  • Ma S, Li Z, Lee K-J, Chowdhury SK. Determination of exposure multiples of human metabolites for MIST assessment in preclinical safety species without using reference standards or radiolabeled compounds. Chem Res Toxicol 2010;23:1871-3
  • Marathe PH, Shyu WC, Humphreys WC. The use of radiolabeled compounds for ADME studies in discovery and exploratory development. Curr Pharm Design 2004;10:2991-3008
  • Roffey SJ, Obach RS, Gedge JI, Smith DA. What is the objective of the mass balance study? A retrospective analysis of data in animal and human excretion studies employing radiolabeled drugs. Drug Metab Rev 2007;13:17-42
  • Solon EG, Schweitzer A, Stoeckli M, Prideaux B. Autoradiography, MALDI-MS, and SIMS-MS imaging in pharmaceutical discovery and development. AAPS J 2010;12:11-26
  • Prakash C, Shaffer CL, Tremaine LM, Application of liquid chromatography-accelerator mass spectrometry to evaluate the metabolite profiles of a drug candidate in human urine and plasma. Drug Metab Lett 2007;1:226-31
  • Lappin G, Stevens L. Biomedical acceleratory mass spectrometry: recent applications in metabolism and pharmacokinetics. Expert Opin Drug Metab Toxicol 2008;4:1021-33
  • Nedderman A. The use of accelerator MS in support of MIST. Bioanalysis 2011;3:2695-9
  • Cheung C, Gonzalez FJ. Humanized mouse lines and their application for prediction of human drug metabolism and toxicological risk assessment. J Pharmacol Exp Ther 2008;327:288-9
  • Powley MW, Frederick CB, Sistare FD, DeGeorge JJ. Safety assessment of drug metabolites: implications of regulatory guidance and potential application of genetically engineered mouse models that express human P450s. Chem Res Toxicol 2009;22:257-62
  • Tateno C, Yoshizane Y, Saito N, Near completely humanized liver in mice shows human-type metabolic responses to drugs. Am J Pathol 2004;165:901-12
  • Shultz LD, Ishikawa F, Greiner DL. Humanized mice in translational biomedical research. Nat Rev Immunol 2007;7:118-30
  • Azuma H, Paulk N, Ranade A, Robust expansion of human hepatocytes in Fah-/-/Rag2-/-/Il2rg-/- mice. Nat Biotechnol 2007;25:903-10
  • Chen AA, Thomas DK, Ong LL, Humanized mice with ectopic artificial liver tissues. PNAS 2011;108:11842-7
  • Wright P, Miao Z, Shilliday B. Metabolite quantification: detector technology and MIST implications. Bioanalysis 2009;1:831-45
  • Kall MA, Gordon B, Laakso S, Best practices in a tiered approach to metabolite qualification: views and recommendations of the European Bioanalysis Forum. Bioanalysis 2010;2:1185-94
  • The US FDA. Guidance for Industry: Bioanalytical Method Validation. Available from: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM070107.pdf 2001
  • EMA. Draft guideline on validation of bioanalytical methods . Available from http://www.ema.europa.eu/pdfs/human/ewp/19221709en.pdf 2009
  • Tiller PR, Yu S, Bateman KP, Fractional mass filtering as a means to assess circulating metabolites in early human clinical studies. Rapid Commun Mass Spectrom 2008;22:3510-16
  • Zhu P, Tong W, Alton K, Chowdhury S. An accurate-mass-based spectral-averaging isotope-pattern-filtering algorithm for extraction of drug metabolites possessing a distinct isotope pattern from LC-MS data. Anal Chem 2009;81:5910-17
  • Srivastava A, Lian L-Y, Maggs JL, Quantifying the metabolic activation of nevirapine in patients by integrated applications of NMR and mass spectrometries. Drug Metab Dispos 2010;38:122-32
  • Ellis MK, Naylor JL, Green T, Collins MA. Identification and quantification of fluorine-containing metabolites of 1-chloro-2,2,2-trifluoroethane (HCFC133A) in the rat by 19F-NMR spectroscopy. Drug Metab Dispos 1995;3:102-6
  • Dear GJ, Roberts AD, Beaumont C, North SE. Evaluation of preparative high performance liquid chromatography and cryoprobe-nuclear magnetic resonance spectroscopy for the early quantitative estimation of drug metabolites in human plasma. J Chromatogr B Analyst Technol Biomed Life Sci 2008;876:182-90
  • Espina R, Yu L, Wang J, Nuclear magnetic resonance spectroscopy as a quantitative tool to determine the concentrations of biologically produced metabolites: implications in metabolites in safety testing. Chem Res Toxicol 2009;22:299-310
  • Walker GS, Ryder TF, Sharma R, Validation of isolated metabolites from drug metabolism studies as analytical standards by quantitative NMR. Drug Metab Dispos 2011;39:433-40
  • Yu CP, Chen CL, Gorycki FL, Neiss TG. 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. Rapid Commun Mass Spectrom 2007;21:497-502
  • Zhang D, Raghavan N, Chando T, LC-MS/MS-based approach for obtaining exposure estimates of metabolites in early clinical trials using radioactive metabolites as reference standards. Drug Metab Lett 2007;1:293-8
  • Yi P, Luffer-Atlas D. A radiocalibration method with pseudo internal standard to estimate circulating metabolite concentrations. Bioanalysis 2010;2:1195-210
  • Comezoglu SN, Ly VT, Zhang D, Biotransformation profiling of [14C]ixabepilone in human plasma, urine and feces samples using accelerator mass spectrometry (AMS). Drug Metab Pharamacokinet 2009;24:511-22
  • Cuyckens F, Pauwels N, Koppen V, Leclercq L. Use of relative 12C/14C isotope ratios to estimate metabolite concentrations in the absence of authentic standards. Bioanalysis 2012;4:143-56
  • Kola I. The state of innovation in drug development. Clin Pharmacol Ther 2008;83:227-30
  • Prueksaritanont T, Lin JH, Baillie TA. Complicating factors in safety testing of drug metabolites: kinetic differences between generated and preformed metabolites. Toxicol Appl Pharmacol 2006;217:143-52
  • NIH, DARPA and FDA collaborate to develop cutting-edge technologies to predict drug safety. Available from: http://govhealthit.com/press-release/nih-darpa-and-fda-collaborate-develop-cutting-edge-technologies-predict-drug-safety 2011

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.