Achmad Arifudin, Hanaoka Hirofumi, Holik Holis Abdul, Endo Keigo, Tsushima Yoshito, Kartamihardja Achmad Hussein S
Department of Nuclear Medicine and Molecular Theranostics, Faculty of Medicine, Universitas Padjadjaran, Bandung 40161, West Java, Indonesia.
Theranostic Radiopharmaceutical Research Collaboration Center, Universitas Padjadjaran, Sumedang 45363, West Java, Indonesia.
Theranostics. 2025 Jan 2;15(5):1864-1878. doi: 10.7150/thno.99490. eCollection 2025.
The quest for a cancer-specific positron emission tomography (PET) tracer has been ongoing for decades. Current evidence shows that targeting amino acid metabolism dysregulation is a valid alternative cancer detection method and can complement the conventional approach, which relies on targeting increased glucose metabolism. The rate of amino acid metabolism in all major organs is mostly equally low and does not change in any physiological dynamics. The amino acid metabolism rate only spikes in malignant tissues. PET imaging targeting LAT1 (L-type amino acid transporter 1) demonstrated accurate cancer imaging of various cancer types with nearly negligible background uptake. LAT1 is a biomarker of amino acid metabolism dysregulation. The upregulated LAT1 expression in cancer cells depicts their dynamic behavior and aggressiveness. This review discussed PET radiotracers developed as a LAT1-specific agent and how this new class of cancer-specific radiopharmaceuticals could deliver PET images with clinical properties we yearn for, such as high specificity toward various malignancies, robust non-cancer exclusion (mainly inflammatory reactions), accurate malignant lesion delineation, representative therapeutic monitoring, and long-term prognostication.
数十年来，人们一直在寻找一种癌症特异性正电子发射断层扫描（PET）示踪剂。目前的证据表明，针对氨基酸代谢失调是一种有效的癌症检测替代方法，并且可以补充依赖于针对葡萄糖代谢增加的传统方法。所有主要器官中的氨基酸代谢速率大多同样很低，并且在任何生理动态过程中都不会改变。只有在恶性组织中氨基酸代谢速率才会飙升。针对LAT1（L型氨基酸转运体1）的PET成像显示，对各种癌症类型都能进行准确的癌症成像，且背景摄取几乎可以忽略不计。LAT1是氨基酸代谢失调的一个生物标志物。癌细胞中LAT1表达上调反映了它们的动态行为和侵袭性。本文综述了作为LAT1特异性试剂开发的PET放射性示踪剂，以及这类新型癌症特异性放射性药物如何能够提供具有我们所期望临床特性的PET图像，例如对各种恶性肿瘤具有高特异性、强大的非癌症排除能力（主要是炎症反应）、准确的恶性病变描绘、具有代表性的治疗监测以及长期预后评估。
