Preclinical evaluation and first patient application of 99mTc-PSMA-I&S for SPECT imaging and radioguided surgery in prostate cancer

Journal of Nuclear Medicine

Volumn 58, Issue 2, 2017, Pages 235-242

  Robu, Stephanie ^a   Schottelius, Margret ^a   Eiber, Matthias ^b   Maurer, Tobias ^b   Gschwend, Jürgen ^b   Schwaiger, Markus ^b   Wester, Hans Jürgen ^a  

^a TECHNICAL UNIVERSITY OF MUNICH   (Germany)

^b TECHNICAL UNIVERSITY OF MUNICH   (Germany)

Author keywords

111In PSMA I T; 99mTc PSMA I S; Gamma probe; PSMA; Radioguided surgery; RGS; SPECT

Indexed keywords

PROSTATE SPECIFIC MEMBRANE ANTIGEN INDIUM IN 111; PROSTATE SPECIFIC MEMBRANE ANTIGEN TECHNETIUM TC 99M; RADIOPHARMACEUTICAL AGENT; TRACER; UNCLASSIFIED DRUG; GLUTAMATE CARBOXYPEPTIDASE II; GLUTAMATE CARBOXYPEPTIDASE II, HUMAN; MEMBRANE ANTIGEN; TECHNETIUM;

AGED; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BONE METASTASIS; CASE REPORT; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG METABOLISM; DRUG SYNTHESIS; DRUG UPTAKE; EVALUATION STUDY; HUMAN; HUMAN CELL; IC50; LIPOPHILICITY; LYMPH NODE METASTASIS; MALE; METABOLIC STABILITY; MOUSE; NONHUMAN; PRECLINICAL EVALUATION; PROSTATE CANCER; PROTEIN BINDING; RADIOSURGERY; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY-COMPUTED TOMOGRAPHY; ANIMAL; COMPUTER ASSISTED SURGERY; DIAGNOSTIC IMAGING; METABOLISM; PILOT STUDY; PROCEDURES; PROSTATECTOMY; PROSTATIC NEOPLASMS; SCID MOUSE; TREATMENT OUTCOME;

AGED; ANIMALS; ANTIGENS, SURFACE; GLUTAMATE CARBOXYPEPTIDASE II; HUMANS; MALE; MICE; MICE, SCID; PILOT PROJECTS; PROSTATECTOMY; PROSTATIC NEOPLASMS; RADIOPHARMACEUTICALS; SURGERY, COMPUTER-ASSISTED; TECHNETIUM; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON; TREATMENT OUTCOME;

EID: 85011967211     PISSN: 01615505     EISSN: 2159662X     Source Type: Journal    
DOI: 10.2967/jnumed.116.178939     Document Type: Article

References (37)

