Exploring Hydrophilic PD-L1 Radiotracers Utilizing Phosphonic Acids: Insights into Unforeseen Pharmacokinetics.

ABSTRACT: Immune checkpoint inhibitor therapy targeting the PD-1/PD-L1 axis in cancer patients, is a promising oncological treatment. However, the number of non-responders remains high, causing a burden for the patient and the healthcare system. Consequently, a diagnostic tool to predict treatment outcomes would help with patient stratification. Molecular imaging provides said diagnostic tool by offering a whole-body quantitative assessment of PD-L1 expression, hence supporting therapy decisions. Four PD-L1 radioligand candidates containing a linker-chelator system for radiometalation, along with three hydrophilizing units-one sulfonic and two phosphonic acids-were synthesized. After labeling with ⁶⁴Cu, log D_7.4 values of less than -3.03 were determined and proteolytic s

SUBMITTER: Krutzek F 

PROVIDER: S-EPMC10606431 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature