Exploring Structural Parameters for Pretargeting Radioligand Optimization.

ABSTRACT: Pretargeting offers a way to enhance target specificity while reducing off-target radiation dose to healthy tissue during payload delivery. We recently reported the development of an ¹⁸F-based pretargeting strategy predicated on the inverse electron demand Diels-Alder reaction as well as the use of this approach to visualize pancreatic tumor tissue in vivo as early as 1 h postinjection. Herein, we report a comprehensive structure: pharmacokinetic relationship study of a library of 25 novel radioligands that aims to identify radiotracers with optimal pharmacokinetic and dosimetric properties. This investigation revealed key relationships between molecular structure and in vivo behavior and produced two lead candidates exhibiting rapid tumor targeting with high target-to-backgroun

SUBMITTER: Meyer JP 

PROVIDER: S-EPMC6521719 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature