I-贝伐单抗的临床前评估——一种用于VEGF表达型癌症放射免疫治疗的前瞻性药物。

Preclinical evaluation of I-Bevacizumab - A prospective agent for radioimmunotherapy in VEGF expressing cancers.

作者信息

Kameswaran Mythili, Sarma Haladhar Dev, Dash Ashutosh

机构信息

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400085, India.

Radiation Biology & Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400085, India.

出版信息

Appl Radiat Isot. 2017 May;123:109-113. doi: 10.1016/j.apradiso.2017.02.024. Epub 2017 Feb 16.

DOI:10.1016/j.apradiso.2017.02.024

PMID:28260607

Abstract

This study focuses on preparation and evaluation of I-bevacizumab by Iodogen method for targeting VEGF over-expressing cancers for therapy. I-Bevacizumab exhibited radiochemical purity of 98.0±0.7%. In vitro stability of I-Bevacizumab was retained at >85% in both saline and serum at 37°C upto 5 days post iodination. In vitro cell studies showed good immunoreactivity and uptake by VEGF expressing tumor cells. Uptake and retention of I-Bevacizumab in tumor with reduction in uptake in presence of cold Bevacizumab confirmed its specificity to VEGF.

摘要

本研究聚焦于通过碘标记法制备碘贝伐单抗，并对其进行评估，以用于靶向治疗血管内皮生长因子（VEGF）过表达的癌症。碘贝伐单抗的放射化学纯度为98.0±0.7%。碘贝伐单抗在碘化后5天内，于37°C的生理盐水和血清中，体外稳定性均保持在85%以上。体外细胞研究表明，其对表达VEGF的肿瘤细胞具有良好的免疫反应性和摄取能力。碘贝伐单抗在肿瘤中的摄取和滞留情况，以及在冷贝伐单抗存在下摄取减少，证实了其对VEGF的特异性。