A novel PSMA-targeting tracer with highly negatively charged linker demonstrates decreased salivary gland uptake in mice compared to [⁶⁸Ga]Ga-PSMA-11.

ABSTRACT:

Background

The current generation of radiolabeled PSMA-targeting therapeutic agents is limited by prominent salivary gland binding, which results in dose-limiting xerostomia from radiation exposure. JB-1498 is a urea-based small molecule with a highly negatively charged linker targeting prostate specific membrane antigen (PSMA). Prior work on a similar tracer with the same negatively charged linker demonstrated low normal organ/soft tissue background uptake compared to [⁶⁸Ga]Ga-PSMA-11. The purpose of this study was to investigate if [⁶⁸Ga]Ga-JB-1498 had reduced salivary gland uptake in mice compared to [⁶⁸Ga]Ga-PSMA-11.

Results

JB-1498 demonstrated high affinity for PSMA binding and tumor uptake in a murine tumor model. In an initial biodist

SUBMITTER: Huang SS 

PROVIDER: S-EPMC10828251 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature