Formulation and Biodistribution of 99mTc-Dacarbazine, a Radioligand for Neoplasm Imaging

A method for preparing 99 m Tc-Dacarbazine, a potential cancer diagnostic agent, was developed. The method is based on direct labeling of Dacarbazine with 99 m Tc in the presence of stannous chloride as reducing agent. The reaction conditions were optimized to obtain the radiochemical yield of 99 m Tc-Dacarbazine higher than 90%. The biodistribution of 99 m Tc-Dacarbazine in normal and tumor-bearing Albino Swiss mice was studied. 99 m Tc-Dacarbazine has a high tumor affinity and shows promise for cancer imaging. Quantitative relationship between the optimized structures and computed molecular properties related to Dacarbazine binding sites was analyzed using molecular modeling.