[68Ga]Ga-PSMA-11: The First FDA-Approved 68Ga-Radiopharmaceutical for PET Imaging of Prostate Cancer
Abstract
:1. Introduction
2. Chemical Overview
2.1. Names and Chemical Structure of [68Ga]Ga-PSMA-11
2.2. Gallium-68
2.3. Production and Quality Control of [68Ga]Ga-PSMA-11
3. Medicinal and Pharmaceutical Overview
3.1. Clinical Indication
3.2. Application
3.3. Pharmacology and Pharmacokinetics
4. Perspective
5. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
- FDA Letter of Approval for [68Ga]Ga-PSMA-11. Available online: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212642Orig1s000TOC.cfm (accessed on 31 May 2021).
- Minner, S.; Wittmer, C.; Graefen, M.; Salomon, G.; Steuber, T.; Haese, A.; Huland, H.; Bokemeyer, C.; Yekebas, E.; Dierlamm, J. High level PSMA expression is associated with early PSA recurrence in surgically treated prostate cancer. Prostate 2011, 71, 281–288. [Google Scholar] [CrossRef] [PubMed]
- Ross, J.S.; Sheehan, C.E.; Fisher, H.A.G.; Kaufman, R.P., Jr.; Kaur, P.; Gray, K.; Webb, I.; Gray, G.S.; Mosher, R.; Kallakury, B.V.S. Correlation of primary tumor prostate-specific membrane antigen expression with disease recurrence in prostate cancer. Clin. Cancer Res. 2003, 9, 6357–6362. [Google Scholar]
- Perner, S.; Hofer, M.D.; Kim, R.; Shah, R.B.; Li, H.; Möller, P.; Hautmann, R.E.; Gschwend, J.E.; Kuefer, R.; Rubin, M.A. Prostate-specific membrane antigen expression as a predictor of prostate cancer progression. Hum. Pathol. 2007, 38, 696–701. [Google Scholar] [CrossRef] [PubMed]
- Tomlins, S.A.; Mehra, R.; Rhodes, D.R.; Cao, X.; Wang, L.; Dhanasekaran, S.M.; Kalyana-Sundaram, S.; Wei, J.T.; Rubin, M.A.; Pienta, K.J. Integrative molecular concept modeling of prostate cancer progression. Nat. Genet. 2007, 39, 41–51. [Google Scholar] [CrossRef] [PubMed]
- Pomper, M.G.; Musachio, J.L.; Zhang, J.; Scheffel, U.; Zhou, Y.; Hilton, J.; Maini, A.; Dannals, R.F.; Wong, D.F.; Kozikowski, A.P. 11C-MCG: Synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase). Mol. Imaging 2002, 1, 96–101. [Google Scholar] [CrossRef] [PubMed]
- Foss, C.A.; Mease, R.C.; Fan, H.; Wang, Y.; Ravert, H.T.; Dannals, R.F.; Olszewski, R.T.; Heston, W.D.; Kozikowski, A.P.; Pomper, M.G. Radiolabeled small-molecule ligands for prostate-specific membrane antigen: In Vivo imaging in experimental models of prostate cancer. Clin. Cancer Res. 2005, 11, 4022–4028. [Google Scholar] [CrossRef] [Green Version]
- Pandit-Taskar, N.; O’Donoghue, J.A.; Durack, J.C.; Lyashchenko, S.K.; Cheal, S.M.; Beylergil, V.; Lefkowitz, R.A.; Carrasquillo, J.A.; Martinez, D.F.; Fung, A.M.; et al. A Phase I/II Study for Analytic Validation of 89Zr-J591 ImmunoPET as a Molecular Imaging Agent for Metastatic Prostate Cancer. Clin. Cancer Res. 2015, 21, 5277–5285. [Google Scholar] [CrossRef] [Green Version]
