Molecular Imaging Drug Design and Evaluation Techniques

1.1 Molecular Imaging Drug Design Technology

We have a technical platform for designing and constructing molecular imaging drugs by labeling target molecules with near-infrared fluorescence, radioactive nuclides (99mTc, 125I, 18F, 68Ga, etc.), and magnetic resonance enhancers (Gd). Technetium [99mTc] dextran (Class II new drug, certificate number X19990152), Technetium [99mTc] folic acid polyethylene glycol diethylenetriamine pentaacetic acid (approved by TYL2009-0051), etc. were developed by using this technology platform. Currently, we are developing Gd nuclear magnetic imaging agents for VAP and 68Ga and 18F PET imaging agents for VAP. The relevant patents have also been transferred, with a transfer amount of 1 million yuan.

1.2. Molecular Imaging Drug Evaluation Technology

Evaluation techniques include: characterization of physical and chemical properties of molecular imaging drugs or kits, molecular interactions, molecular imaging (CT, fluorescence, SPECT, PET, MRI), and other techniques.

Example: Tumor Active Targeting PET Diagnostic Agent VAP-NOTA-18F

VAP was prepared by labeling 18F with chelating agent NOTA to obtain VAP-NOTA-18F. The distribution results in the tumor animal model (Figure 15) show that VAP-NOTA-18F is cleared quickly in the tumor bearing mice, and the high distribution in the kidneys indicates that it is mainly eliminated through the kidneys, with significant accumulation at the tumor site; The tumor/blood ratio of VAP-NOTA-18F reached its maximum value of 10.67 at 120 minutes, and the optimal imaging time window was 60 minutes after administration. The imaging results of microPET/CT scan showed that VAP-NOTA-18F had high radiation intensity at the tumor site, while no radiation signal enhancement was observed in other major organs (the kidneys and bladder were drug clearance sites with high radiation intensity), which was superior to the clinical tumor targeted diagnostic drug 18F-FDG.

Figure 15. In vivo distribution and imaging results of VAP-NOTA-18F in tumor bearing mice

Related patents:

1. Lu Weiyue, Gu Bing, Xie Cao, Liu Min, Zhu Jianhua; A Folic Acid Complex for Imaging Diagnosis of Tumors and Lymphatic Metastasis (2008102009819, Authorization Date April 6, 2012)

2. Chen Jian, Lu Weiyue, Xie Cao, Li Zhuoyun; Radionuclide drugs targeting high expression of glucose regulatory protein GRP78 in tumors and their applications (2018116538402, application date December 29, 2018) have been transferred with a transfer amount of 1 million yuan