Preclinical in vivo ADME studies in drug development: a critical review

Bibliography

• Baille TA. Metabolism and toxicity of drugs. Two decades of progresses in industrial drug metabolism. Chem Res Toxicol 2008;21:129-37
   PubMed Web of Science ®Google Scholar
• Cartwright ME, Cohen S, Fleishaker JC, Proof of concept: a PhRMA position paper with recommendations for best practice. Clin Pharmacol Ther 2010;87(3):278-85
   PubMed Web of Science ®Google Scholar
• Mahajan R, Gupta K. Food and drug administration's critical path initiative and innovations in drug development paradigm: challenges, progress and controversies. J Pharm Bioallied Sci 2010;2(4):307-13
   PubMedGoogle Scholar
• Summerfield S, Jeffrey P. Discovery DMPK: changing paradigms in the eighties, nineties and noughties. Expert Opin Drug Discov 2009;4(2):207-18
   PubMedGoogle Scholar
• Miwa GT. Goals, design, timing and future opportunities for nonclinical drug metabolism studies. Toxicol Pathol 1995;23(2):131-5
   PubMed Web of Science ®Google Scholar
• Glocklin VC. General considerations for studies of the metabolism of drugs and other chemicals. Drug Metab Rev 1982;13(6):929-39
   PubMed Web of Science ®Google Scholar
• Note for guidance on Toxicokinetics: a guidance for assessing systemic exposure in toxicology studies CPMP/ICH/384/95 (2009). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002770.pdf
   Google Scholar
• Landskroner KA, Hess P, Treiber A. Surgical and pharmacological animal models used in drug metabolism and pharmacokinetics. Xenobiotica 2011;41(8):687-700
   PubMed Web of Science ®Google Scholar
• Tsaioun K, Bottlaender M, Mabondzo A. ADDME- Avoiding drug development mistakes early: central nervous system drug discovery perspective. BMC Neurol 2009;9(S1): doi 10.1186/1471-2377-9-S1-S1
   PubMedGoogle Scholar
• Summerfield SG, Lucas AJ, Porter RA, Toward an improved prediction of human in vivo brain penetration. Xenobiotica 2008;38(12):1518-35
   PubMed Web of Science ®Google Scholar
• White RE, Manitpisitkul P. Pharmacokinetic theory of cassette dosing in drug discovery setting. Drug Met Dispos. 2001;29(7):957-66
   Google Scholar
• Nagilla R, Nord M, Mcatee JJ, Jolivette LJ. Cassette dosing for pharmacokinetic screening in drug discovery: comparison of clearance, volume of distribution, half-life, mean residence time and oral bioavailability obtained by cassette and discrete dosing in rats. J Pharm Sci 2011;100(9):3862-74
   PubMed Web of Science ®Google Scholar
• Baille TA, Cayen MN, Fouda H, Drug metabolites in safety testing. Toxicol Appl Pharmacol 2002;182:188-96
   PubMed Web of Science ®Google Scholar
• Guidance on Nonclinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorization for Pharmaceuticals M3(R2) CPMP/ICH/286/95 (2009). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002720.pdf
   Google Scholar
• 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(12):1539-49
   PubMed Web of Science ®Google Scholar
• Nedderman ANR, Dear GJ, North S, From definition to implementation: a cross-industry perspective of past, current and future MIST strategies. Xenobiotica 2011;41(8):605-22
   PubMed Web of Science ®Google Scholar
• Nedderman ANR. Metabolites in safety testing: metabolite identification strategies in discovery and development. Biopharm Drug Dispos 2009;30:153-62
   PubMed Web of Science ®Google Scholar
• Espina R, Yu L, Wang G, 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
   PubMed Web of Science ®Google Scholar
• 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 Analyt Technol Biomed Life Sci 2008;876:182-90
   PubMed Web of Science ®Google Scholar
• 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
   PubMed Web of Science ®Google Scholar
• Ramanathan R, Josephs JL, Jemal M, Novel MS solutions inspired by MIST. Bioanalysis 2010;2:1291-313
   PubMed Web of Science ®Google Scholar
• Yengi LG, Leung L, Kao J. The evolving role of drug metabolism in drug discovery and development. Pharm Res 2007;24(5); 842-58
   PubMed Web of Science ®Google Scholar
• Giacomini KM, Huang SM, Tweedie DJ, Membrane transporters in drug development. Nat Rev Drug Discov 2010;9:215-34
   PubMed Web of Science ®Google Scholar
• Pelkonen O, Kapitulnik J, Gundert-Remy U, Local kinetics and dynamics of xenobiotics. Crit Rev Toxicol 2008;38:697-720
   PubMed Web of Science ®Google Scholar
• Jamei M, Marciniak S, Feng K, The SymCyp population-based ADME simulator. Expert Opin Drug Metab Toxicol 2009;5:211-23
   PubMed Web of Science ®Google Scholar
• Rostami-Hodjegan A, Tucker GT. Simulation and prediction of in vivo drug metabolism in human populations from in vitro data. Nat Rev Drug Discov 2007;6:140-8
   PubMed Web of Science ®Google Scholar
• Balakin KV, Ivanenkov YA, Savchuk NP Comprehensive computational assessment of ADME properties using mapping techniques. Curr Drug Discov Technol 2005;2:99-113
   PubMedGoogle Scholar
• Jones HM, Gardner IB, Collard WT, Simulation of human intravenous and oral pharmacokinetics of 21 diverse compounds using physiologically based pharmacokinetic modelling. Clin Pharmacokinet 2011;50(5):331-47
   PubMed Web of Science ®Google Scholar
• Dickins M. Prediction of pathways of drug metabolism. In:. Daly A, editor. Drug metabolizing enzymes: fundamentals, study methods, recent advances and clinical significance. The Biomedical & Life sciences collection. Henry Stewards talks Ltd, London; 2007. Available from: http:/hstalks.com/bio
   Google Scholar
• Nestorov I. Whole body pharmacokinetic models. Clin pharmacokinet 2003;42(10):883-908
   PubMed Web of Science ®Google Scholar
• Sung JH, Esh MB, Shuler ML. Integration of in silico and in vitro platforms for PK-PD modelling. Expert Opin Drug Metab Toxicol 2010;6:1063-81
   PubMed Web of Science ®Google Scholar
• Lanao JM, Fraile MA. Drug tissue distribution: study methods and therapeutic implications. Curr Pharm Des 2005;11:3829-45
   PubMed Web of Science ®Google Scholar
• Langer O, Muller M. Methods to assess tissue-specific distribution and metabolism of drugs. Curr Drug Metab 2004;5:463-81
   PubMed Web of Science ®Google Scholar
• Russell WMS, Burch RL. The principle of human experimental technique. Methuen, London, UK; 1959
   Google Scholar
• Andersen ME, Krewski D. Toxicity testing in the 21st century: bringing the vision to life. Toxicol Sci 2009;107(2):324-30
   PubMed Web of Science ®Google Scholar
• Balls M. Replacing, reducing and refining animal experiments: making sound progress, but must do better. ATLA 2009;37:579-80
   Google Scholar
• Zhang D, Comezoglu SN. ADME studies in animals and humans. In: Zhang D, Zhu M, Humphreys WG, editors. Experimental design, metabolite profiling and identification, and data presentation in “Drug metabolism in drug design and development”. Hoboken, NJ, USA; John Wiley & sons, Inc.; 2008
   Google Scholar
• Luffer-Atlas D. Unique/major metabolites: why, how and when to test for safety in animals. Drug Metab Rev 2008, 40(3):447-63
   PubMed Web of Science ®Google Scholar
• Li Y, Landqvist C, Grimm SW. Disposition and metabolism of ticagrelor, a novel P2Y12 receptor antagonist, in mice, rats and marmosets. Drug Metab Dispos 2011;39(9):1555-67
   PubMed Web of Science ®Google Scholar
• Musick TJ, Gohdes M, Duffy A, Pharmacokinetics, disposition and metabolism of bicifadine in the mouse, rat and monkey. Drug Metab Dispos 2008;36(2):241-51
   PubMed Web of Science ®Google Scholar
