Title: BIOTINYLATED AND CHELATED POLY-L-LYSINE AS EFFECTOR FOR PRETARGETING IN CANCER THERAPY AND IMAGING
Authors: GUSTAFSSON-LUTZ AnnaBAECK TomANEHEIM EmmaPALM StigMORGENSTERN AlfredBRUCHERTSEIFER FrankALBERTSSON PerLINDEGREN Sture
Citation: INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES vol. 9 no. 1 p. 87 - 93
Publisher: INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES
Publication Year: 2017
JRC N°: JRC101796
ISSN: 0975-1491
URI: http://innovareacademics.in/journals/index.php/ijpps/article/view/11109
http://publications.jrc.ec.europa.eu/repository/handle/JRC101796
DOI: 10.22159/ijpps.2017v9i1.11109
Type: Articles in periodicals and books
Abstract: Objective: The aim of this study was to synthesise and evaluate polylysine-based effectors for pretargeted radioimmunotherapy and imaging. These molecules can readily be size-modified and charge-modified to decrease the renal uptake of radioactivity, which is often a major problem for small radiolabeled molecules. Several chelators and biotin molecules (for antibody-streptavidin-binding in vivo) are also easily incorporated into one structure because of the polylysine. Methods: The effectors were synthesised using poly-L-lysine, NHS-LC-biotin, CHX-A’’-DTPA or p-SCN-Bn-DOTA and succinic anhydride. They were characterised, labelled with 213Bi for targeted α therapy, 68Ga for PET and 111In for SPECT, and evaluated in vitro. A kidney uptake study was performed as well with two different-sized 213Bi-labeled effectors, to evaluate how the difference in size affects the renal filtration. Results: Radiochemical purities between 97.4±0.6 % and 99.6±0.1 % and decay-corrected yields of 80.2±2.4 % after purification were achieved with the radiolabeled molecules, as well as a specific activity of 7.6 × 103GBq/μmol. The avidin binding capacity was 94.4±1.9%. The kidney uptake study demonstrated a reduction of renal absorbed dose by 80% when modifying the molecular size and charge. Conclusion: The synthesised polylysine-based effectors show potential for further in vivo evaluation in pretargeted radioimmunotherapy and imaging.
JRC Directorate:Nuclear Safety and Security

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