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Targeted radionuclide therapy with RAFT-RGD radiolabelled with 90Y or 177Lu in a mouse model of αvβ3-expressing tumours
Targeted radionuclide therapy with RAFT-RGD radiolabelled with 90Y or 177Lu in a mouse model of αvβ3-expressing tumours
- Source :
- European Journal of Nuclear Medicine and Molecular Imaging, European Journal of Nuclear Medicine and Molecular Imaging, 2015, 42 (2), pp.252-263. ⟨10.1007/s00259-014-2891-7⟩, European Journal of Nuclear Medicine and Molecular Imaging, Springer Verlag (Germany), 2015, 42 (2), pp.252-263. ⟨10.1007/s00259-014-2891-7⟩
- Publication Year :
- 2015
- Publisher :
- HAL CCSD, 2015.
-
Abstract
- International audience; PurposeThe αvβ3 integrin plays an important role in tumour-induced angiogenesis, tumour proliferation, survival and metastasis. The tetrameric RGD-based peptide, regioselectively addressable functionalized template-(cyclo-[RGDfK])4 (RAFT-RGD), specifically targets the αvβ3 integrin in vitro and in vivo. The aim of this study was to evaluate the therapeutic potential of RAFT-RGD radiolabelled with β− emitters in a nude mouse model of αvβ3 integrin-expressing tumours.MethodsBiodistribution and SPECT/CT imaging studies were performed after injection of 90Y-RAFT-RGD or 177Lu-RAFT-RGD in nude mice subcutaneously xenografted with αvβ3 integrin-expressing U-87 MG cells. Experimental targeted radionuclide therapy with 90Y-RAFT-RGD or 177Lu-RAFT-RGD and 90Y-RAFT-RAD or 177Lu-RAFT-RAD (nonspecific controls) was evaluated by intravenous injection of the radionuclides into mice bearing αvβ3 integrin-expressing U-87 MG tumours of different sizes (small or large) or bearing TS/A-pc tumours that do not express αvβ3. Tumour volume doubling time was used to evaluate the efficacy of each treatment.ResultsInjection of 37 MBq of 90Y-RAFT-RGD into mice with large αvβ3-positive tumours or 37 MBq of 177Lu-RAFT-RGD into mice with small αvβ3-positive tumours caused significant growth delays compared to mice treated with 37 MBq of 90Y-RAFT-RAD or 37 MBq of 177Lu-RAFT-RAD or untreated mice. In contrast, injection of 30 MBq of 90Y-RAFT-RGD had no effect on the growth of αvβ3-negative tumours.Conclusion90Y-RAFT-RGD and 177Lu-RAFT-RGD are potent agents targeting αvβ3-expressing tumours for internal targeted radiotherapy.
- Subjects :
- Pathology
medicine.medical_specialty
Internal targeted radiotherapy
Angiogenesis
Mice, Nude
Peptide
[SDV.IB.MN]Life Sciences [q-bio]/Bioengineering/Nuclear medicine
Lutetium
Peptides, Cyclic
030218 nuclear medicine & medical imaging
Metastasis
03 medical and health sciences
Mice
0302 clinical medicine
Nude mouse
In vivo
Cell Line, Tumor
[CHIM] Chemical Sciences
medicine
Animals
Humans
[CHIM]Chemical Sciences
Radiology, Nuclear Medicine and imaging
Tissue Distribution
Yttrium Radioisotopes
90Y
ComputingMilieux_MISCELLANEOUS
chemistry.chemical_classification
αvβ3 integrin
biology
General Medicine
Raft
Neoplasms, Experimental
RGD peptide
177Lu
medicine.disease
biology.organism_classification
Integrin alphaVbeta3
Xenograft Model Antitumor Assays
In vitro
3. Good health
chemistry
030220 oncology & carcinogenesis
Cancer research
lipids (amino acids, peptides, and proteins)
Radiopharmaceuticals
Subjects
Details
- Language :
- English
- ISSN :
- 16197070 and 16197089
- Database :
- OpenAIRE
- Journal :
- European Journal of Nuclear Medicine and Molecular Imaging, European Journal of Nuclear Medicine and Molecular Imaging, 2015, 42 (2), pp.252-263. ⟨10.1007/s00259-014-2891-7⟩, European Journal of Nuclear Medicine and Molecular Imaging, Springer Verlag (Germany), 2015, 42 (2), pp.252-263. ⟨10.1007/s00259-014-2891-7⟩
- Accession number :
- edsair.doi.dedup.....2da339bdeba40064007421a30c6d016c
- Full Text :
- https://doi.org/10.1007/s00259-014-2891-7