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PET imaging with radiolabeled antibodies and tyrosine kinase inhibitors: immuno-PET and TKI-PET

机译:使用放射性标记的抗体和酪氨酸激酶抑制剂进行PET成像:免疫PET和TKI-PET

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摘要

During the last decade, the discovery of critical tumor targets has boosted the design of targeted therapeutic agents with monoclonal antibodies (mAbs) and tyrosine kinase inhibitors (TKIs) receiving most of the attention. Immuno-positron emission tomography (immuno-PET) and TKI-PET, the in vivo tracking and quantification of mAbs and TKIs biodistribution with PET, are exciting novel options for better understanding of the in vivo behavior and efficacy of these targeted drugs in individual patients and for more efficient drug development. Very recently, current good manufacturing practice compliant procedures for labeling of mAbs with positron emitters have been described, as well as the preparation of some radiolabeled TKIs, while the first proof of principle studies has been performed in patients. In this review, technical developments in immuno-PET and TKI-PET are described, and their clinical potential is discussed. An overview is provided for the most appealing preclinical immuno-PET and TKI-PET studies, as well as the first clinical achievements with these emerging technologies.
机译:在过去的十年中,关键肿瘤靶点的发现促进了单克隆抗体(mAb)和酪氨酸激酶抑制剂(TKIs)引起的靶向治疗剂的设计,引起了大多数关注。免疫正电子发射断层扫描(immuno-PET)和TKI-PET,体内跟踪和定量单克隆抗体和TKIs与PET的生物分布,是令人兴奋的新选择,可以更好地了解这些靶向药物在个体患者中的体内行为和功效以及更有效的药物开发。最近,已经描述了使用正电子发射器标记mAb的当前符合良好生产规范的程序,以及一些放射性标记的TKI的制备方法,同时已经在患者中进行了原理验证的第一个证明。在这篇综述中,描述了免疫PET和TKI-PET的技术发展,并讨论了它们的临床潜力。概述了最有吸引力的临床前免疫PET和TKI-PET研究,以及这些新兴技术的首批临床成就。

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