3-羟基-4-吡啶酮类螯合剂在镓放射性药物中的研究进展及展望

Progress and Prospects of 3-Hydroxy-4-Pyridinone Chelators in Gallium Radiopharmaceuticals

目前,在肿瘤等重大疾病的早期诊断中,PET/CT(或PET/MRI)是灵敏度最高、分辨率最好的医学影像手段。PET/CT(或PET/MRI)依赖于PET药物,很大程度上依赖于18F PET药物。然而,随着世界上第一个68Ga药物(68Ga-DOTATATE)获得美国FDA批准进入市场,68Ga及其药物的研究正受到越来越多的关注。本文首先介绍了镓的基本核性质和化学性质,然后提出了金属双功能螯合剂的设计要求,并讨论了一些常用镓螯合剂的优缺点。由于3-羟基-4-吡啶酮基团对三价镓离子具有高的亲和力和选择性,因此,特别重点关注了3-羟基-4-吡啶酮多齿螯合剂在镓放射性药物中的最新研究进展。最后,还对3-羟基-4-吡啶酮多齿螯合剂在镓放射性药物中的应用前景进行了展望。

At present, PET/CT(or PET/MRI) is a powerful imaging technique with the highest sensitivity and spatial resolution for the early diagnoses of major diseases, such as cancers. PET/CT(or PET/MRI) relies on PET radiopharmaceuticals, especially heavily relies on 18F PET radiopharmaceuticals. However, with a market approval of FDA for the first 68Ga radiopharmaceutical(68Ga-DOTATATE) in the world, 68Ga and its radiopharmaceuticals receive more and more attention. In this review article, firstly, basic nuclear characteristics and chemical properties of gallium were described. Secondly, the requirement of design for bifunctional metallic chelators was suggested. Then, the advantages and disadvantages of some common gallium chelators were discussed. Due to the high affinity and selectivity of 3-hydroxy-4-pyridinones(3, 4-HPs) to Ga(Ⅲ), the newest progress of 3-hydroxy-4-pyridinone multidentate chelators, which were used in gallium radiopharmaceuticals, was focused on. Finally, the prospects of 3-hydroxy-4-pyridinone multidentate chelators in gallium radiopharmaceuticals were also proposed.