Development and Preclinical Evaluation of [⁶⁸Ga]BMSH as a New Potent Positron Emission Tomography Tracer for Imaging Programmed Death-Ligand 1 Expression.

ABSTRACT: Immunotherapy targeting the programmed death-ligand 1 (PD-L1)/programmed cell death protein 1 (PD-1) pathway has shown remarkable efficacy against various cancers, but the overall response rate (ORR) is still low. PD-L1 expression in tumors may predict treatment response to immunotherapy. Indeed, ongoing clinical studies utilize a few PD-L1 radiotracers to assess PD-L1 expression as a predictive biomarker for immunotherapy. Here, we present a novel positron emission tomography (PET) radiotracer called [⁶⁸Ga]BMSH, which is derived from a small molecule inhibitor specifically targeting the binding site of PD-L1. The inhibitor was modified to optimize its in vivo pharmacokinetic properties and enable chelation of ⁶⁸Ga. In vitro evaluation revealed [⁶⁸Ga]BMSH p

SUBMITTER: Huang Y 

PROVIDER: S-EPMC10610256 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature