Preclinical evaluation of 68Ga- and 177Lu-Labeled AP-01 for the targeted treatment of prostate cancer with moderate PSMA expression

In this study, AP-01 was successfully synthesized. ⁶⁸Ga-AP-01 and ¹⁷⁷Lu-AP-01 were obtained with high radiochemical purity and stability. High binding affinity and PSMA targeting specificity were identified in vitro and in vivo. With significantly enhanced tumor uptake and retention, ¹⁷⁷Lu-AP-01 has the potential to improve therapeutic efficacy for the treatment of prostate cancer with moderate PSMA expression.