Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy
Abstract
1. Introduction
2. Somatostatin Analogs
3. Targeting of Somatostatin Receptors with Radiopharmaceuticals
3.1. Radiolabeled Somatostatin Analogs for Imaging
3.1.1. Gallium-68 and Indium-111
3.1.2. Technetium-99m
3.1.3. Copper-64
3.1.4. Other Radiometals
3.1.5. Fluorine-18
3.2. Radiolabeled Somatostatin Analogs for Therapy
3.2.1. Yttrium-90 and Lutetium-177
3.2.2. Rhenium-188 and Other β-Emitting Radionuclides
3.2.3. Alpha and Auger Emitters
4. Antagonists vs. Agonists
5. Future Prospects
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Tumor Type | SSTR Expression | Ref |
---|---|---|
Astrocytoma | + | [17] |
Breast carcinoma | + (SSTR2) | [11] |
Cholangiocarcinoma | + (SSTR2) | [18] |
Colorectal carcinoma | - | [17] |
Endometrial carcinoma | - | [17] |
Ependymoma | + (SSTR1, SSTR5) | [11] |
Esophageal carcinoma | - | [17] |
Ewing sarcoma | - | [17] |
Exocrine pancreatic tumor | - | [17] |
Gastric carcinoma | + (SSTR1 > SSTR2, SSTR5) | [11] |
Gastrinoma | + (SSTR2) | [17] |
Glioblastoma | - | [17] |
Growth hormone-producing pituitary adenoma | + (SSTR2, SSTR5) | [17] |
Gut carcinoid | + (SSTR2 > SSTR1, SSTR5) | [17] |
Hepatocellular carcinoma | + (SSTR2, SSTR5) | [19] |
Insulinoma | + (SSTR1, SSTR2, SSTR3) | [20] |
Leiomyoma | + | [17] |
Lymphoma | + (SSTR2) | [11] |
Medullary thyroid carcinoma | + (SSTR2) | [11] |
Medulloblastoma | + (SSTR2) | [17] |
Meningioma | + (SSTR2) | [17] |
Neuroblastoma | + (SSTR2) | [17] |
Non-functioning pituitary adenoma | + (SSTR3 > SSTR2) | [17] |
Non-small cell lung cancer | - | [17] |
Ovarian carcinoma | + | [17] |
Paraganglioma | + (SSTR2) | [17] |
Pheochromocytoma | + (SSTR1, SSTR2) | [17] |
Prostate carcinoma | + (SSTR1) | [17] |
Renal cell carcinoma | + (SSTR2) | [11] |
Small cell lung cancer | + (SSTR2) | [17] |
Urinary bladder carcinoma | - | [17] |
Radionuclide | Half-Life (h) | Type of Emission | Energy of Emitted Radiation (keV) | Source | Application |
---|---|---|---|---|---|
99mTc | 6.01 | γ | 140 | Generator | SPECT imaging |
111In | 67.4 | γ | 172, 245 | Cyclotron | SPECT imaging |
18F | 1.83 | β+ | 634 | Cyclotron | PET imaging |
64Cu | 12.7 | β+/γ/β- | 653 | Cyclotron | PET imaging |
68Ga | 1.1 | β+ | 1190 | Generator/Cyclotron | PET imaging |
90Y | 64.1 | β− | 2284 | Generator | Therapy |
177Lu | 160.8 | β−/γ | 497 | Cyclotron | Therapy |
188Re | 17 | β−/γ | 2118 | Generator | Therapy |
211At | 7.2 | α | 5870 | Cyclotron | Therapy |
225Ac | 238 | α | 5830 | Generator | Therapy |
Peptide | Peptidic Sequence |
---|---|
OC Octreotide | d-Phe1-cyclo(Cys2-Phe3-d-Trp4-Lys5-Thr6-Cys7)Thr(ol)8 |
LAN Lanreotide | β-d-Nal1-cyclo(Cys2-Tyr3-d-Trp4-Lys5-Val6-Cys7)Thr8-NH2 |
VAP Vapreotide | d-Phe1-cyclo(Cys2-Phe3-d-Trp4-Lys5-Val6-Cys7)Trp8-NH2 |
TOC [Tyr3]-Octreotide | d-Phe1-cyclo(Cys2-Tyr3-d-Trp4-Lys5-Thr6-Cys7)Thr(ol)8 |
TATE [Tyr3]-Octreotate | d-Phe1-cyclo(Cys2-Tyr3-d-Trp4-Lys5-Thr6-Cys7)Thr8 |
NOC [1-Nal3]-Octreotide | d-Phe1-cyclo(Cys2-1-Nal3-d-Trp4-Lys5-Thr6-Cys7)Thr(ol)8 |
NOC-ATE [1-Nal3, Thr8]-Octreotide | d-Phe1-cyclo(Cys2-1-Nal3-d-Trp4-Lys5-Thr6-Cys7)Thr8 |
BOC [BzThi3]-Octreotide | d-Phe1-cyclo(Cys2-BzThi3-d-Trp4-Lys5-Thr6-Cys7)Thr(ol)8 |
BOC-ATE [BzThi3, Thr8]-Octreotide | d-Phe1-cyclo(Cys2-BzThi3-d-Trp4-Lys5-Thr6-Cys7)Thr8 |
Antagonist Peptide | Peptidic Sequence |
---|---|
Sst2-ANT (BASS) | p-NO2-Phe1-cyclo(d-Cys2-Tyr3-d-Trp4-Lys5-Thr6-Cys7)d-Tyr8-NH2 |
LM3 | p-Cl-Phe1-cyclo(d-Cys2-Tyr3-d-Aph4(Cbm)-Lys5-Thr6-Cys7)d-Tyr8-NH2 |
JR10 | p-NO2-Phe1-cyclo(d-Cys2-Tyr3-d-Aph4(Cbm)-Lys5-Thr6-Cys7)d-Tyr8-NH2 |
JR11 (Satoreotide) | p-Cl-Phe1-cyclo(d-Cys2-Aph3(Hor)-d-Aph4(Cbm)-Lys5-Thr6-Cys7)d-Tyr8-NH2 |
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Eychenne, R.; Bouvry, C.; Bourgeois, M.; Loyer, P.; Benoist, E.; Lepareur, N. Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy. Molecules 2020, 25, 4012. https://doi.org/10.3390/molecules25174012
Eychenne R, Bouvry C, Bourgeois M, Loyer P, Benoist E, Lepareur N. Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy. Molecules. 2020; 25(17):4012. https://doi.org/10.3390/molecules25174012
Chicago/Turabian StyleEychenne, Romain, Christelle Bouvry, Mickael Bourgeois, Pascal Loyer, Eric Benoist, and Nicolas Lepareur. 2020. "Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy" Molecules 25, no. 17: 4012. https://doi.org/10.3390/molecules25174012
APA StyleEychenne, R., Bouvry, C., Bourgeois, M., Loyer, P., Benoist, E., & Lepareur, N. (2020). Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy. Molecules, 25(17), 4012. https://doi.org/10.3390/molecules25174012