Targeted therapies, such as radioimmunotherapy (RIT), present a promising treatment option for the eradication of tumor lesions. RIT has shown promising results especially for hematologic malignancies, but the therapeutic efficacy is limited by unfavorable tumor-tobackground ratios resulting in high radiotoxicity. Pretargeting strategies can play an important role in addressing the high toxicity profile of RIT. Key to pretargeting is the concept of decoupling the targeting vehicle from the cytotoxic agent and administrating them separately. Studies have shown that this approach has the ability to enhance the therapeutic index as it can reduce side effects caused by off-target irradiation and thereby increase curative effects due to higher tolerated doses. Pretargeted RIT (PRIT) has been explored for imaging and treatment of different cancer types over the years. This review will give an overview of the various targeted therapies in which pretargeting has been applied, discussing PRIT with alpha-and beta-emitters and as part of combination therapy, plus its use in drug delivery systems.

Biotin, Bispecific antibody, Cancer, Click chemistry, Nanoparticles, Oligonucleotides, Pretargeting, Radioimmunotherapy, Streptavidin, Targeted radionuclide therapy,
Department of Radiology

Verhoeven, M. (Marjolein), Seimbille, Y. (Yann), & Dalm, S.U. (2019). Therapeutic applications of pretargeting. Pharmaceutics (Vol. 11). doi:10.3390/pharmaceutics11090434