1. Wright GL, Grob BM, Haley C, et al. Upregulation of prostate-specific membrane antigen after androgen-deprivation therapy. Urology. 1996;48:326-334.
2. Perner S, Hofer MD, Kim R, et al. Prostate-specific membrane antigen expression as a predictor of prostate cancer progression. Hum Pathol. 2007;38: 696-701.
3. Lütje S, Heskamp S, Cornelissen AS, et al. PSMA ligands for radionuclide imaging and therapy of prostate cancer: clinical status. Theranostics. 2015;5:1388-1401.
4. Evangelista L, Zattoni F, Rossi E, Karnes RJ, Lowe V. Early detection of prostate cancer relapse by biochemistry and diagnostic imaging. Q J Nucl Med Mol Imaging. 2015;59:359-373.
5. Kiess AP, Banerjee SR, Mease RC, et al. Prostate-specific membrane antigen as a target for cancer imaging and therapy. Q J Nucl Med Mol Imaging. 2015;59:241-268.
6. Maurer T, Eiber M, Schwaiger M, Gschwend JE. Current use of PSMA-PET in prostate cancer management. Nat Rev Urol. 2016;13:226-235.
7. Maresca KP, Hillier SM, Lu GL, et al. Small molecule inhibitors of PSMA incorporating technetium-99m for imaging prostate cancer: effects of chelate design on pharmacokinetics. Inorg Chim Acta. 2012;389:168-175.
8. 99mTc-labeled small-molecule inhibitors of prostate-specific membrane antigen: pharmacokinetics and biodistribution studies in healthy subjects and patients with metastatic prostate cancer. J Nucl Med. 2014;55:1791-1798.
9. Eder M, Schafer M, Bauder-Wust U, et al. Ga-68-complex lipophilicity and the targeting property of a urea-based PSMA inhibitor for PET imaging. Bioconjug Chem. 2012;23:688-697.
10. Eiber M, Maurer T, Souvatzoglou M, et al. Evaluation of hybrid Ga-68-PSMA ligand PET/CT in 248 patients with biochemical recurrence after radical prostatectomy. J Nucl Med. 2015;56:668-674.
11. 68Ga-labelled PSMA ligand HBED-CC in the diagnosis of recurrent prostate cancer. Eur J Nucl Med Mol Imaging. 2015;42:197-209.
12. Mease RC, Dusich CL, Foss CA, et al. N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-4-[F-18]fluorobenzyl-L-cysteine, [F-18]DCFBC: a new imaging probe for prostate cancer. Clin Cancer Res. 2008;14:3036-3043.
13. 18F-DCFBC PET/CT for PSMA-based detection and characterization of primary prostate cancer. J Nucl Med. 2015;56: 1003-1010.
14. 18F]DCFPy L, a PSMA-based PET imaging agent for prostate cancer. Clin Cancer Res. 2011;17:7645-7653.
15. 18F]DCFPyL for prostatespecific membrane antigen (PSMA)-targeted PET imaging of prostate cancer. Mol Imaging Biol. 2015;17:565-574.
16. 68gallium-PSMA positron emission tomography compared to conventional imaging for lymph node staging of 130 consecutive patients with intermediate to high risk prostate cancer. J Urol. 2016;195:1436-1443.
17. 18F-DCFBC PET/CT to conventional imaging modalities for detection of hormone-naive and castration-resistant metastatic prostate cancer. J Nucl Med. 2016;57:46-53.
18. Eiber M, Weirich G, Holzapfel K, et al. Simultaneous Ga-PSMA HBED-CC PET/MRI improves the localization of primary prostate cancer. Eur Urol. January 18, 2016 [Epub ahead of print].
19. 131I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy. Eur J Nucl Med Mol Imaging. 2014;41:1280-1292.
20. Benesova M, Kratochwil C, Schafer M, et al. PSMA-617: a novel theranostic PSMA inhibitor for both diagnosis and endoradiotherapy of prostate cancer [abstract]. J Nucl Med. 2015;56(suppl 3):63.
21. Afshar-Oromieh A, Hetzheim H, Kratochwil C, et al. The theranostic PSMA ligand PSMA-617 in the diagnosis of prostate cancer by PET/CT: biodistribution in humans, radiation dosimetry, and first evaluation of tumor lesions. J Nucl Med. 2015;56:1697-1705.
22. 177Lu-labeled PSMA I&T: optimization of a PSMA-targeted theranostic concept and first proof-ofconcept human studies. J Nucl Med. 2015;56:1169-1176.
23. 177Lu labeled prostate specific membrane antigen ligand for imaging and therapy in patients with metastatic castration resistant prostate cancer. J Urol. 2016;196:382-391.
24. 111In]PSMA-I&T: expanding the spectrum of PSMA-I&T applications towards SPECT and radioguided surgery. EJNMMI Res. 2015;5.
25. Maurer T, Weirich G, Schottelius M, et al. Prostate-specific membrane antigenradioguided surgery for metastatic lymph nodes in prostate cancer. Eur Urol. 2015;68:530-534.
26. 99mTc-chelator engineering to improve tumour targeting properties of a HER2-specific affibody molecule. Eur J Nucl Med Mol Imaging. 2007;34:1843-1853.
27. Ray Banerjee S, Pullambhatla M, Foss CA, et al. Effect of chelators on the pharmacokinetics of Tc-99m-labeled imaging agents for the prostate-specific membrane antigen (PSMA). J Med Chem. 2013;56:6108-6121.
28. Weineisen M, Simecek J, Schottelius M, Schwaiger M, Wester HJ. Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer. EJNMMI Res. 2014;4:63-77.
29. Wang Y, Liu GZ, Hnatowich DJ. Methods for MAG3 conjugation and Tc-99m radiolabeling of biomolecules. Nat Protoc. 2006;1:1477-1480.
30. Baker RJ, Bellen JC, Fornasiero D, Penglis S. The preparation of Tc-99m tertiarybutylisonitrile (Tc-99m-Tbi) by a method suitable for routine clinical use. Int J Rad Appl Instrum B. 1986;13:527-532.
31. Chen Y, Foss CA, Byun Y, et al. Radiohalogenated prostate-specific membrane antigen (PSMA)-based ureas as imaging agents for prostate cancer. J Med Chem. 2008;51:7933-7943.
32. 99mTc-EDDA-HYNIC-D-Phe1, Tyr3]-octreotide, a somatostatin analog for tumor diagnosis. J Pharm Sci. 2004;93:2497-2506.
33. Taylor A, Eshima D, Christian PE, Wooten WW, Hansen L, Mcelvany K. Technetium-99m Mag3 kit formulation: preliminary-results in normal volunteers and patients with renal-failure. J Nucl Med. 1988;29:616-622.
34. Maresca K, Wang JC, Hillier S, et al. Development of a simple kit for Tc-99m-MIP-1404, a single amino acid chelate (SAAC II) derived small molecule inhibitor of prostate specific membrane antigen (PSMA) for imaging prostate cancer. J Nucl Med. 2012;53(suppl 1):523.
35. Maurer T, Weineisen M, Wester HJ, et al. Psma-radioguided surgery: introducing molecular surgery in patients with recurrent prostate cancer. J Urol. 2015;193: E1040-E1041.
36. 99mTc-labeled small-molecule inhibitors of prostate-specific membrane antigen for molecular imaging of prostate cancer. J Nucl Med. 2013;54:1369-1376.
37. van Oosterom MN, Simon H, Mengus L, et al. Revolutionizing (robot-assisted) laparoscopic gamma tracing using a drop-in gamma probe technology. Am J Nucl Med Mol Imaging. 2016;6:1-17.