Uppsala Applied Science Laboratory, GE Healthcare, Uppsala, Sweden.
Med Chem. 2011 Sep;7(5):345-79. doi: 10.2174/157340611796799195.
Positron Emission Tomography (PET) field and, in particular utilization of (68)Ga radiometal is getting momentum. The development of new imaging agents for targeted, pre-targeted, non-targeted imaging and their clinical applications is accelerating worldwide. The pharmacopoeia monographs regarding generator produced (68)Ga radionuclide and (68)Ga-labeled somatostatin (SST) analogues are in progress. The number of commercial generators and automated synthesizers for (68)Ga-labeling chemistry is increasing constantly. Development of a molecular imaging agent is a complex process including identification of the biological target, respective lead compound, synthesis of the imaging agent, its chemical characterization, pre-clinical, and clinical evaluation. The introduction of new radiopharmaceuticals and their accessibility are important factors determining the expansion of clinical nuclear medicine for early disease detection and personalized medicine with higher therapeutic efficiency. Further, the availability of the technology for GMP compliant automated tracer production can facilitate the introduction of new radiopharmaceuticals due to the ability to conduct standardized and harmonized multi-center studies for regulatory approval. This review reflects on the current status of (68)Ga in PET field with the focus on the achievements in the chemistry as well as diversity and potential of the resulting tracers.
正电子发射断层扫描（PET）领域，特别是（68）Ga 放射性金属的应用正在获得动力。新型靶向、预靶向、非靶向成像试剂及其临床应用的开发在全球范围内正在加速。关于发生器产生的（68）Ga 放射性核素和（68）Ga 标记生长抑素（SST）类似物的药典专论正在进行中。用于（68）Ga 标记化学的商业发生器和自动化合成器的数量不断增加。分子成像剂的开发是一个复杂的过程，包括生物靶标的识别、相应的先导化合物、成像剂的合成、其化学表征、临床前和临床评估。新型放射性药物的开发及其可及性是决定临床核医学早期疾病检测和提高治疗效率的个体化医学扩展的重要因素。此外，由于能够进行符合 GMP 的自动化示踪剂生产的技术的可用性，可以促进新型放射性药物的引入，因为它能够进行标准化和协调的多中心研究以获得监管批准。这篇综述反映了（68）Ga 在 PET 领域的现状，重点介绍了化学方面的成就以及由此产生的示踪剂的多样性和潜力。
