Abstract
The principle of pretargeted radioimmunoimaging and therapy has been investigated over the past 30 y in preclinical and clinical settings with the aim of reducing the radiation burden of healthy tissue for antibody-based nuclear medicine techniques. In the past few decades, 4 pretargeting methodologies have been proposed, and 2 of them-the bispecific antibody-hapten and the streptavidin-biotin platforms-have been evaluated in humans in phase 1 and 2 studies. With this review article, we aim to survey clinical pretargeting studies in order to understand the challenges that these platforms have faced in human studies and to provide an overview of how the clinical approval of the pretargeting system has proceeded in the past several decades. Additionally, we will discuss the successes of the pretargeting human studies and compare and highlight the pretargeting approaches and conditions that will advance clinical translation of the pretargeting platform in the future.