Abstract
Targeted internal radionuclide therapy (TRT) would be an effective alternative to current therapies for disseminated melanoma treatment. At our institution, a class of iodobenzamides has been developed as potent melanomaseeking agents. This review described the preclinical validations 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 clearance 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 synthetic 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 aggressiveness 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.
Highlights
Results presented here support the concept of Targeted internal radionuclide therapy (TRT) using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment
Results presented here support the concept of TRT using a [131I] labelled iodoquinoxaline derivative for an effective melanoma treatment
The response rate is still rather low and there has been no progress in systemic palliative melanoma treatment for three decades partly due to their high toxicity (Eigentler et al, 2003; Garbe and Eigentler, 2007)
Summary
Promising Pre-clinical Validation of Targeted Radionuclide Therapy Using a [131I] Labelled Iodoquinoxaline Derivative for an Effective Melanoma Treatment. Bonnet-Duquennoy M1*, Papon J1, Mishellany F2, Denoyer D1, Labarre P1, Guerquin-Kern JL3,4, Penault-llorca F2, Madelmont JC1, Miot-Noirault E1, Cayre A2, Chezal JM1, Moins N1
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
