Cancer Biotherapy and Radiopharmaceuticals 2015-03-01

A (99m)Tc-labeled misonidazole analogue: step toward a (99m)Tc-alternative to [18F]fluromisonidazole for detecting tumor hypoxia.

Madhava B Mallia, Anupam Mathur, Haladhar D Sarma, Sharmila Banerjee

Index: Cancer Biother. Radiopharm. 30(2) , 79-86, (2015)

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Abstract

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.