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131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1
131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1
- Source :
- The Journal of Nuclear Medicine. 61(2):242-248
- Publication Year :
- 2019
- Publisher :
- Society of Nuclear Medicine and Molecular Imaging, 2019.
-
Abstract
- Targeted radionuclide therapy (TRT) targeting oncoproteins facilitates the delivery of therapeutic radionuclides to tumor tissues with high precision. Herein, we developed two new radiopharmaceuticals, 4-131I-iodo- and 4-211At-astato-N-[4-(6-(isopropylamino)pyridine-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide (131I-IITM and 211At-AITM), targeting the ectopic metabotropic glutamate receptor 1 (mGluR1) in melanomas for TRT studies. Methods: 131I-IITM and 211At-AITM were synthesized by reacting a stannyl precursor with 131I-NaI and 211At in the presence of an oxidizing agent. The therapeutic efficacy and safety of the two radiopharmaceuticals were investigated using mGluR1-expressing B16F10 melanoma cells and melanoma-bearing mice. Results: 131I-IITM and 211At-AITM were obtained with radiochemical purity of >99% and radiochemical yields of 42.7% ± 10.4% and 28.9% ± 9.9%, respectively, based on the total radioactivity of used radionuclides. 131I-IITM and 211At-AITM exhibited maximum uptakes of 4.66% ± 0.70% ID/g and 7.68% ± 0.71% ID/g in the targeted melanomas, respectively, and were rapidly cleared from non-target organs after intravenous injection. Both agents markedly inhibited melanoma growth compared with the controls (61.00% and 95.68%, respectively). In the melanoma model, considerably greater therapeutic efficacy with negligible toxicity was observed using 211At-AITM. Conclusion: The non-toxic radiopharmaceuticals 131I-IITM and 211At-AITM are useful high-precision TRT agents that can be used to target the oncoprotein mGluR1 for melanoma therapy.
Details
- Language :
- English
- ISSN :
- 01615505
- Volume :
- 61
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- The Journal of Nuclear Medicine
- Accession number :
- edsair.jairo.........4b1ae780377c7ea5bd5f2f576c8e789d