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The following is a list of articles relevant to Phase-0 including Microdosing approaches in reverse order by year of publication. Please contact us if you are aware of a publication that is not included in the list.


1            Xiao, H. et al. Developing a cassette microdosing approach to enhance the throughput of PET imaging agent screening. J Pharm Biomed Anal 154, 48-56, doi:10.1016/j.jpba.2018.02.063 (2018).

2            Sjogren, E., Halldin, M. M., Stalberg, O. & Sundgren-Andersson, A. K. Preclinical characterization of three transient receptor potential vanilloid receptor 1 antagonists for early use in human intradermal microdose analgesic studies. European journal of pain (London, England), doi:10.1002/ejp.1175 (2018).

3            Schwarz, S. W. & Clarke, B. N. Invited Perspective on JNM manuscript titled, "How Should FDA Review Diagnostic Radiopharmaceuticals?" by Carol Marcus. J Nucl Med, doi:10.2967/jnumed.117.204446 (2018).

4            Sanai, N. et al. Phase 0 Trial of AZD1775 in First-Recurrence Glioblastoma Patients. Clin Cancer Res, doi:10.1158/1078-0432.ccr-17-3348 (2018).

5            Law, M. et al. Cumulative effective dose and cancer risk for pediatric population in repetitive full spine follow-up imaging: How micro dose is the EOS microdose protocol? European journal of radiology 101, 87-91, doi:10.1016/j.ejrad.2018.02.015 (2018).

6            Kratochwil, N. A. et al. Nanotracing and cavity-ring down spectroscopy: A new ultrasensitive approach in large molecule drug disposition studies. PLoS One 13, e0205435, doi:10.1371/journal.pone.0205435 (2018).

7            Kramer, L. A. & Greek, R. Human Stakeholders and the Use of Animals in Drug Development. Business and Society Review 123, 3-58, doi:doi:10.1111/basr.12134 (2018).

8            Keat, N. et al. A Microdose PET Study of the Safety, Immunogenicity, Biodistribution, and Radiation Dosimetry of (18)F-FB-A20FMDV2 for Imaging the Integrin alphavbeta6. Journal of nuclear medicine technology 46, 136-143, doi:10.2967/jnmt.117.203547 (2018).

9            Chavez-Eng, C. M., Lutz, R. W., Goykhman, D. & Bateman, K. P. Microdosing Cocktail Assay Development for Drug-Drug Interaction Studies. J Pharm Sci 107, 1973-1986, doi:10.1016/j.xphs.2018.02.023 (2018).

10         Burt, T. et al. Phase 0, including microdosing approaches: Applying the Three Rs and increasing the efficiency of human drug development. Altern Lab Anim 46, 335-346 (2018).

11         Burt, T., Combes, R. D. . in The History of Alternative Test Methods in Toxicology   (ed R.D. Combes M. Balls, A. Worth )  229-240 (Elsevier/Academic Press, 2018).



12         Zimmermann, M. et al. Microdose-Induced Drug-DNA Adducts as Biomarkers of Chemotherapy Resistance in Humans and Mice. Molecular cancer therapeutics 16, 376-387, doi:10.1158/1535-7163.mct-16-0381 (2017).

13         Zhang, L. & Sparreboom, A. Predicting transporter-mediated drug interactions: Commentary on: "Pharmacokinetic evaluation of a drug transporter cocktail consisting of digoxin, furosemide, metformin and rosuvastatin" and "Validation of a microdose probe drug cocktail for clinical drug interaction assessments for drug transporters and CYP3A". Clin Pharmacol Ther 101, 447-449, doi:10.1002/cpt.588 (2017).

14         Wotherspoon, A. T., Safavi-Naeini, M. & Banati, R. B. Microdosing, isotopic labeling, radiotracers and metabolomics: relevance in drug discovery, development and safety. Bioanalysis 9, 1913-1933, doi:10.4155/bio-2017-0137 (2017).

15         Wang, X. et al. Rolapitant Absolute Bioavailability and PET Imaging Studies in Healthy Adult Volunteers. Clin Pharmacol Ther 102, 332-339, doi:10.1002/cpt.637 (2017).

