UMMS Affiliation

Department of Radiology

Publication Date


Document Type



Medical Pharmacology | Neoplasms | Pharmacology | Radiology


Pretargeting is often used as a tumor targeting strategy that provides much higher tumor to non-tumor ratios than direct-targeting using radiolabeled antibody. Due to the multiple injections, pretargeting is investigated less than direct targeting, but the high T/NT ratios have rendered it more useful for therapy. While the progress in using this strategy for tumor therapy has been regularly reviewed in the literature, this review focuses on the nature and quantitative understanding of the pretargeting concept. By doing so, it is the goal of this review to accelerate pretargeting development and translation to the clinic and to prepare the researchers who are not familiar with the pretargeting concept but are interested in applying it. The quantitative understanding is presented in a way understandable to the average researchers in the areas of drug development and clinical translation who have the basic concept of calculus and general chemistry.


pretargeting, quantitative correlation, semi-empirical model, target conversion, tumor accumulation

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Copyright © 2018 Liu. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

DOI of Published Version



Front Pharmacol. 2018 Dec 17;9:1476. doi: 10.3389/fphar.2018.01476. eCollection 2018. Link to article on publisher's site

Journal/Book/Conference Title

Frontiers in pharmacology

Related Resources

Link to Article in PubMed

PubMed ID


Creative Commons License

Creative Commons Attribution 4.0 License
This work is licensed under a Creative Commons Attribution 4.0 License.