In Vivo investigation of radiolabeled Bevacizumab in healthy rat tissues

Abstract

In this study, BevMab was conjugated with the bifunctional chelating agent [diethylenetriamine pentaacetic acid (DTPA)] and the product (BevMab-DTPA) was labeled with 99mTc using stannous chloride reducing method. The quality control studies of radiolabeled compound (99mTc-BevMab-DTPA) were done with Thin Layer Radio Chromatography (TLRC) and High Performance Liquid Radio Chromatography (HPLRC) methods (% 95 <) to confirm the labeling efficiency. High radiochemical yield [98.07 % ± 2.17 (n = 13)] was obtained by TLRC method. Biodistribution studies of 99mTc labeled BevMab-DTPA was run on healthy female and male Albino Wistar rats. The distribution figures demonstrated that the radiolabeled compound was eliminated through the kidneys and accumulated in urinary bladder. The values of the BevMab-DTPA uptakes were similar in heart, blood, liver and spleen in both sexes

Preclinical evaluation of holmium‐166 labeled anti‐VEGF‐A(Bevacizumab)

“…The same relationship also has been observed for liver and lung which expresses the receptor at some extent. The similar maximum uptake for the urinary tract and kidneys has also been reported for 99m Tc‐DTPA‐bevacizumab …”

“…The similar maximum uptake for the urinary tract and kidneys has also been reported for 99m Tc-DTPA-bevacizumab. 22 For 89 Zr-bevasizumab, lung, liver, kidneys, and also spleen demonstrated the major organs of uptake. Surprisingly, the blood uptake is significant for 166 Ho-DOTA-bevacizumab, whereas in case of 64 Cu-DOTA-VEGF and Tc-99m, radioimmunoconjugate blood content is not significant.…”

Desenvolvimento de radioimunoconjugados como agentes teranósticos baseados no anticorpo monoclonal anti-HER2 (trastuzumabe): influência dos agentes quelantes e dos radionuclídeos nas propriedades biológicas

“…Esse comportamento in vivo pode ser previsto pela avaliação prévia da lipofilicidade. [12,13,[145][146][147] Os resultados encontrados nesse estudo permitem supor que o AcM-DTPA- 111 In e o AcM-DOTA-177 Lu podem apresentar ligeiras diferenças nos estudos de biodistribuição, conforme será discutido a seguir. In vivo, os radioimunoconjugados acumulam-se no fígado e nos rins, onde ocorrem o catabolismo das proteínas e o processo de eliminação, sendo que a retenção da radioatividade inespecífica resulta da transferência do metal radioativo às metaloproteínas endógenas.…”