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

References

• Anderson S, Luffer-Atlas D, Knadler MP. (2009). Predicting circulating human metabolites: How good are we? Chem Res Toxicol 22:243–256.
   PubMed Web of Science ®Google Scholar
• Baillie TA, Cayen MN, Fouda H, Gerson RJ, Green JD, Grossman SJ, Klunk LJ, LeBlanc B, Perkins DG, Shipley LA. (2002). Drug metabolites in safety testing. Toxicol Appl Pharmacol 182:188–196.
   PubMed Web of Science ®Google Scholar
• Balani SK, Xu X, Pratha V, Koss MA, Amin RD, Dufresne C, Miller RR, Arison BH, Doss GA, Chiba M, Freeman A, Holland SD, Schwartz JI, Lasseter KC, Gertz BJ, Isenberg JI, Rogers JD, Lin JH, Baillie TA. (1997). Metabolic profiles of montelukast sodium (Singulair), a potent cysteinyl leukotriene1 receptor antagonist, in human plasma and bile. Drug Metab Dispos 25:1282–1287.
   PubMed Web of Science ®Google Scholar
• Cömezoglu SN, Ly VT, Zhang D, Humphreys WG, Bonacorsi SJ, Everett DW, Cohen MB, Gan J, Beumer JH, Beijnen JH, Schellens HM, Lappin G. (2009). Biotransformation profiling of [(14)C]ixabepilone in human plasma, urine and feces samples using accelerator mass spectrometry (AMS). Drug Metab Pharmacokinet 24:511–522.
   PubMed Web of Science ®Google Scholar
• Dalvie D, Obach RS, Kang P, Prakash C, Loi CM, Hurst S, Nedderman A, Goulet L, Smith E, Bu HZ, Smith DA. (2009). Assessment of three human in vitro systems in the generation of major human excretory and circulating metabolites. Chem Res Toxicol 22:357–368.
   PubMed Web of Science ®Google Scholar
• Dear GJ, Roberts AD, Beaumont C, North SE. (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. J Chromatogr B Analyt Technol Biomed Life Sci 876:182–190.
   PubMed Web of Science ®Google Scholar
• Dobo KL, Obach RS, Luffer-Atlas D, Bercu JP. (2009). A strategy for the risk assessment of human genotoxic metabolites. Chem Res Toxicol 22:348–356.
   PubMed Web of Science ®Google Scholar
• Dow J, Piriou F, Wolf E, Dulery BD, Haegele KD. (1994). Novel carbamate metabolites of mofegiline, a primary amine monoamine oxidase B inhibitor, in dogs and humans. Drug Metab Dispos 22:738–749.
   PubMedGoogle Scholar
• Erve JC. (2008). Cyclic metabolites: Chemical and biological considerations. Curr Drug Metab 9:175–188.
   PubMedGoogle Scholar
• Espina R, Yu L, Wang J, Tong Z, Vashishtha S, Talaat R, Scatina J, Mutlib A. (2009). 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 22:299–310.
   PubMed Web of Science ®Google Scholar
• Gao H, Deng S, Obach RS. (2010). 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 38:2147–2156.
   PubMed Web of Science ®Google Scholar
• Guengerich FP. (2001). Uncommon P450-catalyzed reactions. Curr Drug Metab 2:93–115.
   PubMed Web of Science ®Google Scholar
• Guiney WJ, Beaumont C, Thomas SR. (2010). Use of the entero-test, a novel approach for the noninvasive capture of biliary metabolites in dogs. Drug Metab Dispos 38:851–856.
   PubMed Web of Science ®Google Scholar
• International Conference on Harmonization. (2009) M3(R2): Guidance on Non-Clinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorization for Pharmaceuticals Available at: http://private.ich.org/cache/compo/502-272-1.html Accessed February 5, 2011.
   Google Scholar
• Kall MA, GordonB, Laakso S, Freisleben A, Hucker R, Fischmann S, Globig S, Sennbro C-J, Jansat JM, Mulder H, Thomas E, Brundy-Kloeppel M, Luedtke S, Knutsson M, Pusecker K, White SA, Lausecker B, Mokrzycki-Issartel N, Romero F, Anderson MP, Knebel N, de Zwart M, Schmidt D, van Amsterdam P, Abbott R, Boulanger P, Timmerman P. (2010). Best practices in a tiered approach to metabolite quantification: Views and recommendations of the European Bioanalysis Forum. Bioanalysis 2:1185–1194.
   PubMedGoogle Scholar
• Lappin G, Seymour M. (2010). Addressing metabolite safety during first-in-man studies using 14C-labeled drug and accelerator mass spectrometry. Bioanalysis 2:1315–1324.