16         Wang, S. S. et al. A diagnostic microdosing approach to investigate platinum sensitivity in non-small cell lung cancer. Int J Cancer 141, 604-613, doi:10.1002/ijc.30747 (2017).

17         van Nuland, M. et al. Ultra-sensitive LC-MS/MS method for the quantification of gemcitabine and its metabolite 2',2'-difluorodeoxyuridine in human plasma for a microdose clinical trial. J Pharm Biomed Anal 151, 25-31, doi:10.1016/j.jpba.2017.12.048 (2017).

18         Swain, N. A. et al. Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4 -ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7. Journal of medicinal chemistry, doi:10.1021/acs.jmedchem.7b00598 (2017).

19         Samkoe, K. S. et al. Toxicity and Pharmacokinetic Profile for Single-Dose Injection of ABY-029: a Fluorescent Anti-EGFR Synthetic Affibody Molecule for Human Use. Mol Imaging Biol 19, 512-521, doi:10.1007/s11307-016-1033-y (2017).

20         Rizk, M. L., Zou, L., Savic, R. M. & Dooley, K. E. Importance of Drug Pharmacokinetics at the Site of Action. Clinical and translational science, n/a-n/a, doi:10.1111/cts.12448 (2017).

21         Rajagopalan, R. et al. Preclinical Characterization and Human Microdose Pharmacokinetics of ITMN-8187, a Nonmacrocyclic Inhibitor of the Hepatitis C Virus NS3 Protease. Antimicrob Agents Chemother 61, doi:10.1128/aac.01569-16 (2017).

22         Prueksaritanont, T. et al. Validation of a microdose probe drug cocktail for clinical drug interaction assessments for drug transporters and CYP3A. Clin Pharmacol Ther 101, 519-530, doi:10.1002/cpt.525 (2017).

23         Park, W.-S. et al. Human microdosing and mice xenograft data of AGM-130 applied to estimate efficacious doses in patients. Cancer Chemotherapy and Pharmacology 80, 363-369, doi:10.1007/s00280-017-3373-y (2017).

24         Okour, M. et al. A Human Microdose Study of the Anti-Malarial GSK3191607 in Healthy Volunteers. Br J Clin Pharmacol, doi:10.1111/bcp.13476 (2017).

25         Ng, S. Y. & Bettany-Saltikov, J. Imaging in the Diagnosis and Monitoring of Children with Idiopathic Scoliosis. The open orthopaedics journal 11, 1500-1520, doi:10.2174/1874325001711011500 (2017).

26         Nandal, S. & Burt, T. Integrating Pharmacoproteomics into Early-Phase Clinical Development: State-of-the-Art, Challenges, and Recommendations. International journal of molecular sciences 18, doi:10.3390/ijms18020448 (2017).

27         Mooij, M. G. et al. Successful Use of [14C]Paracetamol Microdosing to Elucidate Developmental Changes in Drug Metabolism. Clin Pharmacokinet, doi:10.1007/s40262-017-0508-6 (2017).

28         Lamberts, L. E. et al. Tumor-Specific Uptake of Fluorescent Bevacizumab-IRDye800CW Microdosing in Patients with Primary Breast Cancer: A Phase I Feasibility Study. Clin Cancer Res 23, 2730-2741, doi:10.1158/1078-0432.ccr-16-0437 (2017).

29         Kusuhara, H. et al. Comparison of pharmacokinetics of newly discovered aromatase inhibitors by a cassette microdosing approach in healthy Japanese subjects. Drug metabolism and pharmacokinetics 32, 293-300, doi:10.1016/j.dmpk.2017.09.003 (2017).

30         Koch, M. et al. Threshold Analysis and Biodistribution of Fluorescently Labeled Bevacizumab in Human Breast Cancer. Cancer Res 77, 623-631, doi:10.1158/0008-5472.can-16-1773 (2017).

31         Kim, A. et al. An accelerator mass spectrometry-enabled microtracer study to evaluate the first-pass effect on the absorption of YH4808. Clin Pharmacol Ther, doi:10.1002/cpt.672 (2017).

32         Jensen, K. G. et al. Lack of Exposure in a First-in-Man Study Due to Aldehyde Oxidase Metabolism: Investigated by Use of 14C-microdose, Humanized Mice, Monkey Pharmacokinetics, and In Vitro Methods. Drug Metab Dispos 45, 68-75, doi:10.1124/dmd.116.072793 (2017).

