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Promising pre-clinical validation of targeted radionuclide therapy using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment

Bonnet-Duquennoy, M., Papon, J., Mishellany, F., Denoyer, D., Labarre, P, Guerquin-Kern, J.L., Penault-llorca, F., Madelmont, J.C., Miot-Noirault, E., Cayre, A., Chezal, J.M. and Moins, N. 2009, Promising pre-clinical validation of targeted radionuclide therapy using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment, Journal of cancer science & therapy, vol. 1, no. 1, pp. 1-7, doi: 10.4172/1948-5956.1000001.

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Title Promising pre-clinical validation of targeted radionuclide therapy using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment
Formatted title Promising pre-clinical validation of targeted radionuclide therapy using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment
Author(s) Bonnet-Duquennoy, M.
Papon, J.
Mishellany, F.
Denoyer, D.ORCID iD for Denoyer, D. orcid.org/0000-0001-8932-5116
Labarre, P
Guerquin-Kern, J.L.
Penault-llorca, F.
Madelmont, J.C.
Miot-Noirault, E.
Cayre, A.
Chezal, J.M.
Moins, N.
Journal name Journal of cancer science & therapy
Volume number 1
Issue number 1
Start page 1
End page 7
Total pages 7
Publisher Omics Publishing Group
Place of publication Los Angeles, California
Publication date 2009-11
ISSN 1948-5956
Keyword(s) targeted internal radionuclide therapy (TRT)
tumor
melanoma treatment
[131I] labelled iodoquinoxaline derivative
preclinical validation
Summary Targeted internal radionuclide therapy (TRT) would be an effective alternative to current therapies for dissemi- nated melanoma treatment. At our institution, a class of iodobenzamides has been developed as potent melanoma- seeking agents. This review described the preclinical vali- dations of a quinoxaline derivative molecule (ICF01012) as tracer for TRT application. It was selected for its high, specific and long-lasting uptake in tumour with rapid clear- ance from non-target organs providing suitable dosimetry parameters for TRT. Extended in vivo study of metabolic profiles confirmed durable tumoural concentration of the unchanged molecule form. Moreover melanin specificity of ICF01012 was determined by binding assay with syn- thetic melanin and in vivo by SIMS imaging. Then, we showed in vivo that [131I] ICF01012 treatment drastically inhibited growth of B16F0, B16Bl6 and M4Beu tumours whereas [131I] NaI or unlabelled ICF01012 treatment was without significant effect. Histological analysis showed that residual tumour cells exhibit a significant loss of aggres- siveness after treatment. This anti-tumoural effect was associated with a lengthening of the treated-mice survival time and an inhibition of lung dissemination for B16Bl6 model. Results presented here support the concept of TRT using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment.
Language eng
DOI 10.4172/1948-5956.1000001
Field of Research 111204 Cancer Therapy (excl Chemotherapy and Radiation Therapy)
Socio Economic Objective 920102 Cancer and Related Disorders
HERDC Research category C1.1 Refereed article in a scholarly journal
Copyright notice ©2009, Omics Publishing Group
Free to Read? Yes
Use Rights Creative Commons Attribution licence
Persistent URL http://hdl.handle.net/10536/DRO/DU:30063127

Document type: Journal Article
Collections: School of Life and Environmental Sciences
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Every reasonable effort has been made to ensure that permission has been obtained for items included in DRO. If you believe that your rights have been infringed by this repository, please contact drosupport@deakin.edu.au.