- Mease, R.C.; Dusich, C.L.; Foss, C.A.; Ravert, H.T.; Dannals, R.F.; Seidel, J.; Prideaux, A.; Fox, J.J.; Sgouros, G.; Kozikowski, A.P.; et al. N-[N-[(S)-1,3-Dicarboxypropyl]carbamoyl]-4-[18F]fluorobenzyl-L-cysteine, [18F]DCFBC: A new imaging probe for prostate cancer. Clin. Cancer Res. 2008, 14, 3036–3043. [Google Scholar] [CrossRef] [Green Version]
- Chen, Y.; Pullambhatla, M.; Foss, C.A.; Byun, Y.; Nimmagadda, S.; Senthamizhchelvan, S.; Sgouros, G.; Mease, R.C.; Pomper, M.G. 2-(3-{1-Carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid, [18F]DCFPyL, a PSMA-based PET Imaging Agent for Prostate Cancer. Clin. Cancer Res. 2011, 17, 7645–7653. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Giesel, F.L.; Kesch, C.; Yun, M.; Cardinale, J.; Haberkorn, U.; Kopka, K.; Kratochwil, C.; Hadaschik, B.A. 18F-PSMA-1007 PET/CT Detects Micrometastases in a Patient with Biochemically Recurrent Prostate Cancer. Clin. Genitourin Cancer 2017, 15, e497–e499. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Cardinale, J.; Schäfer, M.; Benešová, M.; Bauder-Wüst, U.; Leotta, K.; Eder, M.; Neels, O.C.; Haberkorn, U.; Giesel, F.L.; Kopka, K. Preclinical evaluation of 18F-PSMA-1007: A new PSMA ligand for prostate cancer imaging. J. Nucl. Med. 2017, 58, 425–431. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Eder, M.; Schäfer, M.; Bauder-Wüst, U.; Hull, W.-E.; Wängler, C.; Mier, W.; Haberkorn, U.; Eisenhut, M. 68Ga-Complex Lipophilicity and the Targeting Property of a Urea-Based PSMA Inhibitor for PET Imaging. Bioconj. Chem. 2012, 23, 688–697. [Google Scholar] [CrossRef]
- Benešová, M.; Bauder-Wüst, U.; Schäfer, M.; Klika, K.D.; Mier, W.; Haberkorn, U.; Kopka, K.; Eder, M. Linker Modification Strategies to Control the Prostate-Specific Membrane Antigen (PSMA)-Targeting and Pharmacokinetic Properties of DOTA-Conjugated PSMA Inhibitors. J. Med. Chem. 2016, 59, 1761–1775. [Google Scholar] [CrossRef] [PubMed]
- Afshar-Oromieh, A.; Haberkorn, U.; Eder, M.; Eisenhut, M.; Zechmann, C.M. [68Ga]Gallium-labelled PSMA ligand as superior PET tracer for the diagnosis of prostate cancer: Comparison with 18F-FECH. Eur. J. Nucl. Med. Mol. Imaging 2012, 39, 1085–1086. [Google Scholar] [CrossRef] [PubMed]
- Kratochwil, C.; Giesel, F.L.; Stefanova, M.; Benešová, M.; Bronzel, M.; Afshar-Oromieh, A.; Mier, W.; Eder, M.; Kopka, K.; Haberkorn, U. PSMA-Targeted Radionuclide Therapy of Metastatic Castration-Resistant Prostate Cancer with 177Lu-Labeled PSMA-617. J. Nucl. Med. 2016, 57, 1170–1176. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Fendler, W.P.; Schmidt, D.F.; Wenter, V.; Thierfelder, K.M.; Zach, C.; Stief, C.; Bartenstein, P.; Kirchner, T.; Gildehaus, F.J.; Gratzke, C.; et al. 68Ga-PSMA PET/CT Detects the Location and Extent of Primary Prostate Cancer. J. Nucl. Med. 2016, 57, 1720–1725. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Sterzing, F.; Kratochwil, C.; Fiedler, H.; Katayama, S.; Habl, G.; Kopka, K.; Afshar-Oromieh, A.; Debus, J.; Haberkorn, U.; Giesel, F.L. (68)Ga-PSMA-11 PET/CT: A new technique with high potential for the radiotherapeutic management of prostate cancer patients. Eur. J. Nucl. Med. Mol. Imaging 2016, 43, 34–41. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Zamboglou, C.; Eiber, M.; Fassbender, T.R.; Eder, M.; Kirste, S.; Bock, M.; Schilling, O.; Reichel, K.; van der Heide, U.A.; Grosu, A.L. Multimodal imaging for radiation therapy planning in patients with primary prostate cancer. Phys. Imaging Radiat. Oncol. 2018, 8, 8–16. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Zamboglou, C.; Sachpazidis, I.; Koubar, K.; Drendel, V.; Wiehle, R.; Kirste, S.; Mix, M.; Schiller, F.; Mavroidis, P.; Meyer, P.T.; et al. Evaluation of intensity modulated radiation therapy dose painting for localized prostate cancer using (68)Ga-HBED-CC PSMA-PET/CT: A planning study based on histopathology reference. Radiother. Oncol. 2017, 123, 472–477. [Google Scholar] [CrossRef] [Green Version]
- Zamboglou, C.; Drendel, V.; Jilg, C.A.; Rischke, H.C.; Beck, T.I.; Schultze-Seemann, W.; Krauss, T.; Mix, M.; Schiller, F.; Wetterauer, U.; et al. Comparison of (68)Ga-HBED-CC PSMA-PET/CT and multiparametric MRI for gross tumour volume detection in patients with primary prostate cancer based on slice by slice comparison with histopathology. Theranostics 2017, 7, 228–237. [Google Scholar] [CrossRef]
- Afshar-Oromieh, A.; Zechmann, C.M.; Malcher, A.; Eder, M.; Eisenhut, M.; Linhart, H.G.; Holland-Letz, T.; Hadaschik, B.A.; Giesel, F.L.; Debus, J.; et al. Comparison of PET imaging with a (68)Ga-labelled PSMA ligand and (18)F-choline-based PET/CT for the diagnosis of recurrent prostate cancer. Eur. J. Nucl. Med. Mol. Imaging 2014, 41, 11–20. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Schwenck, J.; Rempp, H.; Reischl, G.; Kruck, S.; Stenzl, A.; Nikolaou, K.; Pfannenberg, C.; la Fougère, C. Comparison of 68Ga-labelled PSMA-11 and 11C-choline in the detection of prostate cancer metastases by PET/CT. Eur. J. Nucl. Med. Mol. Imaging 2017, 44, 92–101. [Google Scholar] [CrossRef] [PubMed]
- Afshar-Oromieh, A.; Livorsi da Cunha, M.; Wagner, J.; Haberkorn, U.; Debus, N.; Weber, W.; Eiber, M.; Holland-Letz, T.; Rauscher, I. Performance of [68Ga]Ga-PSMA-11 PET/CT in patients with recurrent prostate cancer after prostatectomy—a multicentre evaluation of 2533 patients. Eur. J. Nucl. Med. Mol. Imaging 2021, 1–10. [Google Scholar] [CrossRef]
- Farolfi, A.; Gafita, A.; Calais, J.; Eiber, M.; Afshar-Oromieh, A.; Spohn, F.; Barbato, F.; Weber, M.; Ilhan, M.; Cervati, V.; et al. (68)Ga-PSMA-11 Positron Emission Tomography Detects Residual Prostate Cancer after Prostatectomy in a Multicenter Retrospective Study. J. Urol. 2019, 202, 1174–1181. [Google Scholar] [CrossRef]
- Afshar-Oromieh, A.; Holland-Letz, T.; Giesel, F.L.; Kratochwil, C.; Mier, W.; Haufe, S.; Debus, N.; Eder, M.; Eisenhut, M.; Schäfer, M.; et al. Diagnostic performance of 68Ga-PSMA-11 (HBED-CC) PET/CT in patients with recurrent prostate cancer: Evaluation in 1007 patients. Eur. J. Nucl. Med. Mol. Imaging 2017, 44, 1258–1268. [Google Scholar] [CrossRef] [Green Version]
- Fendler, W.P.; Ferdinandus, J.; Czernin, J.; Eiber, M.; Flavell, R.R.; Behr, S.C.; Wu, I.K.; Lawhn-Heath, C.; Pampaloni, M.H.; Reiter, R.E.; et al. Impact of (68)Ga-PSMA-11 PET on the Management of Recurrent Prostate Cancer in a Prospective Single-Arm Clinical Trial. J. Nucl. Med. 2020, 61, 1793–1799. [Google Scholar] [CrossRef] [PubMed]
- Sonni, I.; Eiber, M.; Fendler, W.P.; Alano, R.M.; Vangala, S.S.; Kishan, A.U.; Nickols, N.; Rettig, M.B.; Reiter, R.E.; Czernin, J.; et al. Impact of (68)Ga-PSMA-11 PET/CT on Staging and Management of Prostate Cancer Patients in Various Clinical Settings: A Prospective Single-Center Study. J. Nucl. Med. 2020, 61, 1153–1160. [Google Scholar] [CrossRef] [PubMed]
- Eiber, M.; Herrmann, K.; Calais, J.; Hadaschik, B.; Giesel, F.L.; Hartenbach, M.; Hope, T.; Reiter, R.; Maurer, T.; Weber, W.A.; et al. Prostate Cancer Molecular Imaging Standardized Evaluation (PROMISE): Proposed miTNM Classification for the Interpretation of PSMA-Ligand PET/CT. J. Nucl. Med. 2018, 59, 469–478. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Fendler, W.P.; Eiber, M.; Beheshti, M.; Bomanji, J.; Ceci, F.; Cho, S.; Giesel, F.; Haberkorn, U.; Hope, T.A.; Kopka, K.; et al. (68)Ga-PSMA PET/CT: Joint EANM and SNMMI procedure guideline for prostate cancer imaging: Version 1.0. Eur. J. Nucl. Med. Mol. Imaging 2017, 44, 1014–1024. [Google Scholar] [CrossRef]
- Carlucci, G.; Ippisch, R.; Slavik, R.; Mishoe, A.; Blecha, J.; Zhu, S. 68Ga-PSMA-11 NDA Approval: A Novel and Successful. Acad. Partnersh. J. Nucl. Med. 2021, 62, 149–155. [Google Scholar] [CrossRef] [PubMed]
- Schuhmacher, J.; Klivényi, G.; Hull, W.E.; Matys, R.; Hauser, H.; Kalthoff, H.; Schmiegel, W.H.; Maier-Borst, W.; Matzku, S. A bifunctional HBED-derivative for labeling of antibodies with 67Ga, 111In and 59Fe. Comparative biodistribution with 111In-DPTA and 131I-labeled antibodies in mice bearing antibody internalizing and non-internalizing tumors. Int. J. Rad. Appl. Instrum. B 1992, 19, 809–824. [Google Scholar] [CrossRef]
- Eder, M.; Neels, O.; Müller, M.; Bauder-Wüst, U.; Remde, Y.; Schäfer, M.; Hennrich, U.; Eisenhut, M.; Afshar-Oromieh, A.; Haberkorn, U.; et al. Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer. Pharmaceuticals 2014, 7, 779–796. [Google Scholar] [CrossRef] [PubMed]
- Decay Characteristics of 68Ga. Available online: https://www.nndc.bnl.gov/nudat2/dec_searchi.jsp (accessed on 20 May 2021).
- Sanchez-Crespo, A. Comparison of Gallium-68 and Fluorine-18 imaging characteristics in positron emission tomography. Appl. Rad. Isot. 2013, 76, 55–62. [Google Scholar] [CrossRef] [PubMed]
- Brandt, M.; Cardinale, J.; Aulsebrook, M.L.; Gasser, G.; Mindt, T.L. An Overview of PET Radiochemistry, Part 2: Radiometals. J. Nucl. Med. 2018, 59, 1500–1506. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Gallium-68 Cyclotron Production. IAEA-TECDOC-1863. Available online: https://www.researchgate.net/publication/331035585_Gallium-68_Cyclotron_Production (accessed on 20 May 2021).
