Bioorthogonal click chemistry-employing antibody-conjugated trans-cyclooctenes (TCO) and tetrazine (Tz)-based radioligands able to covalently bind in vivo-appeared recently as a potential alternative to circumvent the hematotoxicity induced by radioimmunotherapy of solid tumors. This Review focuses on the recent advances concerning TCO/Tz pretargeting in both cancer imaging and targeted-radionuclide therapy for prospective clinical transfer. We exhaustively identified 25 PubMed publications reporting preclinical imaging and 5 therapy studies with full mAbs as targeting vectors, since its first application in 2010. The fast, safe, modulable, and specific TCO/Tz pretargeting showed high potential as a theranostic tool to get more personalized and precise cancer care. The recent optimizations reported here highlighted a possible first clinical evaluation of IEDDA pretargeting in the coming years.

中文翻译：

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基于生物正交点击化学的抗体预靶向用于癌症成像和靶向放射性核素治疗。

能够在体内共价结合的基于生物正交点击化学的抗体偶联的反式环辛烯（TCO）和基于四嗪（Tz）的放射性配体最近出现，作为一种潜在的替代品，它可以规避实体瘤放射免疫疗法所引起的血液毒性。这篇综述着重于有关TCO / Tz预靶向在癌症影像学和靶向放射性核素治疗中进行前瞻性临床转移的最新进展。自2010年首次应用以来，我们详尽地鉴定了25篇PubMed出版物，它们报告了临床前成像和5项以全mAb为靶向载体的治疗研究。快速，安全，可调节且特异的TCO / Tz预先靶向显示了作为治疗更多内容的治疗手段的巨大潜力个性化和精确的癌症护理。