33         de Souza, A. L. et al. Fluorescent Affibody Molecule Administered In Vivo at a Microdose Level Labels EGFR Expressing Glioma Tumor Regions. Mol Imaging Biol 19, 41-48, doi:10.1007/s11307-016-0980-7 (2017).

34         Chen, M. et al. An ultra-sensitive LC-MS/MS method to determine midazolam levels in human plasma: development, validation and application to a clinical study. Bioanalysis 9, 297-312, doi:10.4155/bio-2016-0191 (2017).

35         Burt, T. et al. Intra-Target Microdosing (ITM): A Novel Drug Development Approach Aimed at Enabling Safer and Earlier Translation of Biological Insights Into Human Testing. Clinical and translational science, 1-14, doi:10.1111/cts.12464 (2017).

36         Burt, T. et al. Intra-Target Microdosing - A Novel Drug Development Approach: Proof of Concept, Safety, and Feasibility Study in Humans. Clinical and translational science, doi:10.1111/cts.12477 (2017).

37         Burt, T., Button, K. S., Thom, H., Noveck, R. J. & Munafo, M. R. The Burden of the "False-Negatives" in Clinical Development: Analyses of Current and Alternative Scenarios and Corrective Measures. Clinical and translational science 10, 470-479, doi:10.1111/cts.12478 (2017).

38         Bergstrom, M. The Use of Microdosing in the Development of Small Organic and Protein Therapeutics. J Nucl Med 58, 1188-1195, doi:10.2967/jnumed.116.188037 (2017).



39         Togashi, K. et al. Systematic approach to optimize a pretreatment method for ultrasensitive liquid chromatography with tandem mass spectrometry analysis of multiple target compounds in biological samples. Journal of separation science 39, 3212-3220, doi:10.1002/jssc.201600282 (2016).

40         Swart, P., Lozac'h, F., Simon, M., van Duijn, E. & Vaes, W. H. The impact of early human data on clinical development: there is time to win. Drug Discov Today 21, 873-879, doi:10.1016/j.drudis.2016.03.012 (2016).

41         Svendsen, P. et al. The application of human phase 0 microdosing trials: A systematic review and perspectives. Leuk Lymphoma 57, 1281-1290, doi:10.3109/10428194.2015.1101097 (2016).

42         Seymour, M. A. Adding value through accelerator mass spectrometry-enabled first in human studies. Journal of labelled compounds & radiopharmaceuticals 59, 640-647, doi:10.1002/jlcr.3420 (2016).

43         Rowland, M. Microdosing of protein drugs. Clin Pharmacol Ther 99, 150-152, doi:10.1002/cpt.275 (2016).

44         Roffel, A. F., van Marle, S. P., van Lier, J. J., Hartstra, J. & van Hoogdalem, E. J. An evaluation of human ADME and mass balance studies using regular or low doses of radiocarbon. Journal of labelled compounds & radiopharmaceuticals 59, 619-626, doi:10.1002/jlcr.3473 (2016).

45         Madeen, E. P. et al. Human Microdosing with Carcinogenic Polycyclic Aromatic Hydrocarbons: In Vivo Pharmacokinetics of Dibenzo[def,p]chrysene and Metabolites by UPLC Accelerator Mass Spectrometry. Chem Res Toxicol 29, 1641-1650, doi:10.1021/acs.chemrestox.6b00169 (2016).

46         Jones, H. M. et al. Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels. Clin Pharmacokinet 55, 875-887, doi:10.1007/s40262-015-0365-0 (2016).

47         de Vries, R. et al. Stable isotope-labelled intravenous microdose for absolute bioavailability and effect of grapefruit juice on ibrutinib in healthy adults. Br J Clin Pharmacol 81, 235-245, doi:10.1111/bcp.12787 (2016).

48         Burt, T. et al. Microdosing and other Phase-0 Clinical Trials: Facilitating Translation in Drug Development. Clinical and translational science 9, 74-88, doi:10.1111/cts.12390 (2016).

