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KMID : 1145520200060010053
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Journal of Radiopharmaceuticals and Molecular Probes
2020 Volume.6 No. 1 p.53 ~ p.58
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Pretargeting : A concept refraining traditional flaws in tumor targeting
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Bhise Abhinav
Yoo Jeong-Soo
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Abstract
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Pretargeting is a two-component strategy often used for tumor targeting to enhance the tumor-to-background ratio in cancer diagnosis as well as therapy. In the multistep strategy, the highly specific unlabeled monoclonal antibodies (mAbs) with the reactive site is allowed to get localized at tumor site first, and then small and fastclearing radiolabeled chelator with counter reactive site is administered which covalently attaches to mAbs via inverse electron demand Diels-Alder reaction (IEDDA). The catalyst-free IEDDA cycloaddition reaction between 1,2,4,5-tetrazines and strained alkene dienophiles aid with properties like selective bioconjugation, swift and high yielding bioorthogonal reactions are emergent in the development of radiopharmaceutical. Due to its fast pharmacokinetics, the in vivo formed radioimmunoconjugates can be imaged at earlier time points by short-lived radionuclides like 18F and 68Ga; it can also reduce radiation damage to the normal cells. Ultimately, this review elucidates the updated status of pretargeting based on antibodies and IEDDA for tumor diagnosis (PET and SPECT) and therapy.
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KEYWORD
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pretargeting, monoclonal antibodies, radioisotopes, tumor targeting, tumor-to-background, tumor accumulation
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