Insight into the Development of PET Radiopharmaceuticals for Oncology
Abstract
:1. Introduction
2. Targeting Vectors
2.1. Probes Based on Bioactive Molecules
2.2. Probes Based on Drugs
2.3. Chemical Screens
3. Radiochemistry
3.1. Radiolabeling Strategies
3.2. Automation
3.3. Quality Control
4. Preclinical Experiments
4.1. Binding Affinity
4.2. Internalization and Efflux Assays
4.3. Stability
4.4. Plasma Protein Binding
4.5. Immunoreactivity
4.6. Antagonist and Agonist Assays
4.7. Imaging
4.8. Biodistribution by Dissection
4.9. Specificity
4.10. Time Points
4.11. Dosimetry
4.12. Toxicity
5. Regulatory Considerations
5.1. Nonclinical Evaluation of Radiopharmaceuticals
5.2. Exploratory Approaches for First-in-Human Studies
5.3. Marketing Authorization
6. Perspectives and Summary
Author Contributions
Funding
Conflicts of Interest
References
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Biological Process/Target | Radiopharmaceutical | Vector | Indication | References |
---|---|---|---|---|
A33 | [124I]I-huA33 | Antibody | Colorectal cancer | [13] |
Acetyl-CoA synthetase | [11C]acetate # | Salt | General cancers | [14] |
Amino acid transport | [11C]methionine # [18F]FDOPA # [18F]FET # [18F]FGln [18F]FSPG [18F]FACBC * [18F]FACPC | Amino acid | Glioma, neuroendocrine tumors, prostate cancer | [15,16,17,18,19,20,21,22,23] |
Androgen receptor (AR) | [18F]FDHT | Hormone | Prostate cancer | [24,25] |
Apoptosis | [18F]ML-10 [18F]ICMT-11 | Small molecule | Glioblastoma multiforme, breast cancer, lung cancer | [26,27] |
Bone remodeling | [18F]NaF *,# | Salt | Osseous lesions | [28] |
CA19.9 | [89Zr]Zr-DFO-HuMab-5B1 | Antibody | Pancreatic cancer and bladder cancer | [29] |
Carbonic anhydrase 9 (CA-IX) | [124I]I-girentuximab [89Zr]Zr-girentuximab | Antibody | Clear-cell renal cell carcinoma | [30,31,32] |
Carcinoembryonic antigen (CEA) | [89Zr]Zr-AMG 211 | Bispecific T-cell engager | Gastrointestinal adenocarcinoma | [33] |
CD8 | [89Zr]Zr-Df-IAB22M2C | Minibody | Melanoma, lung cancer, hepatocarcinoma | [34] |
CD20 | [89Zr]Zr-rituximab [89Zr]Zr-obinutuzumab | Antibody | B cell lymphoma | [35,36] |
CD44v6 | [89Zr]Zr-U36 | Antibody | Head and neck cancer | [37] |
C-X-C chemokine receptor type 4 (CXCR4) | [64Cu]Cu-plerixafor | Small molecule | Hematological and solid malignancies | [38,39,40] |
[68Ga]Ga-pentixafor [68Ga]Ga-NOTA-NFB | Peptide | |||
Cytotoxic T-lymphocyte-associated protein 4 (CTLA-4) | [89Zr]Zr-ipilimumab | Antibody | Melanoma | [41] |
Epidermal growth factor receptor (EGFR) | [11C]erlotinib [11C]PD153035 [18F]afatinib | Small molecule | Nonsmall cell lung carcinoma; colorectal cancer | [42,43,44,45,46] |