49         Burt, T. et al. Intra-Target Microdosing (ITM), A Novel Drug Development Approach: Proof-of-Concept in Humans. 2016 Annual Meeting of the American College of Clinical Pharmacology, September 25–27, 2016, Bethesda, MD. Clinical Pharmacology in Drug Development 5, 3-56, doi:10.1002/cpdd.292 (2016).

50         Burt, T., John, C. S., Ruckle, J. L. & Vuong, L. T. Phase-0/microdosing studies using PET, AMS, and LC-MS/MS: a range of study methodologies and conduct considerations. Accelerating development of novel pharmaceuticals through safe testing in humans - a practical guide. Expert opinion on drug delivery, 1-16, doi:10.1080/17425247.2016.1227786 (2016).

51         Bosgra, S., Vlaming, M. L. & Vaes, W. H. To Apply Microdosing or Not? Recommendations to Single Out Compounds with Non-Linear Pharmacokinetics. Clin Pharmacokinet 55, 1-15, doi:10.1007/s40262-015-0308-9 (2016).

52         Bal, C. et al. Pharmacokinetic, Dosimetry and Toxicity Study of (1)(7)(7)Lu-EDTMP in Patients: Phase 0/I study. Current radiopharmaceuticals 9, 71-84 (2016).



53         Yamashita, S. et al. An Assessment of the Oral Bioavailability of Three Ca-Channel Blockers Using a Cassette-Microdose Study: A New Strategy for Streamlining Oral Drug Development. J Pharm Sci 104, 3154-3161, doi:10.1002/jps.24499 (2015).

54         Woolsey, S. J. et al. Relationships between Endogenous Plasma Biomarkers of Constitutive CYP3A Activity with Single Time-Point Oral Midazolam Microdose Phenotype in Healthy Subjects. Basic & clinical pharmacology & toxicology, doi:10.1111/bcpt.12492 (2015).

55         Vuong, L. T. et al. Opportunities in low-level radiocarbon microtracing: applications and new technology. Future Science OA 2, 1-22, doi:10.4155/fso.15.74 (2015).

56         Vlaming, M. et al. Microdosing of a Carbon-14 Labeled Protein in Healthy Volunteers Accurately Predicts Its Pharmacokinetics at Therapeutic Dosages. Clin Pharmacol Ther 98, 196-204, doi:10.1002/cpt.131 (2015).

57         Van Dongen, G. A. et al. 89Zr-immuno-PET for imaging of long circulating drugs and disease targets: why, how and when to be applied? The quarterly journal of nuclear medicine and molecular imaging : official publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the So 59, 18-38 (2015).

58         Uhl, P., Fricker, G., Haberkorn, U. & Mier, W. Radionuclides in drug development. Drug Discov Today 20, 198-208, doi:10.1016/j.drudis.2014.09.027 (2015).

59         Turner, M. A. et al. Pediatric microdose and microtracer studies using (14) C in Europe. Clin Pharmacol Ther 98, 234-237, doi:10.1002/cpt.163 (2015).

60         Shingaki, T. et al. Quantitative Evaluation of mMate1 Function Based on Minimally Invasive Measurement of Tissue Concentration Using PET with [C]Metformin in Mouse. Pharm Res, doi:10.1007/s11095-015-1642-1 (2015).

61         Schwarz, S. W. & Oyama, R. The role of exploratory investigational new drugs for translating radiopharmaceuticals into first-in-human studies. J Nucl Med 56, 497-500, doi:10.2967/jnumed.114.146472 (2015).

62         Schou, M. et al. Large Variation in Brain Exposure of Reference CNS Drugs: a PET Study in Nonhuman Primates. Int J Neuropsychopharmacol 18, pyv036, doi:10.1093/ijnp/pyv036 (2015).

63         Schou, M. et al. Large Variation in Brain Exposure of Reference CNS Drugs: a PET Study in Nonhuman Primates. Int J Neuropsychopharmacol 18, doi:10.1093/ijnp/pyv036 (2015).

64         Saleem, A. et al. Lapatinib access into normal brain and brain metastases in patients with Her-2 overexpressing breast cancer. EJNMMI research 5, 30, doi:10.1186/s13550-015-0103-5 (2015).

65         Roth-Cline, M. & Nelson, R. M. Microdosing Studies in Children: A US Regulatory Perspective. Clin Pharmacol Ther 98, 232-233, doi:10.1002/cpt.165 (2015).

66         Park, M. H. et al. Validation of a liquid chromatography-triple quadrupole mass spectrometric method for the determination of 5-nitro-5'-hydroxy-indirubin-3'-oxime (AGM-130) in human plasma and its application to microdose clinical trial. Biomed Chromatogr, doi:10.1002/bmc.3551 (2015).

67         Lappin, G. The expanding utility of microdosing. Clin Pharmacol Drug Dev 4, 401-406, doi:10.1002/cpdd.235 (2015).

68         Johnstrom, P. et al. Development of rapid multistep carbon-11 radiosynthesis of the myeloperoxidase inhibitor AZD3241 to assess brain exposure by PET microdosing. Nuclear medicine and biology 42, 555-560, doi:10.1016/j.nucmedbio.2015.02.001 (2015).

69         Hohmann, N. et al. Midazolam microdose to determine systemic and pre-systemic metabolic CYP3A activity in humans. Br J Clin Pharmacol 79, 278-285, doi:10.1111/bcp.12502 (2015).

70         Hohmann, N., Haefeli, W. E. & Mikus, G. Use of Microdose Phenotyping to Individualise Dosing of Patients. Clin Pharmacokinet 54, 893-900, doi:10.1007/s40262-015-0278-y (2015).

71         Hillyar, C. R., Knight, J. C., Vallis, K. A. & Cornelissen, B. PET and SPECT Imaging for the Acceleration of Anti-Cancer Drug Development. Current drug targets 16, 582-591 (2015).

72         Gupta, S., Gersing, K. R., Erkanli, A. & Burt, T. Antidepressant Regulatory Warnings, Prescription Patterns, Suicidality and Other Aggressive Behaviors in Major Depressive Disorder and Anxiety Disorders. The Psychiatric quarterly, doi:10.1007/s11126-015-9389-8 (2015).

73         Garner, C. R. et al. Observational infant exploratory [(14)C]-paracetamol pharmacokinetic microdose/therapeutic dose study with accelerator mass spectrometry bioanalysis. Br J Clin Pharmacol 80, 157-167, doi:10.1111/bcp.12597 (2015).

74         Fujita, K. et al. A clinical pharmacokinetic microdosing study of docetaxel with Japanese patients with cancer. Cancer Chemother Pharmacol 76, 793-801, doi:10.1007/s00280-015-2844-2 (2015).

75         Devineni, D. et al. Absolute oral bioavailability and pharmacokinetics of canagliflozin: A microdose study in healthy participants. Clin Pharmacol Drug Dev 4, 295-304, doi:10.1002/cpdd.162 (2015).

76         DeMarco, V. P. et al. Determination of [11C]Rifampin Pharmacokinetics within Mycobacterium tuberculosis-Infected Mice by Using Dynamic Positron Emission Tomography Bioimaging. Antimicrob Agents Chemother 59, 5768-5774, doi:10.1128/aac.01146-15 (2015).

77         Burt T, W. H., Layton AT, Rouse DC, Chin BB, Hawk TC, Weitzel DH, Cohen-Wolkowiez M, Chow S, Noveck RJ. Intra-Arterial Microdosing (IAM), a novel drug development approach, proof of concept in rats. Clinical Pharmacology in Drug Development 4, 1-60, doi:10.1002/cpdd.216 (2015).

78         Burt, T. et al. Intra-Arterial Microdosing (IAM), a novel drug development approach, proof of concept in rats. Clinical therapeutics 37, e40-e41, doi:10.1016/j.clinthera.2015.05.122 (2015).

79         Burt, T. et al. Intraarterial Microdosing: A Novel Drug Development Approach, Proof-of-Concept PET Study in Rats. J Nucl Med 56, 1793-1799, doi:10.2967/jnumed.115.160986 (2015).

80         Burt, T., Rouse, D.C.; Chin, B.B.; Chow, S.; Weitzel, D.H.; Wu, H.; Hawk, T.C.; Cohen-Wolkowiez, M.; Noveck, R.J. Intra-Arterial Microdosing (IAM), A Novel Drug Development Approach, Proof of Concept in Rats. Clinical Pharmacology & Therapeutics 97, S62, doi:10.1002/cpt.52 (2015).

81         Annes, W. F. et al. Relative contributions of presystemic and systemic peptidases to oral exposure of a novel metabotropic glutamate 2/3 receptor agonist (LY404039) after oral administration of prodrug pomaglumetad methionil (LY2140023). J Pharm Sci 104, 207-214, doi:10.1002/jps.24226 (2015).



82         Xu, X. S. et al. Sensitivity-based analytical approaches to support human absolute bioavailability studies. Bioanalysis 6, 497-504, doi:10.4155/bio.13.318 (2014).

83         Wurz, G. T. & Degregorio, M. W. Response to: "Deceptive argumentation against diagnostic microdosing of anti-cancer drugs" by Dirk Theile and Gerd Mikus (Letter dated February 13, 2014). Int J Cancer, doi:10.1002/ijc.28805 (2014).

84         Wurz, G. T. & Degregorio, M. W. Activating adaptive cellular mechanisms of resistance following sublethal cytotoxic chemotherapy: Implications for diagnostic microdosing. Int J Cancer, doi:10.1002/ijc.28773 (2014).

85         van der Veldt, A. A. & Lammertsma, A. A. In vivo imaging as a pharmacodynamic marker. Clin Cancer Res 20, 2569-2577, doi:10.1158/1078-0432.ccr-13-2666 (2014).

86         Theile, D. & Mikus, G. Deceptive argumentation against diagnostic microdosing of anti-cancer drugs. Int J Cancer, doi:10.1002/ijc.28806 (2014).

87         Mooij, M. G. et al. Pediatric microdose study of [(14)C]paracetamol to study drug metabolism using accelerated mass spectrometry: proof of concept. Clin Pharmacokinet 53, 1045-1051, doi:10.1007/s40262-014-0176-8 (2014).

88         Malfatti, M. A., Lao, V., Ramos, C. L., Ong, V. S. & Turteltaub, K. W. Use of microdosing and accelerator mass spectrometry to evaluate the pharmacokinetic linearity of a novel tricyclic GyrB/ParE inhibitor in rats. Antimicrob Agents Chemother 58, 6477-6483, doi:10.1128/aac.03300-14 (2014).

89         Madeen, E. et al. Human in Vivo Pharmacokinetics of [C]Dibenzo[def,p]chrysene by Accelerator Mass Spectrometry Following Oral Microdosing. Chem Res Toxicol, doi:10.1021/tx5003996 (2014).

90         Hohmann, N., Halama, B., Siller, N., Mikus, G. & Haefeli, W. E. Response to "can CYP3A activity be evaluated for drug interaction using a nanogram dose of probe drug?": evaluation of CYP3A activity with microdoses of midazolam. Clin Pharmacol Ther 95, 490-491, doi:10.1038/clpt.2014.28 (2014).

91         Gordi, T. et al. Pharmacokinetic analysis of 14C-ursodiol in newborn infants using accelerator mass spectrometry. J Clin Pharmacol 54, 1031-1037, doi:10.1002/jcph.327 (2014).

92         Carls, A. et al. Systemic exposure of topical erythromycin in comparison to oral administration and the effect on cytochrome P450 3A4 activity. Br J Clin Pharmacol 78, 1433-1440, doi:10.1111/bcp.12497 (2014).

93         Burt, T. et al. Clinical Research Environment in India: Challenges and Proposed Solutions. Journal of clinical research & bioethics 5, 1-8, doi:10.4172/2155-9627.1000201 (2014).



94         Yamane, N. et al. Cost-effectiveness analysis of microdose clinical trials in drug development. Drug metabolism and pharmacokinetics 28, 187-195 (2013).

95         van der Veldt, A. A., Smit, E. F. & Lammertsma, A. A. Positron Emission Tomography as a Method for Measuring Drug Delivery to Tumors in vivo: The Example of [(11)C]docetaxel. Frontiers in oncology 3, 208, doi:10.3389/fonc.2013.00208 (2013).

96         van der Veldt, A. A. et al. Toward prediction of efficacy of chemotherapy: a proof of concept study in lung cancer patients using [(1)(1)C]docetaxel and positron emission tomography. Clin Cancer Res 19, 4163-4173, doi:10.1158/1078-0432.ccr-12-3779 (2013).

97         Schou, M. et al. Radiolabeling of the cannabinoid receptor agonist AZD1940 with carbon-11 and PET microdosing in non-human primate. Nuclear medicine and biology 40, 410-414, doi:10.1016/j.nucmedbio.2012.10.011 (2013).

98         Mochida, I. et al. Whole body pharmacokinetics of C-11 donepezil hydrochloride in humans: A positron emission tomography study. J NUCL MED MEETING ABSTRACTS 54, 1188- (2013).

99         Liu, A. & Aubry, A. F. Conference Report: Energized bioanalytical solutions at the 2012 Eastern Analytical Symposium & Exposition. Bioanalysis 5, 2341-2344, doi:10.4155/bio.13.228 (2013).

100       Lesche, R. et al. Preclinical evaluation of BAY 1075553, a novel F-labelled inhibitor of prostate-specific membrane antigen for PET imaging of prostate cancer. European journal of nuclear medicine and molecular imaging, doi:10.1007/s00259-013-2527-3 (2013).

101       Lappin, G., Noveck, R. & Burt, T. Microdosing and drug development: past, present and future. Expert Opin Drug Metab Toxicol 9, 817-834, doi:10.1517/17425255.2013.786042 (2013).

102       Lappin, G. et al. A microdose study of (1)(4)C-AR-709 in healthy men: pharmacokinetics, absolute bioavailability and concentrations in key compartments of the lung. Eur J Clin Pharmacol 69, 1673-1682, doi:10.1007/s00228-013-1528-2 (2013).

103       Lamers, R. J., de Jong, A. F., Lopez-Gutierrez, J. M. & Gomez-Guzman, J. Iodine-129 microdosing for protein and peptide drug development: erythropoietin as a case study. Bioanalysis 5, 53-63, doi:10.4155/bio.12.297 (2013).

104       Kummar, S. et al. First-in-human phase 0 trial of oral 5-iodo-2-pyrimidinone-2'-deoxyribose in patients with advanced malignancies. Clin Cancer Res 19, 1852-1857, doi:10.1158/1078-0432.ccr-12-3118 (2013).

105       Kim, B. I. et al. First in human imaging of amyloid deposition in Alzheimer disease using the [18F]FC119S. J NUCL MED MEETING ABSTRACTS 54, 1803- (2013).

106       Kaplan, N., Garner, C. & Hafkin, B. AFN-1252 in vitro absorption studies and pharmacokinetics following microdosing in healthy subjects. Eur J Pharm Sci 50, 440-446, doi:10.1016/j.ejps.2013.08.019 (2013).

107       IOM. Improving the Utility and Translation of Animal Models for Nervous System Disorders: Workshop Summary.  (The National Academies Press, 2013).

108       IOM. Improving and Accelerating Therapeutic Development for Nervous System Disorders: Workshop Summary.  (The National Academies Press, 2013).

109       Ikeda, T. et al. Microdose pharmacogenetic study of (1)(4)C-tolbutamide in healthy subjects with accelerator mass spectrometry to examine the effects of CYP2C9 *3 on its pharmacokinetics and metabolism. Eur J Pharm Sci 49, 642-648, doi:10.1016/j.ejps.2013.05.016 (2013).

110       Ieiri, I. et al. Mechanisms of pharmacokinetic enhancement between ritonavir and saquinavir; micro/small dosing tests using midazolam (CYP3A4), fexofenadine (p-glycoprotein), and pravastatin (OATP1B1) as probe drugs. J Clin Pharmacol 53, 654-661, doi:10.1002/jcph.62 (2013).

111       Heuveling, D. A. et al. Phase 0 microdosing PET study using the human mini antibody F16SIP in head and neck cancer patients. J Nucl Med 54, 397-401, doi:10.2967/jnumed.112.111310 (2013).

112       Hensel, F., Eckstein, M., Rosenwald, A. & Brandlein, S. Early development of PAT-SM6 for the treatment of melanoma. Melanoma research 23, 264-275, doi:10.1097/CMR.0b013e328362cbc8 (2013).

