Clinical Advances and Perspectives in Targeted Radionuclide Therapy
Abstract
:1. Introduction
2. Radioimmunotherapy (RIT)
2.1. Antibodies and Derivatives
2.2. Pretargeting Approach
2.3. Dose Fractionation Approach
3. Oligonucleotides
4. Peptide Receptor Radionuclide Therapy (PRRT)
4.1. The G Protein-Coupled Receptors Family
4.1.1. Somatostatin Analogs
4.1.2. Bombesin Analogs
4.1.3. Substance P
4.1.4. Other Analogs
4.2. C-X-C Chemokine Receptor Type 4 (CXCR-4)
4.3. Other Peptide Derivatives
5. Radioligand Therapy (RLT)
5.1. Bone-Seeking Agents
5.2. [131I]mIBG
5.3. Prostate-Specific Membrane Antigen (PSMA) Inhibitors
5.4. Fibroblast-Activation Protein (FAP) Inhibitors
5.5. Poly(ADP-Ribose)Polymerase (PARP) Inhibitors
5.6. Carbonic Anhydrase IX (CA IX) Inhibitors
5.7. Vitamins
5.8. Phospholipid Ether Analogues
5.9. Melanin Targeting Agents
6. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Radionuclide | Half-life | Energy (MeV) | Eγ (keV) | Tissue Penetration Range (mm) |
---|---|---|---|---|
β-emitter | ||||
90Y | 2.7 days | 2.284 | / | 12 |
131I | 8 days | 0.81 | 0.364 | 2.4 |
161Tb | 6.9 days | 0.593 | 74.6 | 3 |
177Lu | 6.7 days | 0.497 | 208113 | 2.2 |
188Re | 17 h | 2.118 | 155 | 11 |
α-emitter | ||||
149Tb | 4.1 h | 3.97 | Multiple emissions (165–800) | <100 µm |
211At | 7.2 h | 7.45 | 85 (X-ray) | |
212Pb/212Bi * | 10.6 h | 8.78 | 238, 300 | |
213Bi | 0.8 h | 8.38 | 440 | |
223Ra | 11.4 days | 5.71, 6.82, 7.39, 6.62 | 270 | |
225Ac | 10 days | 5.8, 6.3, 7.1, 8.38 | 218, 440 (from daughters) | |
227Th | 18.7 days | 6.14, 5.71, 6.82, 7.39, 6.62 | 236 | |
Auger e− emitter | ||||
111In | 2.8 days | 0.007 | 405 | <1 µm |
125I | 60 days | 0.019 | 42 |
Peptide | Receptor | Tumor Expression |
---|---|---|
α-Melanocyte-stimulating hormone | MCR1, MCR3, and MCR5 | Melanomas |
Bombesin/Gastrin-releasing peptide | BB1, BB2 (GRPR), BB3, and BB4 | Glioblastomas, prostate, breast, pancreatic, gastric, colorectal cancers, and small cell lung |
Cholecystokinin/gastrin | CCK1, and CCK2 | Adenomas, astrocytomas, gastrointestinal and ovarian stromal tumors, medullary thyroid, pancreatic and small cell lung cancers |
Epidermal Growth Factor | EGFR | Breast cancer |
Exendin | GLP-1 | Gastrinomas, insulinomas, medullary thyroid carcinomas, paragangliomas and pheochromocytomas |
Gonadotropin-releasing hormone | GnRH-R | Breast and prostate cancers |
Neuropeptide Y | Y1, Y2, Y4, and Y5 | Breast, ovary, adrenal, brain, kidney, GI-tract, and bone (Ewing’s sarcoma) |
Neurotensin | NTR1, NTR2, and NTR3 | Breast, colon, pancreatic, prostate, small cell lung cancers, and meningiomas |
RGD | αVβ3 integrin | Tumor-induced angiogenesis |