- Kumar, K. The Current Status of the Production and Supply of Gallium-68. Cancer Biother. Radiopharm. 2020, 35, 163–165. [Google Scholar] [CrossRef]
- Rodnick, M.E.; Sollert, C.; Stark, D.; Clark, M.; Katsifis, A.; Hockley, B.G.; Parr, D.C.; Frigell, J.; Henderson, B.D.; Abghari-Gerst, M.; et al. Cyclotron-based production of 68Ga, [68Ga]GaCl3, and [68Ga]Ga-PSMA-11 from a liquid target. EJNMMI Radiopharm. Chem. 2020, 5, 25. [Google Scholar] [CrossRef] [PubMed]
- Thisgaard, H.; Kumlin, J.; Langkjær, N.; Chua, J.; Hook, B.; Jensen, M.; Kassaian, A.; Zeisler, S.; Borjian, S.; Cross, M.; et al. Multi-curie production of gallium-68 on a biomedical cyclotron and automated radiolabelling of PSMA-11 and DOTATATE. EJNMMI Radiopharm. Chem. 2021, 6. [Google Scholar] [CrossRef]
- European Pharmacopeia, Monograph Gallium (68Ga) Chloride Solution for Radiolabelling (01/2021:3109). European Pharmacopeia, 10th Edition. 2020. Available online: https://extranet.edqm.eu/4DLink1/4DCGI/Web_View/mono/2464 (accessed on 15 July 2021).
- TLX591-CDX. Available online: https://telixpharma.com/pipeline/tlx591-cdx-illumet/ (accessed on 4 May 2021).
- isoPROtrace-11. Available online: https://isotopia.co.il/products/isoprotrace-11/ (accessed on 4 May 2021).
- Calderoni, L.; Farolfi, A.; Pianori, D.; Maietti, E.; Cabitza, V.; Lambertini, A.; Ricci, G.; Telo, S.; Lodi, F.; Castellucci, P.; et al. Evaluation of an Automated Module Synthesis and a Sterile Cold Kit–Based Preparation of 68Ga-PSMA-11 in Patients with Prostate Cancer. J. Nucl. Med. 2020, 61, 716–722. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Satpati, D. Recent Breakthrough in 68Ga-Radiopharmaceuticals Cold Kits for Convenient PET Radiopharmacy. Bioconj. Chem. 2021, 32, 430–447. [Google Scholar] [CrossRef] [PubMed]
- Kurash, M.M.; Gill, R.; Khairulin, M.; Harbosh, H.; Keidar, Z. 68Ga-labeled PSMA-11 (68Ga-isoPROtrace-11) synthesized with ready to use kit: Normal biodistribution and uptake characteristics of tumour lesions. Nat. Res. 2020, 10, 3109. [Google Scholar] [CrossRef] [Green Version]
- European Pharmacopeia Monograph “Gallium 68 PSMA-11 Injection Solution” (04/2021:3044). European Pharmacopeia, 10th Edition. 2020. Available online: https://www.edqm.eu/en/european-pharmacopoeia-ph-eur-10th-edition (accessed on 28 May 2021).
- Label for “Gallium Ga 68 PSMA-11 Injection”. Available online: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212642Orig1s000lbl.pdf (accessed on 16 March 2021).
- Afshar-Oromieh, A.; Malcher, A.; Eder, M.; Eisenhut, M.; Linhart, H.G.; Hadaschik, B.A.; Holland-Letz, T.; Giesel, F.L.; Kratochwil, C.; Haufe, S.; et al. PET imaging with a [(68)Ga]gallium-labelled PSMA ligand for the diagnosis of prostate cancer: Biodistribution in humans and first evaluation of tumour lesions. Eur. J. Nucl. Med. Mol. Imaging 2013, 40, 486–495. [Google Scholar] [CrossRef]
- Tönnesmann, R.; Meyer, P.T.; Eder, M.; Baranski, A.-C. [(177)Lu]Lu-PSMA-617 Salivary Gland Uptake Characterized by Quantitative In Vitro Autoradiography. Pharmaceuticals 2019, 12, 18. [Google Scholar] [CrossRef] [Green Version]
- Rupp, N.J.; Umbricht, C.A.; Pizzuto, D.A.; Lenggenhager, D.; Töpfer, A.; Müller, J.; Muehlematter, U.J.; Ferraro, D.A.; Messerli, M.; Morand, G.B.; et al. First Clinicopathologic Evidence of a Non-PSMA-Related Uptake Mechanism for (68)Ga-PSMA-11 in Salivary Glands. J. Nucl. Med. 2019, 60, 1270–1276. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Kratochwil, C.; Bruchertseifer, F.; Rathke, H.; Bronzel, M.; Apostolidis, C.; Weichert, W.; Haberkorn, U.; Giesel, F.L.; Morgenstern, A. Targeted alpha-Therapy of Metastatic Castration-Resistant Prostate Cancer with 225Ac-PSMA-617: Dosimetry Estimate and Empiric Dose Finding. J. Nucl. Med. 2017, 58, 1624–1631. [Google Scholar] [CrossRef] [PubMed] [Green Version]
- Afshar-Oromieh, A.; Hetzheim, H.; Kübler, W.; Kratochwil, C.; Giesel, F.L.; Hope, T.A.; Eder, M.; Eisenhut, M.; Kopka, K.; Haberkorn, U. Radiation dosimetry of 68Ga-PSMA-11 (HBED-CC) and preliminary evaluation of optimal imaging timing. Eur. J. Nucl. Med. Mol. Imaging 2016, 43, 1611–1620. [Google Scholar] [CrossRef] [PubMed]
- Hofman, M.S.; Lawrentschuk, N.; Francis, R.J.; Tang, C.; Vela, I.; Thomas, P.; Rutherford, N.; Martin, J.M.; Frydenberg, M.; Shakher, R.; et al. Prostate-specific membrane antigen PET-CT in patients with high-risk prostate cancer before curative-intent surgery or radiotherapy (proPSMA): A prospective, randomised, multicentre study. Lancet 2020, 395, 1208–1216. [Google Scholar] [CrossRef]
- Eder, A.-C.; Omrane, M.A.; Stadlbauer, S.; Roscher, M.; Khoder, W.Y.; Gratzke, C.; Kopka, K.; Eder, M.; Meyer, P.T.; Jilg, C.A.; et al. The PSMA-11-derived hybrid molecule PSMA-914 specifically identifies prostate cancer by preoperative PET/CT and intraoperative fluorescence imaging. Eur. J. Nucl. Med. Mol. Imaging 2021, 48, 2057–2058. [Google Scholar] [CrossRef] [PubMed]
- Eiber, M.; Weirich, G.; Holzapfel, K.; Souvatzoglou, M.; Haller, B.; Rauscher, I.; Beer, A.J.; Wester, H.-J.; Gschwend, J.; Schwaiger, M.; et al. Simultaneous 68Ga-PSMA HBED-CC PET/MRI Improves the Localization of Primary Prostate Cancer. Eur. Urol. 2016, 70, 829–836. [Google Scholar] [CrossRef] [PubMed]
- Gorin, M.A.; Rowe, S.P.; Patel, H.D.; Vidal, I.; Mana-Ay, M.; Javadi, M.S.; Solnes, L.B.; Ross, A.E.; Schaeffer, E.M.; Bivalacqua, T.J.; et al. Prostate Specific Membrane Antigen Targeted (18)F-DCFPyL Positron Emission Tomography/Computerized Tomography for the Preoperative Staging of High Risk Prostate Cancer: Results of a Prospective, Phase II, Single Center Study. J. Urol. 2018, 199, 126–132. [Google Scholar] [CrossRef] [Green Version]