• 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;39:17-43
   PubMed Web of Science ®Google Scholar
• Setnikar I, Makovec F, Christe R, Metabolism and excretion of 14C-tiropramide after single intravenous or peroral administration to the rat. Arzneimittel-Forshung 1989;39(3); 328-34
   PubMed Web of Science ®Google Scholar
• Matteo MR, Zavorskas P, Esber H. Tissue distribution and excretion in urine, feces and respiratory CO2 of [14C]-ciclosidomine in beagle dogs. Arzneimittel-Forshung 1985;35:329-32
   PubMed Web of Science ®Google Scholar
• Zang JY, Wang YF, Milton MN, Pharmacokinetics, metabolism and excretion of an inhibitor of inducible nitric oxide synthetase, L-NIL-TA, in dog. Xenobiotica 2003;33(11):1159-71
   PubMed Web of Science ®Google Scholar
• Huskey SE, Dean BJ, Doss GA, The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs. Drug Metab Dispos 2004;32(2):246-58
   PubMed Web of Science ®Google Scholar
• Guiney WJ, Beaumont C, Thomas SR. Use of entero-test, a novel approach for the noninvasive capture of biliary metabolites in dogs. Drug Metab Dispos. 2010;38:851-6
   PubMed Web of Science ®Google Scholar
• Miraglia L, Pagliarusco P, Bordini E, Metabolic disposition of casopitant, a potent neurokinin-1 receptor antagonist, in mice, rats and dogs. Drug Metab Dispos 2010;38:1876-91
   PubMed Web of Science ®Google Scholar
• Potchoiba MJ, West M, Nocerini MR. Quantitative comparison of autoradioluminographic and radiometric tissue distribution studies using carbon-14 labeled xenobiotics. Drug Metab Dispos. 1998;26:272-7
   PubMed Web of Science ®Google Scholar
• Solon EG. Autoradiography: high resolution molecular imaging in pharmaceutical discovery and development. Expert Opin Drug Discov 2007;2(4):503-14
   PubMed Web of Science ®Google Scholar
• Wuis EW, Rijntjes NV, Van der Kleijn E. Whole body autoradiography of 14C-dantrolene in the marmoset monkey. Pharmacol Toxicol 1989;64(1):156-8
   PubMedGoogle Scholar
• Solon EG, Balani SK, Lee FW. Whole body autoradiography in drug discovery. Curr Drug Metab 2002;3:451-62
   PubMed Web of Science ®Google Scholar
• Solon EG, Kraus L. Quantitative whole-body autoradiography in the pharmaceutical industry. Survey results on study design, methods, and regulatory compliance. J Pharmacol Toxicol Methods 2001;46(2):73-81
   PubMed Web of Science ®Google Scholar
• He K, Lago MW, Shyu WC, Lacteal secretion, fetal and maternal tissue distribution of dasatinib in rats. Drug Metab Dispos. 2008;36:2564-70
   PubMed Web of Science ®Google Scholar
• Nicholis I, Kolopp M, Pommier F, Scheiwiller M. The presence of drug in control samples during toxicokinetic investigations – A Novartis perspective. Regul Toxicol Pharmacol 2005;42(2):172-8
   PubMed Web of Science ®Google Scholar
• Lay Y. Identification of interspecies difference in hepatobiliary transporters to improve extrapolation of human biliary secretion. Expert Opin Drug Metab Toxicol 2009;5(10):1175-87
   PubMed Web of Science ®Google Scholar
• Yang X, Gandhi YA, Morris ME. Biliary excretion in dogs: evidence for a molecular weight threshold. Eur J Pharm Sci 2010;40:33-7
   PubMed Web of Science ®Google Scholar
• Maringka M, Giri S, Nieber K, Biotransformation of diazepam in a clinically relevant flat membrane bioreactor model using primary porcine hepatocytes. Fundam Clin Pharmacol 2011;25(3):343-53
   PubMed Web of Science ®Google Scholar
• Gebhardt R, Hengstler JG, Muller D, New hepatocyte in vitro systems for drug metabolism: metabolic capacity and recommendations for application in basic research and drug development, standard operation procedures. Drug Metab Rev 2003;35(2-3):145-213
   PubMed Web of Science ®Google Scholar
• Vishwanathan K, Babalola K, Espina R, 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 2009;22(2):311-22
