Discovery of Near-Infrared Heptamethine Cyanine Probes for Imaging-Guided Surgery in Solid Tumors

• Published in: Journal of medicinal chemistry Vol. 67; no. 7; pp. 5800 - 5812
• Main Authors: Lin, Qiao, Li, Changsheng, Wang, Yuhua, Zhu, Yanqing, Gu, Yueqing
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 11.04.2024; Amer Chemical Soc
• Subjects: Carcinoma, Hepatocellular; Chemistry, Medicinal; Fluorescent Dyes; Humans; Life Sciences & Biomedicine; Liver Neoplasms; Optical Imaging - methods; Pharmacology & Pharmacy; Science & Technology; Surgery, Computer-Assisted - methods
• ISSN: 0022-2623; 1520-4804; 1520-4804
• DOI: 10.1021/acs.jmedchem.4c00010

Near-infrared (NIR) fluorescence imaging has attracted much attention in image-guided interventions with unique advantages. However, the clinical translation rate of fluorescence probes is extremely low, primarily due to weak lesion signal contrast and poor specificity. To address this dilemma, a series of small-molecule near-infrared fluorescence probes have been designed for tumor imaging. Among them, YQ-04-03 showed notable optical stability and remarkable sensitivity toward tumor targeting. Moreover, within a specific concentration and time range against oxidizing reducing agents and laser, it demonstrated better stability than ICG. The retention time of YQ-04-03 in tumors was significantly longer compared to other nonspecific uptake sites in the subjects, and its tumor-to-normal tissue ratio (TNR) outperformed ICG. Successful resection of in situ hepatocarcinoma and peritoneal carcinoma was achieved using probe imaging guidance, with the smallest visual lesion resected measuring approximately 1 mm3. Ultimately, this probe holds great potential for advancing tumor tracer.