PET Imaging of PARP Expression Using ¹⁸F-Olaparib.

ABSTRACT: Poly(ADP-ribose) polymerase (PARP) inhibitors are increasingly being studied as cancer drugs, as single agents, or as a part of combination therapies. Imaging of PARP using a radiolabeled inhibitor has been proposed for patient selection, outcome prediction, dose optimization, genotoxic therapy evaluation, and target engagement imaging of novel PARP-targeting agents. Methods: Here, via the copper-mediated ¹⁸F-radiofluorination of aryl boronic esters, we accessed, for the first time (to our knowledge), the ¹⁸F-radiolabeled isotopolog of the Food and Drug Administration-approved PARP inhibitor olaparib. The use of the ¹⁸F-labeled equivalent of olaparib allows direct prediction of the distribution of olaparib, given its exact structural likeness to the

SUBMITTER: Wilson TC 

PROVIDER: S-EPMC6448459 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature