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DOI 10.1021/acs.jmedchem.5c01010

Медицинская библиотека · Journal of medicinal chemistry · 2025

Development and Preclinical Validation of a Novel 89Zr-Labeled BCMA-Targeting Antibody for ImmunoPET Imaging: Application in Multiple Myeloma Models and First-In-Nonhuman-Primates.

Wang Tianyao, Yang Qi, Huang Wenpeng, Sun Xinyao, Lei Youlan, Xu Hui, Song Lele, Duan Xiaojiang, Liu Futao, Wang Wenzhi, Bao Zheng, Gao Jinquan, Wang Feng, Kang Lei

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Аннотация

B-cell maturation antigen (BCMA) is a clinically validated biomarker and therapeutic target in multiple myeloma (MM). Here, we report the design, synthesis, and preclinical evaluation of an immunoPET probe, [89Zr]Zr-DFO-PFBH0L0, derived from a novel humanized anti-BCMA monoclonal antibody. The antibody was conjugated with deferoxamine (DFO) and radiolabeled with zirconium-89 (89Zr), yielding a probe with excellent in vitro stability. The tracer retained high binding affinity and demonstrated specific binding to BCMA-positive MM cell lines. In vivo PET imaging and biodistribution studies demonstrated significantly higher tumor uptake in H929-bearing BCMA xenografts (10.04 ± 1.04% ID/g) and a tumor-to-blood ratio exceeding 88, outperforming all controls. Notably, this study presents the first BCMA-targeted PET/CT imaging in nonhuman primates (rhesus macaques), revealing favorable pharmacokinetics, biodistribution, and metabolic stability - underscoring its translational potential for clinical immunoPET imaging and therapeutic monitoring. These results establish [89Zr]Zr-DFO-PFBH0L0 as a promising immunoPET imaging agent for noninvasive, whole-body evaluation of BCMA-expressing malignancies.

Для цитирования: Wang Tianyao, Yang Qi, Huang Wenpeng, Sun Xinyao, Lei Youlan, Xu Hui, Song Lele, Duan Xiaojiang, Liu Futao, Wang Wenzhi, Bao Zheng, Gao Jinquan, Wang Feng, Kang Lei. Development and Preclinical Validation of a Novel 89Zr-Labeled BCMA-Targeting Antibody for ImmunoPET Imaging: Application in Multiple Myeloma Models and First-In-Nonhuman-Primates.. Journal of medicinal chemistry. 2025. DOI: 10.1021/acs.jmedchem.5c01010.

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