Preparation and Evaluation of Lu Labeled Nitroimidazole Derivative for Targeting Tumor Hypoxia

Hypoxia has been known be an important physiological parameter for tumor growth and has been reported to be the cause for poor response to chemotherapy. Mechanistically, tumor hypoxia results from an imbalance between oxygen delivery and oxygen consumption. The identification and quantification of tumor hypoxia may predict the out come and may identify patients who might benefit from concomitant radiosensitizing therapy to overcome the hypoxia effect. In nuclear medicine, there is an interesting observation that nitroimidazole derivatives can selectively accumulate in the hypoxic regions, a character of a good radiosensitizer. In this study, we have synthesized a 2-nitroimidazole derivative containing a DOTA chelator by using a solid phase reaction. The nitroimidazole analogue was radiolabeled with Lu. Furthermore biodistribution study was performed to evaluate its tissue uptake, in vivo.