[89Zr]Zr-cetuximab [89Zr]Zr-panitumumab | Antibody | |||
Epidermal growth factor receptor 2 (ERBB2) | [68Ga]Ga-ABY-025 | Affibody | Breast cancer | [47,48,49] |
[68Ga]Ga-HER2-Nanobody | Nanobody | |||
[89Zr]Zr-trastuzumab [89Zr]Zr-pertuzumab | Antibody | |||
Epidermal growth factor receptor 3 (ERBB3) | [89Zr]Zr-GSK2849330 [89Zr]Zr-lumretuzumab | Antibody | Solid malignancies | [50,51] |
Estrogen receptor (ER) | [18F]FES[18F]4FMFES | Hormone | Breast cancer and gynecologic cancers | [52] |
Fibroblast activation protein α | [68Ga]Ga-FAPI-04 [68Ga]Ga-FAPI-21 [68Ga]Ga-FAPI-46 | Small molecule | Solid malignancies | [53,54,55] |
Galactose metabolism | [18F]FDGal | Small molecule | Hepatocarcinoma | [56] |
Gastrin-releasing peptide receptor (GRPR) | [64Cu]Cu-CB-TE2A-AR06 [18F]-BAY 864367 [68Ga]Ga-RM2 [68Ga]Ga-SB3 [68Ga]Ga-RM26 [68Ga]Ga-BBN-RGD [68Ga]Ga-NOTA-Aca-BBN [68Ga]Ga-NeoBOMB1 | Peptide | Prostate cancer, breast cancer, glioma | [57,58,59,60,61,62,63,64,65] |
Glucagon-like peptide 1 receptor (GLP-1R) | [68Ga]Ga-NOTA-exendin-4 | Peptide | Insulinoma | [66] |
Glucose metabolism | [18F]FDG *,# | Small molecule | Neoplasm | [1] |
Glypican 3 | [124I]I-codrituzumab | Antibody | Hepatocarinoma | [67] |
Hypoxia | [18F]EF5 [18F]FMISO# [18F]FAZA [18F]HX4 [64Cu]Cu-ATSM | Small molecule | Solid malignancies | [68,69,70,71,72,73] |
Integrin α4β1 | [64Cu]Cu-LLP2A | Peptidomimetic | Multiple myeloma | [74] |
Integrin αvβ3 | [18F]F-Galacto-RGD [18F]F-FPP(RGD)2 [18F]F-RGD-K5 [18F]F-fluciclatide Al[1 8F]F-alfatide-I Al[18F]F-alfatide-II [68Ga]Ga-NOTA-PRGD2 | Peptide | Solid malignancies | [75,76,77,78,79,80,81,82] |
Integrin αvβ6 | [18F]F-αvβ6-BP [68Ga]Ga-DOTA-SFITGv6 | Peptide | Head and neck cancer, lung cancer, colorectal cancer, breast cancer, pancreatic cancer | [83,84,85] |
[18F]FP-R01-MG-F2 [68Ga]Ga-NODAGA-R01-MG | Cystine knot | |||
Melanocortin-1 receptor (MC1R) | [68Ga]Ga-DOTA-GGNle-CycMSHhex | Peptide | Melanoma | [86] |
Mesothelin | [89Zr]Zr-MMOT0530A | Antibody | Pancreatic ductal adenocarcinoma and ovarian cancer | [87] |
Neurokinin 1 receptor (NK1R) | [68Ga]Ga-DOTA-SP | Peptide | Glioma | [88] |
Neurotensin 1 receptor (NTS1R) | Al[18F]F-NOTA-neurotensin | Peptide | Prostate cancer | [89] |
Phospholipid synthesis | [11C]choline * [18F]F-choline # | Salt | Prostate cancer | [90,91] |
Poly(ADP-ribose) polymerase 1 (PARP1) | [18F]PARPi | Small molecule | Head and neck cancer | [92] |
Prostate-specific membrane antigen (PSMA) | [18F]PSMA-1007 [18F]DCFPyL [18F]DCFBC [18F]rhPSMA-7 [68Ga]Ga-PSMA-11 [68Ga]Ga-PSMA-617 [68Ga]Ga-PSMA-I&T | Peptidomimetic | Prostate cancer | [93,94,95,96,97,98] |
[89Zr]Zr-HuJ591 | Antibody | |||
