Exploring Structural Parameters for Pretargeting Radioligand Optimization. Academic Article uri icon

Overview

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-background activity concentration ratios at early time points. We believe this knowledge to be of high value for the design and clinical translation of next-generation pretargeting agents for the diagnosis and treatment of disease.

publication date

  • September 20, 2017

Research

keywords

  • Neoplasms
  • Radiopharmaceuticals

Identity

PubMed Central ID

  • PMC6521719

Scopus Document Identifier

  • 85031280049

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.7b01108

PubMed ID

  • 28857566

Additional Document Info

volume

  • 60

issue

  • 19