Bao Mei, Gu Xiang, Tong Kai, Chu Fei, Ye Pinmao, Kaneda-Nakashima Kazuko, Hou Wenbin, Li Yiliang, Wei Ling
School of Chinese Materia Medica, Guangdong Pharmaceutical University, Guangzhou 510006, China.
Division of Radiation Science, Institute for Radiation Sciences, Osaka University, 2-4 Yamadaoka, Suita 565-0871, Osaka, Japan.
Int J Mol Sci. 2025 Jun 18;26(12):5848. doi: 10.3390/ijms26125848.
L-3-[F]-fluoro-α-methyl tyrosine ([F]FAMT) is an amino acid positron emission tomography (PET) tracer with high specificity for malignant tumors through its selective transport via L-type amino acid transporter (LAT) 1. Although extensively studied for its diagnostic performance, a comprehensive review of its molecular and clinical characteristics remains lacking. A systematic literature review (1997-2025) was conducted using PubMed and Web of Science, with keywords including "L-3-[F]-fluoro-α-methyl tyrosine", "[F]FAMT", "amino acid PET", and "tumor imaging". The review covered aspects of synthesis, structural properties, pharmacokinetics, and clinical applications. Notably, while research on [F]FAMT has declined significantly in recent years, [F]FAMT PET demonstrates superior specificity to [F]FDG PET in distinguishing malignancies from inflammatory lesions and offers distinct advantages in lung, esophageal, and oral cancers, though with slightly lower sensitivity. Its key features include tumor-specific uptake patterns, rapid blood clearance, and a significant correlation between its uptake levels and both LAT1 expression and tumor proliferation. In conclusion, [F]FAMT is a promising PET tracer with notable advantages in tumor imaging, particularly due to its LAT1 selectivity and favorable pharmacokinetics. Despite challenges in production, these characteristics underscore its clinical value in cancers requiring precise imaging. Future research should focus on optimizing synthesis, expanding clinical validation, and exploring theranostic applications.
L-3-[F]-氟-α-甲基酪氨酸（[F]FAMT）是一种氨基酸正电子发射断层扫描（PET）示踪剂，通过L型氨基酸转运体（LAT）1的选择性转运，对恶性肿瘤具有高特异性。尽管对其诊断性能进行了广泛研究，但仍缺乏对其分子和临床特征的全面综述。使用PubMed和Web of Science进行了一项系统的文献综述（1997 - 2025年），关键词包括“L-3-[F]-氟-α-甲基酪氨酸”、“[F]FAMT”、“氨基酸PET”和“肿瘤成像”。该综述涵盖了合成、结构性质、药代动力学和临床应用等方面。值得注意的是，近年来对[F]FAMT的研究显著减少，然而[F]FAMT PET在区分恶性肿瘤与炎性病变方面显示出比[F]FDG PET更高的特异性，并且在肺癌、食管癌和口腔癌中具有明显优势，尽管敏感性略低。其关键特征包括肿瘤特异性摄取模式、快速的血液清除以及摄取水平与LAT1表达和肿瘤增殖之间的显著相关性。总之，[F]FAMT是一种有前景的PET示踪剂，在肿瘤成像方面具有显著优势，特别是由于其对LAT1的选择性和良好的药代动力学。尽管在生产方面存在挑战，但这些特征突出了其在需要精确成像的癌症中的临床价值。未来的研究应专注于优化合成、扩大临床验证以及探索诊疗应用。