   PubMed Web of Science ®Google Scholar
• Leclercq L, Cuyckens F, Mannens GS, de Vries R, Timmerman P, Evans DC. (2009). Which human metabolites have we MIST? Retrospective analysis, practical aspects, and perspectives for metabolite identification and quantification in pharmaceutical development. Chem Res Toxicol 22:280–293.
   PubMed Web of Science ®Google Scholar
• Ma S, Li Z, Lee K-J, Chowdhury SK. (2010). Determination of exposure multiples of human metabolites for mist assessment in preclinical safety species without using reference standards or radiolabeled compounds. Chem Res Toxicol 23:1871–1873.
   PubMed Web of Science ®Google Scholar
• Nedderman AN, Dear GJ, North S, Obach RS, Higton D. (2011). From definition to implementation: A cross-industry perspective of past, current and future MIST strategies. Xenobiotica 41:605–622.
   PubMed Web of Science ®Google Scholar
• Mutlib A, Espina R, Vishwanathan K, Babalola K, Chen Z, Dehnhardt C, Venkatesan A, Mansour T, Chaudhary I, Talaat R, Scatina J. (2011). Application of quantitative NMR in pharmacological evaluation of biologically generated metabolites: implications in drug discovery. Drug Metab Dispos 39:106–116.
   PubMed Web of Science ®Google Scholar
• Prakash C, Shaffer CL, Nedderman A. (2007). Analytical strategies for identifying drug metabolites. Mass Spectrom Rev 26:340–369.
   PubMed Web of Science ®Google Scholar
• Parkinson A, Oglivie BW. (2008). Biotransformation of xenobiotics. In: Klaassen CD. (ed). Casarett and Doull’s Toxicology: The Basic Science of Poisons. New York: McGraw-Hill, pp. 161–303.
   Google Scholar
• Roffey SJ, Obach RS, Gedge JI, Smith DA. (2007). 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 39:17–43.
   PubMed Web of Science ®Google Scholar
• Smith DA, Obach RS. (2006). Metabolites and safety: What are the concerns, and how should we address them? Chem Res Toxicol 19:1570–1579.
   PubMed Web of Science ®Google Scholar
• Vishwanathan K, Babalola K, Wang J, Espina R, Yu L, Adedoyin A, Talaat R, Mutlib A, Scatina J. (2009). Obtaining exposures of metabolites in preclinical species through plasma pooling and quantitative NMR: addressing metabolites in safety testing (MIST) guidance without using radiolabeled compounds and chemically synthesized metabolite standards. Chem Res Toxicol 22:311–322.
   PubMed Web of Science ®Google Scholar
• Walker D, Brady J, Dalvie D, Davis J, Dowty M, Duncan JN, Nedderman A, Obach RS, Wright P. (2009). A holistic strategy for characterizing the safety of metabolites through drug discovery and development. Chem Res Toxicol 22:1653–1662.
   PubMed Web of Science ®Google Scholar
• Walker GS, Ryder TF, Sharma R, Smith EB, Freund A. (2011). Validation of isolated metabolites from drug metabolism studies as analytical standards by quantitative NMR. Drug Metab Dispos 39:433–440.
   PubMed Web of Science ®Google Scholar
• Wang WW, Khetani SR, Krzyzewski S, Duignan DB, Obach RS. (2010). Assessment of a micropatterned hepatocyte coculture system to generate major human excretory and circulating drug metabolites. Drug Metab Dispos 38:1900–1905.
   PubMed Web of Science ®Google Scholar
• Yi P, Luffer-Atlas D. (2010). A radiocalibration method with pseudo internal standard to estimate circulating metabolite concentrations. Bioanalysis 2:1195–1210.
   PubMed Web of Science ®Google Scholar
• Zhang D, Raghavan N, Chando T, Gambardella J, Fu Y, Zhang D, Unger SE, Humphreys WG. (2007). LC-MS/MS-based approach for obtaining exposure estimates of metabolites in early clinical trials using radioactive metabolites as reference standards. Drug Metab Lett 1:293–298.
   PubMedGoogle Scholar
• Zhang D, Raghavan N, Wang L, Xue Y, Obermeier M, Chen S, Tao S, Zhang H, Cheng PT, Li W, Ramanathan R, Yang Z, Humphreys WG. (2011). Plasma stability-dependent circulation of acyl glucuronide metabolites in humans: how circulating metabolite profiles of muraglitazar and peliglitazar can lead to misleading risk assessment. Drug Metab Dispos 39:123–131.
   PubMed Web of Science ®Google Scholar