Molecular imaging with SPECT as a tool for drug development

Advanced Drug Delivery Reviews

Volumn 63, Issue 7, 2011, Pages 547-554

  Gomes, Célia M ^a   Abrunhosa, Antero J ^b   Ramos, Pedro ^a   Pauwels, Ernest K J ^c  

^a UNIVERSITY OF COIMBRA   (Portugal)

^b UNIVERSITY OF COIMBRA   (Portugal)

^c LEIDEN UNIVERSITY MEDICAL CENTER   (Netherlands)

Author keywords

Drug development; Imaging biomarkers; Microdosing; Pharmacokinetics; SPECT

Indexed keywords

BIODISTRIBUTIONS; CLINICAL TESTING; CLINICAL TRIAL; DRUG CANDIDATES; DRUG DEVELOPMENT; HIGH SENSITIVITY; IMAGING BIOMARKERS; IMAGING MODALITY; IN-VIVO; INITIAL STAGES; INVESTIGATIONAL NEW DRUGS; MICRODOSING; MOLECULAR IMAGING; OVERALL EFFICIENCY; POTENTIAL APPLICATIONS; PRECLINICAL DEVELOPMENT; SPECT; SPECT IMAGING; THERAPEUTIC DOSE;

DRUG DOSAGE; DRUG PRODUCTS; IMAGING TECHNIQUES; MULTIPHOTON PROCESSES; PHARMACOKINETICS; POSITRON EMISSION TOMOGRAPHY;

SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY;

ANTIBODY; ANTIDEPRESSANT AGENT; BIOLOGICAL MARKER; CARBON 11; CENTRAL NERVOUS SYSTEM AGENTS; COPPER 64; DEPREOTIDE TC 99M; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; FLUORINE 18; GALLIUM 67; IMATINIB; INDIUM 111; IODINE 123; IODINE 124; MOLYBDENUM 99; NEUROLEPTIC AGENT; NITROGEN 13; OCTREOTIDE; OXYGEN 15; RECEPTOR PROTEIN; SOMATOSTATIN RECEPTOR; TECHNETIUM 99M; TOSITUMOMAB I 131; TRASTUZUMAB;

APOPTOSIS; BREAST CANCER; CANCER RADIOTHERAPY; DRUG DEVELOPMENT; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG METABOLISM; DRUG MICRODOSE; DRUG RESEARCH; DRUG UPTAKE; GAMMA RADIATION; GASTROINTESTINAL STROMAL TUMOR; HUMAN; IMAGE RECONSTRUCTION; IMMUNOSCINTIGRAPHY; ISOTOPE LABELING; MOLECULAR IMAGING; NONHUMAN; PHARMACOKINETICS; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROTEIN TARGETING; REVIEW; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; TUMOR GROWTH; TUMOR VASCULARIZATION;

ANIMALS; CLINICAL TRIALS AS TOPIC; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; DRUGS, INVESTIGATIONAL; HUMANS; POSITRON-EMISSION TOMOGRAPHY; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 79955445971     PISSN: 0169409X     EISSN: 0169409X     Source Type: Journal    
DOI: 10.1016/j.addr.2010.09.015     Document Type: Review

References (73)

1. Dimasi J.A., Hansen R.W., Grabowski H.G. The price of innovation: new estimates of drug development costs. J. Health Econ. 2003, 22(2):151-185.
2. Kola I., Landis J. Can the pharmaceutical industry reduce attrition rates?. Nat. Rev. Drug Discov. 2004, 3(8):711-715.
3. Johnson J.I., Decker S., Zaharevitz D., Rubinstein L.V., Venditti J.M., Schepartz S., Kalyandrug S., Christian M., Arbuck S., Hollingshead M., Sausville E.A. Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials. Br. J. Cancer 2001, 84(10):1424-1431.
4. Park J.W., Kerbel R.S., Kelloff G.J., Barrett J.C., Chabner B.A., Parkinson D.R., Peck J., Ruddon R.W., Sigman C.C., Slamon D.J. Rationale for biomarkers and surrogate end points in mechanism-driven oncology drug development. Clin. Cancer Res. 2004, 10(11):3885-3896.
5. Murgo A.J., Kummar S., Rubinstein L., Gutierrez M., Collins J., Kinders R., Parchment R.E., Ji J., Steinberg S.M., Yang S.X., Hollingshead M., Chen A., Helman L., Wiltrout R., Tomaszewski J.E., Doroshow J.H. Designing phase 0 cancer clinical trials. Clin. Cancer Res. 2008, 14(12):3675-3682.
6. Kinders R., Parchment R.E., Ji J., Kummar S., Murgo A.J., Gutierrez M., Collins J., Rubinstein L., Pickeral O., Steinberg S.M., Yang S., Hollingshead M., Chen A., Helman L., Wiltrout R., Simpson M., Tomaszewski J.E., Doroshow J.H. Phase 0 clinical trials in cancer drug development: from FDA guidance to clinical practice. Mol. Interv. 2007, 7(6):325-334.
7. Willmann J.K., van Bruggen N., Dinkelborg L.M., Gambhir S.S. Molecular imaging in drug development. Nat. Rev. Drug Discov. 2008, 7(7):591-607.
8. Rudin M., Weissleder R. Molecular imaging in drug discovery and development. Nat. Rev. Drug Discov. 2003, 2(2):123-131.
9. Rudin M. Imaging readouts as biomarkers or surrogate parameters for the assessment of therapeutic interventions. Eur. Radiol. 2007, 17(10):2441-2457.
10. Richter W.S. Imaging biomarkers as surrogate endpoints for drug development. Eur. J. Nucl. Med. Mol. Imaging 2006, 33(Suppl 1):6-10.
11. Lucignani G. Imaging biomarkers: from research to patient care-a shift in view. Eur. J. Nucl. Med. Mol. Imaging 2007, 34(10):1693-1697.
12. Madsen M.T. Recent advances in SPECT imaging. J. Nucl. Med. 2007, 48(4):661-673.
13. Wernick M.N., Aarsvold J.N. Emission Tomography: The Fundamentals of SPECT and PET 2004, Elsevier, San Diego, CA. 1st ed.
14. Difilippo F.P. Design and performance of a multi-pinhole collimation device for small animal imaging with clinical SPECT and SPECT-CT scanners. Phys. Med. Biol. 2008, 53(15):4185-4201.
15. O'Connor M.K., Kemp B.J. Single-photon emission computed tomography/computed tomography: basic instrumentation and innovations. Semin. Nucl. Med. 2006, 36(4):258-266.
16. Kummar S., Rubinstein L., Kinders R., Parchment R.E., Gutierrez M.E., Murgo A.J., Ji J., Mroczkowski B., Pickeral O.K., Simpson M., Hollingshead M., Yang S.X., Helman L., Wiltrout R., Collins J., Tomaszewski J.E., Doroshow J.H. Phase 0 clinical trials: conceptions and misconceptions. Cancer J. 2008, 14(3):133-137.
17. Dimasi J.A. Risks in new drug development: approval success rates for investigational drugs. Clin. Pharmacol. Ther. 2001, 69(5):297-307.
18. Fischman A.J., Alpert N.M., Rubin R.H. Pharmacokinetic imaging: a noninvasive method for determining drug distribution and action. Clin. Pharmacokinet. 2002, 41(8):581-602.
19. Wu A.M., Olafsen T. Antibodies for molecular imaging of cancer. Cancer J. 2008, 14(3):191-197.
20. Liersch T., Meller J., Kulle B., Behr T.M., Markus P., Langer C., Ghadimi B.M., Wegener W.A., Kovacs J., Horak I.D., Becker H., Goldenberg D.M. Phase II trial of carcinoembryonic antigen radioimmunotherapy with 131I-labetuzumab after salvage resection of colorectal metastases in the liver: five-year safety and efficacy results. J. Clin. Oncol. 2005, 23(27):6763-6770.
21. Akabani G., Cokgor I., Coleman R.E., Gonzalez T.D., Wong T.Z., Friedman H.S., Friedman A.H., Garcia-Turner A., Herndon J.E., DeLong D., McLendon R.E., Zhao X.G., Pegram C.N., Provenzale J.M., Bigner D.D., Zalutsky M.R. Dosimetry and dose-response relationships in newly diagnosed patients with malignant gliomas treated with iodine-131-labeled anti-tenascin monoclonal antibody 81C6 therapy. Int. J. Radiat. Oncol. Biol. Phys. 2000, 46(4):947-958.
22. Kenanova V., Olafsen T., Crow D.M., Sundaresan G., Subbarayan M., Carter N.H., Ikle D.N., Yazaki P.J., Chatziioannou A.F., Gambhir S.S., Williams L.E., Shively J.E., Colcher D., Raubitschek A.A., Wu A.M. Tailoring the pharmacokinetics and positron emission tomography imaging properties of anti-carcinoembryonic antigen single-chain Fv-Fc antibody fragments. Cancer Res. 2005, 65(2):622-631.
23. Chrastina A., Valadon P., Massey K.A., Schnitzer J.E. Lung vascular targeting using antibody to aminopeptidase P: CT-SPECT imaging, biodistribution and pharmacokinetic analysis. J. Vasc. Res. 2010, 47(6):531-543.
24. Vaneycken I., Govaert J., Vincke C., Caveliers V., Lahoutte T., De Baetselier P., Raes G., Bossuyt A., Muyldermans S., Devoogdt N. In vitro analysis and in vivo tumor targeting of a humanized, grafted nanobody in mice using pinhole SPECT/micro-CT. J. Nucl. Med. 2010, 51(7):1099-1106.
25. Garner R.C., Lappin G. The phase 0 microdosing concept. Br. J. Clin. Pharmacol. 2006, 61(4):367-370.
26. Pardridge W.M. Blood-brain barrier delivery. Drug Discov. Today 2007, 12(1-2):54-61.
27. Wong D.F., Tauscher J., Grunder G. The role of imaging in proof of concept for CNS drug discovery and development. Neuropsychopharmacology 2009, 34(1):187-203.
28. Brooks D.J. Positron emission tomography and single-photon emission computed tomography in central nervous system drug development. NeuroRx 2005, 2(2):226-236.
29. Pauwels E.K., Bergstrom K., Mariani G., Kairemo K. Microdosing, imaging biomarkers and SPECT: a multi-sided tripod to accelerate drug development. Curr. Pharm. Des. 2009, 15(9):928-934.
30. Talbot P.S., Laruelle M. The role of in vivo molecular imaging with PET and SPECT in the elucidation of psychiatric drug action and new drug development. Eur. Neuropsychopharmacol. 2002, 12(6):503-511.
31. Molecular Imaging and Contrast Agent Database. (MICAD) http://micad%20nih%20gov.
32. van Dort M.E., Rehemtulla A., Ross B.D. PET and SPECT imaging of tumor biology: new approaches towards oncology drug discovery and development. Curr. Comput. Aided Drug Des. 2008, 4(1):46-53.
33. de Jong M., Breeman W.A., Kwekkeboom D.J., Valkema R., Krenning E.P. Tumor imaging and therapy using radiolabeled somatostatin analogues. Acc. Chem. Res. 2009, 42(7):873-880.
34. Krenning E.P., Kooij P.P., Bakker W.H., Breeman W.A., Postema P.T., Kwekkeboom D.J., Oei H.Y., de Jong M., Visser T.J., Reijs A.E. Radiotherapy with a radiolabeled somatostatin analogue, [111In-DTPA-D-Phe1]-octreotide. A case history. Ann. NY Acad. Sci. 1994, 733:496-506.
35. Rodrigues M., Traub-Weidinger T., Li S., Ibi B., Virgolini I. Comparison of 111In-DOTA-DPhe1-Tyr3-octreotide and 111In-DOTA-lanreotide scintigraphy and dosimetry in patients with neuroendocrine tumours. Eur. J. Nucl. Med. Mol. Imaging 2006, 33(5):532-540.
36. Eberle A.N., Froidevaux S. Radiolabeled alpha-melanocyte-stimulating hormone analogs for receptor-mediated targeting of melanoma: from tritium to indium. J. Mol. Recognit. 2003, 16(5):248-254.
37. Bodei L., Ferone D., Grana C.M., Cremonesi M., Signore A., Dierckx R.A., Paganelli G. Peptide receptor therapies in neuroendocrine tumors. J. Endocrinol. Invest. 2009, 32(4):360-369.
38. National Cancer Institute. Breast Imaging Using Indium In 111 CHX-A DTPA Trastuzumab in Patients With Primary Cancer or Metastatic Cancer. 2007. http://clinicaltrials%20gov/ct2/show/NCT00474578.
39. Cheung M.C., Maceachern J.A., Haynes A.E., Meyer R.M., Imrie K. I-Tositumomab in lymphoma. Curr. Oncol. 2009, 16(5):32-47.
40. Lesko L.J., Atkinson A.J. Use of biomarkers and surrogate endpoints in drug development and regulatory decision making: criteria, validation, strategies. Annu. Rev. Pharmacol. Toxicol. 2001, 41:347-366.
41. Biomarkers Definitions Working Group Biomarkers and surrogate endpoints: preferred definitions and conceptual framework. Clin. Pharmacol. Ther. 2001, 69(3):89-95.
42. Peintinger F., Buzdar A.U., Kuerer H.M., Mejia J.A., Hatzis C., Gonzalez-Angulo A.M., Pusztai L., Esteva F.J., Dawood S.S., Green M.C., Hortobagyi G.N., Symmans W.F. Hormone receptor status and pathologic response of HER2-positive breast cancer treated with neoadjuvant chemotherapy and trastuzumab. Ann. Oncol. 2008, 19(12):2020-2025.
43. Rini B.I. Vascular endothelial growth factor-targeted therapy in metastatic renal cell carcinoma. Cancer 2009, 115(10 Suppl):2306-2312.
44. Capdeville R., Buchdunger E., Zimmermann J., Matter A. Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nat. Rev. Drug Discov. 2002, 1(7):493-502.
45. Rudin M. Noninvasive structural, functional, and molecular imaging in drug development. Curr. Opin. Chem. Biol. 2009, 13(3):360-371.
46. Bading J.R., Shields A.F. Imaging of cell proliferation: status and prospects. J. Nucl. Med. 2008, 49(Suppl 2):64S-80S.
47. Kwee S.A., DeGrado T.R., Talbot J.N., Gutman F., Coel M.N. Cancer imaging with fluorine-18-labeled choline derivatives. Semin. Nucl. Med. 2007, 37(6):420-428.
48. Kuwert T., Probst-Cousin S., Woesler B., Morgenroth C., Lerch H., Matheja P., Palkovic S., Schafers M., Wassmann H., Gullotta F., Schober O. Iodine-123-alpha-methyl tyrosine in gliomas: correlation with cellular density and proliferative activity. J. Nucl. Med. 1997, 38(10):1551-1555.
49. Jager P.L., Plaat B.E., de Vries E.G., Molenaar W.M., Vaalburg W., Piers D.A., Hoekstra H.J. Imaging of soft-tissue tumors using L-3-[iodine-123]iodo-alpha-methyl-tyrosine single photon emission computed tomography: comparison with proliferative and mitotic activity, cellularity, and vascularity. Clin. Cancer Res. 2000, 6(6):2252-2259.
50. Bergers G., Benjamin L.E. Tumorigenesis and the angiogenic switch. Nat. Rev. Cancer 2003, 3(6):401-410.
51. Van De W.C., Oltenfreiter R., De Winter O., Signore A., Slegers G., Dierckx R.A. Tumour angiogenesis pathways: related clinical issues and implications for nuclear medicine imaging. Eur. J. Nucl. Med. Mol. Imaging 2002, 29(5):699-709.
52. Cai W., Rao J., Gambhir S.S., Chen X. How molecular imaging is speeding up antiangiogenic drug development. Mol. Cancer Ther. 2006, 5(11):2624-2633.
53. Blankenberg F.G., Backer M.V., Levashova Z., Patel V., Backer J.M. In vivo tumor angiogenesis imaging with site-specific labeled (99m)Tc-HYNIC-VEGF. Eur. J. Nucl. Med. Mol. Imaging 2006, 33(7):841-848.
54. Backer M.V., Levashova Z., Patel V., Jehning B.T., Claffey K., Blankenberg F.G., Backer J.M. Molecular imaging of VEGF receptors in angiogenic vasculature with single-chain VEGF-based probes. Nat. Med. 2007, 13(4):504-509.
55. Hood J.D., Cheresh D.A. Role of integrins in cell invasion and migration. Nat. Rev. Cancer 2002, 2(2):91-100.
56. Yang J., Guo H., Gallazzi F., Berwick M., Padilla R.S., Miao Y. Evaluation of a Novel Arg-Gly-Asp-conjugated alpha-melanocyte stimulating hormone hybrid peptide for potential melanoma therapy. Bioconjug. Chem. 2009, 20(8):1634-1642.
57. Fani M., Psimadas D., Zikos C., Xanthopoulos S., Loudos G.K., Bouziotis P., Varvarigou A.D. Comparative evaluation of linear and cyclic 99mTc-RGD peptides for targeting of integrins in tumor angiogenesis. Anticancer Res. 2006, 26(1A):431-434.
