Department of Pharmacy, Henan Provincial People's Hospital, and People's Hospital of Zhengzhou University, Zhengzhou 450003, China.
Department of Nuclear Medicine, Henan Provincial People's Hospital, and People's Hospital of Zhengzhou University, Zhengzhou 450003, China.
Contrast Media Mol Imaging. 2019 Mar 26;2019:7954854. doi: 10.1155/2019/7954854. eCollection 2019.
Glucose homeostasis plays a key role in numerous fundamental aspects of life, and its dysregulation is associated with many important diseases such as cancer. The atypical glucose metabolic phenomenon, known as the Warburg effect, has been recognized as a hallmark of cancer and serves as a promising target for tumor specific imaging. At present, 2-deoxy-2-[F]fluoro-glucose (F-FDG)-based positron emission tomography/computed tomography (PET/CT) represented the state-of-the-art radionuclide imaging technique for this purpose. The powerful impact of F-FDG has prompted intensive research efforts into other glucose-based radiopharmaceuticals for positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging. Currently, glucose and its analogues have been labeled with various radionuclides such as Tc, In, F, Ga, and Cu and have been successfully investigated for tumor metabolic imaging in many preclinical studies. Moreover, Tc-ECDG has advanced into its early clinical trials and brings a new era of tumor imaging beyond F-FDG. In this review, preclinical and early clinical development of glucose-based radiopharmaceuticals for tumor metabolic imaging will be summarized.
葡萄糖稳态在生命的许多基本方面发挥着关键作用，其失调与许多重要疾病有关，如癌症。非典型的葡萄糖代谢现象，即沃伯格效应，已被认为是癌症的一个标志，并成为肿瘤特异性成像的有前途的靶点。目前，基于 2-脱氧-2-[F]氟葡萄糖（F-FDG）的正电子发射断层扫描/计算机断层扫描（PET/CT）是用于此目的的最先进的放射性核素成像技术。F-FDG 的强大影响促使人们对其他用于正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）成像的基于葡萄糖的放射性药物进行了深入研究。目前，葡萄糖及其类似物已被标记上各种放射性核素，如 Tc、In、F、Ga 和 Cu，并已在许多临床前研究中成功用于肿瘤代谢成像。此外，Tc-ECDG 已进入早期临床试验阶段，为超越 F-FDG 的肿瘤成像带来了一个新时代。本文综述了用于肿瘤代谢成像的基于葡萄糖的放射性药物的临床前和早期临床开发。
