Mallia Madhava B, Mathur Anupam, Sarma Haladhar D, Banerjee Sharmila
1 Radiopharmaceuticals Division, Bhabha Atomic Research Centre , Mumbai, India .
Cancer Biother Radiopharm. 2015 Mar;30(2):79-86. doi: 10.1089/cbr.2014.1705. Epub 2015 Jan 8.
The PET radiopharmaceutical [(18)F]Fluromisonidazole ([(18)F]FMISO) is presently the agent of choice for the clinical imaging of tumor hypoxia. Considering the logistic advantages of (99m)Tc and wider availability of SPECT machines, a (99m)Tc-radiopharmaceutical for this purpose constitutes an attractive choice. In the work presented here, a misonidazole analogue was radiolabeled with (99m)Tc(CO)3 core and the complex was evaluated in Swiss mice bearing fibrosarcoma tumor. The results obtained are compared with the biodistribution of [(18)F]FMISO carried out in the same tumor-bearing animal model. Misonidazole-(99m)Tc(CO)3 complex showed significant uptake and retention in tumor. Notably, the rate of clearance of misonidazole complex from the tumor was slower than that of [(18)F]FMISO. The maximum tumor/muscle ratio obtained with misonidazole-(99m)Tc(CO)3 complex was significantly higher than that of [(18)F]FMISO. The study constitutes a positive step toward the development of a (99m)Tc-analogue of [(18)F]FMISO.
正电子发射断层显像（PET）放射性药物[（18）F]氟米索硝唑（[（18）F]FMISO）目前是肿瘤缺氧临床显像的首选药物。鉴于锝-99m（99mTc）的物流优势以及单光子发射计算机断层扫描（SPECT）仪更广泛的可用性，用于此目的的99mTc放射性药物是一个有吸引力的选择。在本文介绍的研究中，一种米索硝唑类似物用99mTc（CO）3核心进行放射性标记，并在患有纤维肉瘤肿瘤的瑞士小鼠中对该复合物进行了评估。将所得结果与在相同荷瘤动物模型中进行的[（18）F]FMISO的生物分布进行比较。米索硝唑-99mTc（CO）3复合物在肿瘤中显示出显著的摄取和滞留。值得注意的是，米索硝唑复合物从肿瘤中的清除率比[（18）F]FMISO慢。米索硝唑-99mTc（CO）3复合物获得的最大肿瘤/肌肉比值显著高于[（18）F]FMISO。该研究朝着开发[（18）F]FMISO的99mTc类似物迈出了积极的一步。