58. Decristoforo C., Faintuch-Linkowski B., Rey A., von Guggenberg E., Rupprich M., Hernandez-Gonzales I., Rodrigo T., Haubner R. [99mTc]HYNIC-RGD for imaging integrin alphavbeta3 expression. Nucl. Med. Biol. 2006, 33(8):945-952.
59. Janssen M., Oyen W.J., Massuger L.F., Frielink C., Dijkgraaf I., Edwards D.S., Radjopadhye M., Corstens F.H., Boerman O.C. Comparison of a monomeric and dimeric radiolabeled RGD-peptide for tumor targeting. Cancer Biother. Radiopharm. 2002, 17(6):641-646.
60. Chen X., Liu S., Hou Y., Tohme M., Park R., Bading J.R., Conti P.S. MicroPET imaging of breast cancer alphav-integrin expression with 64Cu-labeled dimeric RGD peptides. Mol. Imaging Biol. 2004, 6(5):350-359.
61. Sancey L., Ardisson V., Riou L.M., Ahmadi M., Marti-Batlle D., Boturyn D., Dumy P., Fagret D., Ghezzi C., Vuillez J.P. In vivo imaging of tumour angiogenesis in mice with the alpha(v)beta (3) integrin-targeted tracer 99mTc-RAFT-RGD. Eur. J. Nucl. Med. Mol. Imaging 2007, 34(12):2037-2047.
62. Bach-Gansmo T., Danielsson R., Saracco A., Wilczek B., Bogsrud T.V., Fangberget A., Tangerud A., Tobin D. Integrin receptor imaging of breast cancer: a proof-of-concept study to evaluate 99mTc-NC100692. J. Nucl. Med. 2006, 47(9):1434-1439.
63. Dijkgraaf I., Kruijtzer J.A., Frielink C., Soede A.C., Hilbers H.W., Oyen W.J., Corstens F.H., Liskamp R.M., Boerman O.C. Synthesis and biological evaluation of potent alphavbeta3-integrin receptor antagonists. Nucl. Med. Biol. 2006, 33(8):953-961.
64. Haubner R., Wester H.J., Burkhart F., Senekowitsch-Schmidtke R., Weber W., Goodman S.L., Kessler H., Schwaiger M. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J. Nucl. Med. 2001, 42(2):326-336.
65. Hajra K.M., Liu J.R. Apoptosome dysfunction in human cancer. Apoptosis 2004, 9(6):691-704.
66. Hajra K.M., Tan L., Liu J.R. Defective apoptosis underlies chemoresistance in ovarian cancer. Adv. Exp. Med. Biol. 2008, 622:197-208.
67. Koopman G., Reutelingsperger C.P., Kuijten G.A., Keehnen R.M., Pals S.T., van Oers M.H. Annexin V for flow cytometric detection of phosphatidylserine expression on B cells undergoing apoptosis. Blood 1994, 84(5):1415-1420.
68. Lahorte C.M., Vanderheyden J.L., Steinmetz N., Van De W.C., Dierckx R.A., Slegers G. Apoptosis-detecting radioligands: current state of the art and future perspectives. Eur. J. Nucl. Med. Mol. Imaging 2004, 31(6):887-919.
69. van Dort M.E., Lee K.C., Hamilton C.A., Rehemtulla A., Ross B.D. Radiosynthesis and evaluation of 5-[125I]iodoindol-3-yl-beta-D-galactopyranoside as a beta-galactosidase imaging radioligand. Mol. Imaging 2008, 7(4):187-197.
70. Boersma H.H., Kietselaer B.L., Stolk L.M., Bennaghmouch A., Hofstra L., Narula J., Heidendal G.A., Reutelingsperger C.P. Past, present, and future of annexin A5: from protein discovery to clinical applications. J. Nucl. Med. 2005, 46(12):2035-2050.
71. Belhocine T., Steinmetz N., Hustinx R., Bartsch P., Jerusalem G., Seidel L., Rigo P., Green A. Increased uptake of the apoptosis-imaging agent (99m)Tc recombinant human Annexin V in human tumors after one course of chemotherapy as a predictor of tumor response and patient prognosis. Clin. Cancer Res. 2002, 8(9):2766-2774.
72. Kartachova M., Haas R.L., Olmos R.A., Hoebers F.J., van Zandwijk N., Verheij M. In vivo imaging of apoptosis by 99mTc-Annexin V scintigraphy: visual analysis in relation to treatment response. Radiother. Oncol. 2004, 72(3):333-339.
73. Kartachova M.S., Valdes Olmos R.A., Haas R.L., Hoebers F.J., van den Brekel M.W., van Zandwijk N., Herk M., Verheij M. Mapping of treatment-induced apoptosis in normal structures: 99mTc-Hynic-rh-annexin V SPECT and CT image fusion. Eur. J. Nucl. Med. Mol. Imaging 2006, 33(8):893-899.