Preparation of a Kit Formulation of [99mTc]Tc-CN7DM, a Mannose Derivative for Tumor Imaging, and an Exploratory Human Study.

Abstract

Lung cancer is the most prevalent malignancy worldwide in terms of both incidence and mortality. Therefore, diagnosing lung cancer early is important. Nuclear medicine imaging is an integral modality for cancer diagnosis, in which radiopharmaceuticals are essential elements. Thus, we explored the potential of the novel, previously reported ^99mTc-labeled mannose derivative ([^99mTc]Tc-CN7DM) as a radiopharmaceutical with excellent performance that can be easily clinically translated for tumor imaging. However, when we used a kit formulation which was directly prepared from the ligand CN7DM for preparing [^99mTc]Tc-CN7DM, some unknown radioactive compounds were found. In order to solve this problem, in this study, we synthesized the cuprous complex [Cu(CN7DM)₄]BF₄ for kit formulation to prepare [^99mTc]Tc-CN7DM and evaluated its biological properties and safety profile. Moreover, a preliminary imaging study was conducted with lung cancer patients, and the results demonstrated that [^99mTc]Tc-CN7DM allowed clear visualization of tumor lesions, giving it promising prospects for clinical application.