Synthesis and Imaging of Novel CDK19-Targeted Tracers Incorporating an Albumin-Binding Moiety

Abstract

Cyclin-dependent kinase 19 (CDK19) is a potential target for the diagnosis and treatment of prostate cancer. We have previously studied a series of CDK19-targeted PET tracers, but in-depth drug optimization is needed to improve the physiochemical properties of such large and polar tracers. The albumin strategy has received widespread attention in recent years, and we synthesized ⁶⁸Ga-IRM-14a and ⁶⁸Ga-IRM-14b based on the strategy. After in vivo imaging studies in mice, we found that introducing albumin moiety will significantly change the physicochemical properties of existing large polarity tracers, thereby increasing tissue uptake and retention, which is beneficial for future treatment. In short, the albumin strategy will be an important strategy in the field of radiopharmaceutical optimization.