113       Halama, B. et al. A nanogram dose of the CYP3A probe substrate midazolam to evaluate drug interactions. Clin Pharmacol Ther 93, 564-571, doi:10.1038/clpt.2013.27 (2013).

114       Fuloria, N. K., Fuloria, S. & Vakiloddin, S. Phase zero trials: a novel approach in drug development process. Renal failure 35, 1044-1053, doi:10.3109/0886022x.2013.810543 (2013).

115       Dunphy, M. et al. Progress in first-in-human trial of Hsp90-targeted PET imaging in cancer patients. J NUCL MED MEETING ABSTRACTS 54, 279- (2013).

116       Cho, D. Y., Bae, S. H., Shon, J. H. & Bae, S. K. High-sensitive LC-MS/MS method for the simultaneous determination of mirodenafil and its major metabolite, SK-3541, in human plasma: application to microdose clinical trials of mirodenafil. Journal of separation science 36, 840-848, doi:10.1002/jssc.201200919 (2013).

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163       Moschos, S. J. et al. Pharmacodynamic (phase 0) study using etaracizumab in advanced melanoma. J Immunother 33, 316-325, doi:10.1097/CJI.0b013e3181c1f216 (2010).

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218       Sparreboom, A. Unexplored Pharmacokinetic Opportunities with Microdosing in Oncology. Clin Cancer Res 13, 4033-4034 (2007).

219       Rowland, M. Commentary on ACCP position statement on the use of microdosing in the drug development process. J Clin Pharmacol 47, 1595-1596; author reply 1597-1598 (2007).

220       Rasool, S., Abid, S. & Jafri, W. Validity and cost comparison of 14carbon urea breath test for diagnosis of H Pylori in dyspeptic patients. World J Gastroenterol 13, 925-929 (2007).

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227       Kinders, R. et al. Phase 0 clinical trials in cancer drug development: from FDA guidance to clinical practice. Molecular interventions 7, 325-334 (2007).

228       Kimmelman, J. Ethics at phase 0: clarifying the issues. J Law Med Ethics 35, 727-733, 514 (2007).

229       Hah, S. S., Sumbad, R. A., de Vere White, R. W., Turteltaub, K. W. & Henderson, P. T. Characterization of oxaliplatin-DNA adduct formation in DNA and differentiation of cancer cell drug sensitivity at microdose concentrations. Chem Res Toxicol 20, 1745-1751 (2007).

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239       Lee, C. M. & Farde, L. Using positron emission tomography to facilitate CNS drug development. Trends in pharmacological sciences 27, 310-316 (2006).

240       Lappin, G. et al. Use of microdosing to predict pharmacokinetics at the therapeutic dose: Experience with 5 drugs. Clin Pharmacol Ther 80, 203-215 (2006).

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244       Bauer, M. et al. A positron emission tomography microdosing study with a potential antiamyloid drug in healthy volunteers and patients with Alzheimer's disease. Clin Pharmacol Ther 80, 216-227 (2006).

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246       Wilding, I. R. & Bell, J. A. Improved early clinical development through human microdosing studies. Drug Discov Today 10, 890-894 (2005).

247       Sarapa, N., Hsyu, P. H., Lappin, G. & Garner, R. C. The application of accelerator mass spectrometry to absolute bioavailability studies in humans: simultaneous administration of an intravenous microdose of 14C-nelfinavir mesylate solution and oral nelfinavir to healthy volunteers. J Clin Pharmacol 45, 1198-1205 (2005).

248       Garner, R. C. Less is more: the human microdosing concept. Drug Discov Today 10, 449-451 (2005).

249       Friend, D. R. New oral delivery systems for treatment of inflammatory bowel disease. Adv Drug Deliv Rev 57, 247-265 (2005).

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252       Walker, D. K. The use of pharmacokinetic and pharmacodynamic data in the assessment of drug safety in early drug development. Br J Clin Pharmacol 58, 601-608 (2004).

253       Sandhu, P. et al. Evaluation of microdosing strategies for studies in preclinical drug development: demonstration of linear pharmacokinetics in dogs of a nucleoside analog over a 50-fold dose range. Drug Metab Dispos 32, 1254-1259 (2004).

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