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

Abstract

A method for preparing ^99mTc-Dacarbazine, a potential cancer diagnostic agent, was developed. The method is based on direct labeling of Dacarbazine with ^99mTc in the presence of stannous chloride as reducing agent. The reaction conditions were optimized to obtain the radiochemical yield of ^99mTc-Dacarbazine higher than 90%. The biodistribution of ^99mTc-Dacarbazine in normal and tumor-bearing Albino Swiss mice was studied. ^99mTc-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.