Programmed cell death protein (PD-1) | [89Zr]Zr-durvalumab [89Zr]Zr-nivolumab [89Zr]Zr-pembrolizumab | Antibody | Nonsmall cell lung carcinoma | [99,100] |
Programmed death-ligand 1 (PD-L1) | [18F]BMS-986192 | Adnectin | Nonsmall cell lung carcinoma, bladder cancer, breast cancer | [100,101,102] |
[89Zr]Zr-atezolizumab | Antibody | |||
Six-transmembrane epithelial antigen of prostate-1 (STEAP1) | [89Zr]Zr-DFO-MSTP2109A | Antibody | Prostate cancer | [103] |
Sodium/iodine transporter | Na[124I]I | Salt | Thyroid cancer | [104] |
Somatostatin receptor 2 (SSTR2) | [64Cu]Cu-SARTATE [68Ga]Ga-DOTA-TATE * [68Ga]Ga-DOTA-TOC *,# [68Ga]Ga-DOTA-NOC [68Ga]Ga-NODAGA-JR11 | Peptide | Neuroendocrine tumors | [105,106,107,108] |
Thymidine kinase (DNA replication) | [18F]FLT # | Nucleoside | Solid malignancies | [109] |
Transforming growth factor-beta (TGF-β) | [89Zr]Zr-fresolimumab | Antibody | Glioma | [110] |
Vascular endothelial growth factor receptor (VEGFR) | [89Zr]Zr-bevacizumab | Antibody | Solid malignancies | [111,112,113] |
Half-Life | Decay Mode | Mean β+ Energy [MeV] | Mean Positron Range in Water [mm] | Production Route | |
---|---|---|---|---|---|
11C | 20.4 min | β+ (99.8%) | 0.386 | 1.2 | 14N(p,α)11C |
13N | 10.0 min | β+ (99.8%) | 0.492 | 1.8 | 16O(p,α)13N |
15O | 2.0 min | β+ (99.9%) | 0.735 | 3.0 | 15N(p,n)15O |
18F | 109.7 min | β+ (96.7%) | 0.250 | 0.6 | 18O(p,n)18F |
44Sc | 4.0 h | β+ (94.3%) | 0.632 | 2.4 | 44Ti/44Sc generator |
64Cu | 12.7 h | β+ (17.6%) | 0.278 | 0.7 | 64Ni(p,n)64Cu 67Zn(p,α)64Cu |
68Ga | 67.7 min | β+ (88.9%) | 0.836 | 3.5 | 68Ge/68Ga generator |
82Rb | 1.3 min | β+ (81.8%) β+ (13.1%) | 1.535 1.168 | 7.1 5.0 | 82Sr/82Rb generator |
86Y | 14.7 h | β+ (11.9%) β+ (5.6%) β+ (3.6%) | 0.535 0.681 0.883 | 1.9 2.8 3.7 | 86Sr(p,n)86Y |
89Zr | 78.4 h | β+ (22.7%) | 0.396 | 1.3 | 89Y(p,n)89Zr |
124I | 100.2 h | β+ (11.7%) β+ (10.7%) β+ (0.3%) | 0.687 0.975 0.367 | 2.8 4.4 1.1 | 124Te(p,n)124I |
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Lau, J.; Rousseau, E.; Kwon, D.; Lin, K.-S.; Bénard, F.; Chen, X. Insight into the Development of PET Radiopharmaceuticals for Oncology. Cancers 2020, 12, 1312. https://doi.org/10.3390/cancers12051312
Lau J, Rousseau E, Kwon D, Lin K-S, Bénard F, Chen X. Insight into the Development of PET Radiopharmaceuticals for Oncology. Cancers. 2020; 12(5):1312. https://doi.org/10.3390/cancers12051312
Chicago/Turabian StyleLau, Joseph, Etienne Rousseau, Daniel Kwon, Kuo-Shyan Lin, François Bénard, and Xiaoyuan Chen. 2020. "Insight into the Development of PET Radiopharmaceuticals for Oncology" Cancers 12, no. 5: 1312. https://doi.org/10.3390/cancers12051312