   PubMed Web of Science ®Google Scholar
• ICH Topic S1C(R2). Note for guidance on dose selection for carcinogenicity studies of pharmaceuticals. EMEA/CHMP/ICH/383/1995. 2008. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002768.pdf
   Google Scholar
• Sullivan HR, Hanasomo GK, Miller WM, Wood PG. Species specificity in the metabolism of nabilone. Relationship between toxicity and metabolic routes. Xenobiotica 1987;17(4):459-68
   PubMed Web of Science ®Google Scholar
• Leblanc B, Jezequel S, Davies T Binding of drugs to eye melanin is not predictive of ocular toxicity. Regul Toxicol Pharmacol 1998;28:124-32
   PubMed Web of Science ®Google Scholar
• Guidance for industry. Photosafety testing. FDA/Center for Drug Evaluation and Research. 2003. Available from: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm079252.pdf
   Google Scholar
• Zane PA, Brindle SD, Gause DO, Physicochemical factors associated with binding and retention of compounds in ocular melanin of rats; correlation using data from whole-body autoradiography and molecular modeling for multiple linear regression analyses. Pharm Res 1990;7:935-41
   PubMed Web of Science ®Google Scholar
• Monro AM. Are routine tissue distribution studies justifiable for approval of human drugs? Drug Metab Dispos 1994;22(3):341-2
   PubMed Web of Science ®Google Scholar
• Vonderfect SL, Stone ML, Eversole RR, Myopathy related to administration of a cationic amphiphilic drug and the use of multidose drug distribution analysis to predict its occurrence. Toxicol Pathol 2004, 32:318-25
   PubMed Web of Science ®Google Scholar
• Gum RJ, Hickman D, Fagerland JA, Analysis of two matrix metalloproteinase inhibitors and their metabolites for induction of phospholipidosis in rat and human hepatocytes. Biochem Pharmacol 2001;62:1661-73
   PubMed Web of Science ®Google Scholar
• Arjomand A. Accelerator mass spectrometry- enabled studies: current status and future prospects. Bioanalysis 2010;2(3):519-41
   PubMed Web of Science ®Google Scholar
• Lappin G, Seymour M. Addressing metabolite safety during first-in-man studies using 14C-labeled drug and accelerator mass spectrometry. Bioanalysis 2010;2(7):1315-24
   PubMed Web of Science ®Google Scholar
• Spooner N, Lad R, Barfield M. Dried Blood Spots as a sample collection technique for the determination of pharmacokinetics in clinical studies: considerations for the validation of a quantitative bioanalytical method. Anal Chem 2009;81:1557-63
   PubMed Web of Science ®Google Scholar
• Patel P, Mulla H, Tanna S. Facilitating pharmacokinetic studies in children: a new use of dried blood spots. Arch Dis Child 2010;95:484-7
   PubMed Web of Science ®Google Scholar
• Griffini P, James AD, Roberts AD, Pellegatti M. Metabolites in safety testing: issues and approaches to the safety evaluation of human metabolites in a drug that is extensively metabolized. J Drug Metab Toxicol 2010;1:102
   Google Scholar
• Kim KY, Lee YJ, Chung BC, Relations between toxicity and altered tissue distribution and urinary excretion of nicotine, cotinine and hydroxycotinine after chronic oral administration of nicotine in rats. Drug Chem Toxicol 2010;33(2):166-72
   PubMed Web of Science ®Google Scholar
• Pagliarusco S, Martinucci S, Bordin E, Tissue distribution and characterisation of drug related material in rats and dogs after repeat oral administration of casopitant. Drug Metab Dispos. 2011;39(2):283-93
   PubMed Web of Science ®Google Scholar
• Obach RS, Nedderman AN, Smith DA. Radiolabelled mass-balance excretion and metabolism studies in laboratory animals: are they still necessary? Xenobiotica 2012;42(1):46-56
   PubMed Web of Science ®Google Scholar