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Updated: Apr 16, 2026

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
Published on: February 3, 2015
Antibody positron emission tomography imaging in anticancer drug development
Laetitia E Lamberts1, Simon P Williams1, Anton G T Terwisscha van Scheltinga1
1Laetitia E. Lamberts, Anton G.T. Terwisscha van Scheltinga, Marjolijn N. Lub-de Hooge, Carolien P. Schröder, Jourik A. Gietema, Adrienne H. Brouwers, and Elisabeth G.E. de Vries, University of Groningen, University Medical Center Groningen, Groningen, the Netherlands; and Simon P. Williams, Genentech, South San Francisco, CA.
Abstract:
More than 50 monoclonal antibodies (mAbs), including several antibody-drug conjugates, are in advanced clinical development, forming an important part of the many molecularly targeted anticancer therapeutics currently in development. Drug development is a relatively slow and expensive process, limiting the number of drugs that can be brought into late-stage trials. Development decisions could benefit from quantitative biomarkers, enabling visualization of the tissue distribution of (potentially modified) therapeutic mAbs to confirm effective whole-body target expression, engagement, and modulation and to evaluate heterogeneity across lesions and patients. Such biomarkers may be realized with positron emission tomography imaging of radioactively labeled antibodies, a process called immunoPET. This approach could potentially increase the power and value of early trials by improving patient selection, optimizing dose and schedule, and rationalizing observed drug responses. In this review, we summarize the available literature and the status of clinical trials regarding the potential of immunoPET during early anticancer drug development.
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