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. <sup>68</sup>Ga-AP-01 and <sup>177</sup>Lu-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, <sup>177</sup>Lu-AP-01 has the potential to improve therapeutic efficacy for the treatment of prostate cancer with moderate PSMA expression.

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Publication Details

Journal
European Journal of Nuclear Medicine and Molecular Imaging
Published
2025-12-18
DOI
https://doi.org/10.1007/s00259-025-07704-2
Primary Topic
Prostate Cancer Treatment and Research
Type
article
Field-Weighted Citation Impact
0.00

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article

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

Simin He, Shaoli Song, Yi Liu, Xiao Wang et al.
European Journal of Nuclear Medicine and Molecular Imaging
Prostate Cancer Treatment and Research
article

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

Simin He, Shaoli Song, Yi Liu, Xiao Wang, Jianping Zhang, Xiaoping Xu, Xiaoyu Pan, Xuan Huang
article en

Abstract

In this study, AP-01 was successfully synthesized. <sup>68</sup>Ga-AP-01 and <sup>177</sup>Lu-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, <sup>177</sup>Lu-AP-01 has the potential to improve therapeutic efficacy for the treatment of prostate cancer with moderate PSMA expression.

European Journal of Nuclear Medicine and Molecular Imaging
Shanghai Medical College of Fudan University (CN), Xiamen University (CN), Fudan University (CN), Fudan University Shanghai Cancer Center (CN), United Imaging Healthcare (China) (CN)
National Natural Science Foundation of China
Openalex Percentile: Top 41%
Prostate Cancer Treatment and Research
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Preclinical evaluation of 68Ga- and 177Lu-Labeled AP-01 for the targeted treatment of prostate cancer with moderate PSMA expression — Simin He, Shaoli Song, et al. · European Journal of Nuclear Medicine and Molecular Imaging (2025) | TGRS Research Map | TGRS