- Ferreira, G.; Iravani, A.; Hofman, M.S.; Hicks, R.J. Intra-individual comparison of (68)Ga-PSMA-11 and (18)F-DCFPyL normal-organ biodistribution. Cancer Imaging 2019, 19, 23. [Google Scholar] [CrossRef] [PubMed]
- Rahbar, K.; Afshar-Oromieh, A.; Bögemann, M.; Wagner, S.; Schäfers, M.; Stegger, L.; Weckesser, M. (18)F-PSMA-1007 PET/CT at 60 and 120 min in patients with prostate cancer: Biodistribution, tumour detection and activity kinetics. Eur. J. Nucl. Med. Mol. Imaging 2018, 45, 1329–1334. [Google Scholar] [CrossRef] [PubMed]
- Kesch, C.; Vinsensia, M.; Radtke, J.P.; Schlemmer, H.P.; Heller, M.; Ellert, E.; Holland-Letz, T.; Duensing, S.; Grabe, N.; Afshar-Oromieh, A. Intraindividual Comparison of 18F-PSMA-1007 PET/CT, Multiparametric MRI, and Radical Prostatectomy Specimens in Patients with Primary Prostate Cancer: A Retrospective, Proof-of-Concept Study. J. Nucl. Med. 2017, 58, 1805–1810. [Google Scholar] [CrossRef] [PubMed] [Green Version]
Parameter | Acceptance Criteria |
---|---|
Appearance | Clear, colorless solution |
Radiochemical Identity | Similar retention time to Ga-PSMA-11 reference standard |
Radiochemical Purity | HPLC ≥ 95% |
TLC [68Ga]Ga3+ ≤ 3% | |
Chemical Purity—PSMA-11 Related | PSMA-11 < 30 µg/Vmax 1 |
Sum of related impurities 2 ≤ area of reference peak 3 | |
Disregard limit for peak areas ≤ 0.1 × area of reference peak ³ | |
Chemical Purity—Other Substances | HEPES 4 ≤ 500 µg/Vmax 1 |
Ethanol ≤ 10% V/V | |
pH Value | 4–8 |
Endotoxin Content | 175/Vmax 1 IU/mL |
Radionuclidic Purity | Half-life, 61–74 min |
Gammaspectroscopy 5 511, 1022, and 1077 keV lines | |
90–110% of declared 68Ga radioactivity | |
Sterility 5 | Sterile |
Organ | Absorbed Dose (mGy/MBq) Mean (±SD) |
---|---|
Small Intestine | 0.0163 (±0.0022) |
Upper Colon | 0.0540 (±0.0416) |
Kidneys | 0.2620 (±0.0984) |
Liver | 0.0309 (±0.0042) |
Muscle | 0.0105 (±0.0004) |
Red Marrow | 0.0092 (±0.0003) |
Spleen | 0.0446 (±0.0209) |
Testes | 0.0104 (±0.0006) |
Urinary Bladder | 0.1300 (±0.0341) |
Total Body | 0.0124 (±0.0004) |
Effective Dose (mSv/MBq) | 0.0230 (±0.0036) |
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Hennrich, U.; Eder, M. [68Ga]Ga-PSMA-11: The First FDA-Approved 68Ga-Radiopharmaceutical for PET Imaging of Prostate Cancer. Pharmaceuticals 2021, 14, 713. https://doi.org/10.3390/ph14080713
Hennrich U, Eder M. [68Ga]Ga-PSMA-11: The First FDA-Approved 68Ga-Radiopharmaceutical for PET Imaging of Prostate Cancer. Pharmaceuticals. 2021; 14(8):713. https://doi.org/10.3390/ph14080713
Chicago/Turabian StyleHennrich, Ute, and Matthias Eder. 2021. "[68Ga]Ga-PSMA-11: The First FDA-Approved 68Ga-Radiopharmaceutical for PET Imaging of Prostate Cancer" Pharmaceuticals 14, no. 8: 713. https://doi.org/10.3390/ph14080713