SDF-1α/CXCL12 | CXCR4, and CXCR7 | Leukemias, lymphomas, melanomas, brain, breast, kidney, lung, ovarian, pancreas, and prostate tumors |
Somatostatin | Sstr1, sstr2, sstr3, sstr4, and sstr5 | Neuroendocrine tumors, lymphomas, paragangliomas, brain, breast, renal, and small cell lung cancers |
Substance P | NK1, NK2, and NK3 | Glial tumors, breast, medullary thyroid, pancreas, and small cell lung cancers |
Vasoactive intestinal peptide | VPAC1, and VPAC2 | Bladder, breast, gastrointestinal, non-small cell lung, ovarian, pancreatic, and prostate cancers |
Peptide | Peptidic Sequence |
---|---|
OC Octreotide | d-Phe-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)Thr(ol) |
LAN Lanreotide | β-d-Nal-cyclo(Cys-Tyr-d-Trp-Lys-Val-Cys)Thr-NH2 |
VAP Vapreotide | d-Phe-cyclo(Cys-Phe-d-Trp-Lys-Val-Cys)Trp-NH2 |
TOC [Tyr3]-Octreotide | d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr(ol) |
TATE [Tyr3]-Octreotate | d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr |
NOC [1-Nal3]-Octreotide | d-Phe-cyclo(Cys-1-Nal-d-Trp-Lys-Thr-Cys)Thr(ol) |
SOM230 Pasireotide | Cyclo(Hyp(Unk)-Phg- d-Trp-Lys-Tyr(Bn)-Phe) |
P2045 Tozaride | Ser-Thr-Cys(Trt)-Phe(4-NH2)-(β-DAP)-CH2CO-S-cyclo((N-Me)HCy-Phe-Tyr-d-Trp-Lys-Thr) |
Target | Name | Structure |
---|---|---|
SSTR | DOTA-BASS | |
DOTA-LM3 | ||
DOTA-JR11 (Satoreotide) | ||
GRPR | DOTA-RM2 | |
NeoB | ||
NTR | 3BP-227 |
Radionuclide | Agent |
---|---|
Approved Agents for Clinical Use | |
Strontium-89 (β−) (50.5 d) | [89Sr]SrCl2—Metastron® |
Samarium-153 (β−) (1.9 d) | EDTMP—Quadramet® |
Rhenium-186 (β−) (3.7 d) | HEDP |
Radium-223 (α) (11.4 d) | [223Ra]RaCl2—Xofigo® |
Agents in Clinical Trials | |
Rhenium-188 (β−) (17 h) | HEDP Zoledronic acid |
Lutetium-177 (β−) (6.8 d) | EDTMP DOTMP * Zoledronic acid (Dotazol) |
Holmium-166 (β−) (1.1 d) | DOTMP * |
Tin-117m (CE) (13.6 d) | DTPA ** |
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Lepareur, N.; Ramée, B.; Mougin-Degraef, M.; Bourgeois, M. Clinical Advances and Perspectives in Targeted Radionuclide Therapy. Pharmaceutics 2023, 15, 1733. https://doi.org/10.3390/pharmaceutics15061733
Lepareur N, Ramée B, Mougin-Degraef M, Bourgeois M. Clinical Advances and Perspectives in Targeted Radionuclide Therapy. Pharmaceutics. 2023; 15(6):1733. https://doi.org/10.3390/pharmaceutics15061733
Chicago/Turabian StyleLepareur, Nicolas, Barthélémy Ramée, Marie Mougin-Degraef, and Mickaël Bourgeois. 2023. "Clinical Advances and Perspectives in Targeted Radionuclide Therapy" Pharmaceutics 15, no. 6: 1733. https://doi.org/10.3390/pharmaceutics15061733
APA StyleLepareur, N., Ramée, B., Mougin-Degraef, M., & Bourgeois, M. (2023). Clinical Advances and Perspectives in Targeted Radionuclide Therapy. Pharmaceutics, 15(6), 1733. https://doi.org/10.3390/pharmaceutics15061733