Evaluation of 177Lu-CHX-A′′-DTPA-Bevacizumab as a radioimmunotherapy agent targeting VEGF expressing cancers. (August 2016)

• Record Type: Journal Article
• Authors: Kameswaran, Mythili; Pandey, Usha; Gamre, Naresh; Vimalnath, K.V.; Sarma, Haladhar Dev; Dash, Ashutosh
• Is Part Of: Applied radiation and isotopes. Volume 114(2016:Aug.)
• Page Start: 196
• Page End: 201
• Publication Date: 2016-08
• Subjects: Vascular Endothelial Growth Factor (VEGF) -- Bevacizumab -- 177Lu-CHX-A′′-DTPA-Bevacizumab -- Melanoma; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2016.05.025
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: This study aimed at the preparation and evaluation of 177 Lu-CHX-A′′-DTPA-Bevacizumab for targeting VEGF over-expressing cancers. Bevacizumab conjugated to p-NCS-Bn-CHX-A′′-DTPA was radiolabeled with 177 Lu. The radioimmunoconjugate characterized by SE-HPLC exhibited radiochemical purity of 98.0±0.6%. In vitro stability was retained upto 4 days at 37 °C. In vitro cell binding studies showed good uptake by VEGF expressing U937 tumor cells. Biodistribution studies in melanoma model showed significant uptake and retention of 177 Lu-CHX-A′′-DTPA-Bevacizumab in tumor with reduction in uptake in presence of cold Bevacizumab confirming its specificity to VEGF. Highlights: Bevacizumab conjugated with p-NCS-Bn-CHX-A′′-DTPA was radiolabeled with 177 Lu. Radiochemical purity of 177 Lu-CHX-A′′-DTPA-Bevacizumab was 98.0±0.6%. Good in-vitro stability of radioimmunoconjugate up to 4 days in saline at 37 °C. Good uptake of 177 Lu-CHX-A′′-DTPA-Bevacizumab by VEGF expressing U937 tumor cells. Significant uptake and retention of radioimmunoconjugate in the melanoma tumor.