2025/10/24 by Yuze Ma, Jingyue Gao, Kunyao Wang +2 · 1 citation
Medicine · #Biodistribution #Colorectal Cancer Screening and Detection #Colorectal cancer #Dissociation constant #Gastric Cancer Management and Outcomes #Genetic factors in colorectal cancer #Metabolic stability #Molecular imaging #Pharmacokinetics #Spect imaging #Urinary system
paper · doi:10.1021/acs.jmedchem.5c01224
published in Journal of Medicinal Chemistry 68(21), 22333-22347 (American Chemical Society)
openalex created_date 2025/10/24 · openalex publication_date 2025/10/24 · openalex updated_date 2026/08/01
Abstract Colorectal cancer (CRC) is one of the most common tumors, and discoidin domain receptor 1 (DDR1) expression is significantly higher in CRC. In this study, we designed and synthesized eight novel 68Ga-labeled DDR1-targeted radiotracers. The radiochemical purities (RCPs) of radiotracers were all over 95%; except for [68Ga]Ga-MYZ02 and [68Ga]Ga-MYZ06, other six radiotracers showed high stability in vitro and in vivo. The equilibrium dissociation constants (KD) of radiotracers were all in the nanomolar range. Micro-PET/CT imaging and biodistribution study showed that [68Ga]Ga-MYZ04, which exhibits favorable pharmacokinetic properties, could clearly visualize tumors at 1 h postinjection. Among the six radiotracers, [68Ga]Ga-MYZ04 had the highest tumor-to-muscle ratio (T/M: 4.21 ± 0.51), a higher tumor-to-liver ratio (T/L: 0.71 ± 0.06), and the lowest tumor-to-kidney ratio (T/K: 0.55 ± 0.03), suggesting a superior metabolic pathway with primary clearance through the urinary system. This makes it promising for the imaging diagnosis of DDR1-positive expressing CRC.