SP-103 - Scandium-47 and lutetium-177 radiolabelling and stability studies of 1st and 2nd generation DOTA-triphenylphosphonium ligands – potential radionuclide theranostics for treatment of glioblastoma multi-forme

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dc.contributor.authorWyatt, NAen_AU
dc.contributor.authorHogan, Len_AU
dc.contributor.authorPellegrini, PAen_AU
dc.contributor.authorRoberts, MPen_AU
dc.contributor.authorHall, Aen_AU
dc.contributor.authorSmith, Nen_AU
dc.contributor.authorHemzal, Een_AU
dc.contributor.authorHill, Len_AU
dc.contributor.authorHowell, NRen_AU
dc.contributor.authorMiddleton, RJen_AU
dc.contributor.authorSafavi-Naeini, Men_AU
dc.contributor.authorRendina, LMen_AU
dc.contributor.authorFraser, BHen_AU
dc.date.accessioned2021-06-30T02:50:11Zen_AU
dc.date.available2021-06-30T02:50:11Zen_AU
dc.date.issued2021-05-17en_AU
dc.date.statistics2021-06-25en_AU
dc.descriptionVolumes 96–97 Supplement 1 of Nuclear Medicine and Biology is comprised of the Abstract Book for this Conference. Copyright © 2021 Elsevier Inc.en_AU
dc.description.abstractScandium-47 has emerged as a promising radioisotope for targeted radionuclide tumor therapy. This is due, to a significant extent, from the combination of low energy / short range β- emission, the availability of a “perfect theranostic pair” with Sc-44 for companion PET imaging, the potential to form highly stable radiometal complexes, and the availability of suitable γ emissions for companion SPECT imaging. Sc-47 also has a shorter half-life (3.35 d) than the chemically similar Lu-177 (6.7 d) which is significant given recent in vitro research that suggests longer lived isotopes require more initial radioactivity to have the same effect upon cell viability [3]. The shorter half-life of Sc-47 also suggests it may be more suitable for smaller biological vectors (with shorter biological half-lives) such as small molecules and low MW peptides. One area of clinical treatment where Sc-47 can have impact and where improvements in patient outcomes and survival rates remain stubbornly low is glioblastoma multiforme (GBM). GBM is the most common and aggressive form of malignant brain tumor and represents around 60% of all adult brain tumors with a global incidence of <10 per 100,000 persons. The prognosis for GBM patients is poor with a -ear survival rate of 37%, 5 year rate of 5% and a median survival time of 10 months. The current standard of treatment is resection of the tumor followed by radiation therapy and chemotherapy. Given this poor prognosis there is a clear and unmet need for improved classes of treatment. Although significant progress has been made towards bringing GBM targeted radionuclide therapies to the clinic, the efforts to date have not included utilizing Sc-44/ Sc-47. Given this we are developing and evaluating Sc-44/Sc-47 and Lu-177/Ga-68 radiolabelled triphenylphosphonium (TPP) functionalised DOTA ligands (1st and 2nd generation) as potential theranostics for GBM. Described herein is our work on comparing the radiolabelling efficiency (Sc-47 vs. Lu-177) and stability studies (PBS pH 7.4, rat plasma) for our 1st and 2nd generation DOTA-TPP ligands. The presence of an additional carbonyl group in the 2nd generation DOTATPP ligand was anticipated to increase the number of donor atoms around the radiometal and affect radiolabelling reaction conditions and, more importantly, increase radiometal complex stability. Copyright © 2021 Elsevier Inc.en_AU
dc.description.sponsorshipSociety of Radiopharmaceutical Sciencesen_AU
dc.identifier.citationWyatt, N., Hogan, L., Pellegrini, P., Roberts, M., Hall, A., Smith, N., Hemzal, E., Hill, L., Howell, N., Middleton, R., Safavi-Naeini, M., Rendina, L. & Fraser, B. (2021). SP-103 - Scandium-47 and lutetium-177 radiolabelling and stability studies of 1st and 2nd generation DOTA-triphenylphosphonium ligands – potential radionuclide theranostics for treatment of glioblastoma multi-forme. Paper presented at the Society of Radiopharmaceutical Sciences eSRS Virtual Meeting 2021, 17 to 19 May 2021. In Nuclear Medicine and Biology, 96–97 (Supp. 1), S93-S94. doi:10.1016/S0969-8051(21)00420-0en_AU
dc.identifier.conferenceenddate19 May 2021en_AU
dc.identifier.conferencenameSociety of Radiopharmaceutical Sciences eSRS Virtual Meetingen_AU
dc.identifier.conferenceplaceOnlineen_AU
dc.identifier.conferencestartdate17 May 2021en_AU
dc.identifier.issn0969-8051en_AU
dc.identifier.issueS1en_AU
dc.identifier.journaltitleNuclear Medicine and Biologyen_AU
dc.identifier.paginationS93-S94en_AU
dc.identifier.urihttps://doi.org/10.1016/S0969-8051(21)00420-0en_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/10977en_AU
dc.identifier.volume96-97en_AU
dc.language.isoenen_AU
dc.publisherElsevieren_AU
dc.subjectRadioisotopesen_AU
dc.subjectLutetium 177en_AU
dc.subjectScandium 47en_AU
dc.subjectStabilityen_AU
dc.subjectLigandsen_AU
dc.subjectTheranosticsen_AU
dc.subjectGliomasen_AU
dc.subjectTherapyen_AU
dc.titleSP-103 - Scandium-47 and lutetium-177 radiolabelling and stability studies of 1st and 2nd generation DOTA-triphenylphosphonium ligands – potential radionuclide theranostics for treatment of glioblastoma multi-formeen_AU
dc.typeConference Abstracten_AU
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