ImmunoPET Imaging of Endogenous and Transfected Prolactin Receptor Tumor Xenografts.

Antibodies labeled with positron-emitting isotopes have been used for tumor detection, predicting which patients may respond to tumor antigen-directed therapy, and assessing pharmacodynamic effects of drug interventions. Prolactin receptor (PRLR) is overexpressed in breast and prostate cancers and is a new target for cancer therapy. We evaluated REGN2878, an anti-PRLR monoclonal antibody, as an immunoPET reagent.

Repeatability of [Ga]DKFZ11-PSMA PET Scans for Detecting Prostate-specific Membrane Antigen-positive Prostate Cancer.

Purpose: We studied the effect of varying specific activity of [Ga]DKFZ-PSMA11 ([Ga]DP11) on repeated imaging of prostate-specific membrane antigen-positive (PSMA+) xenograft tumors.

Procedures: Athymic nude mice bearing PC3-PIP (PSMA+) and PC3 (PSMA-) bilateral flank tumors were assessed to study intra- and inter-day repeatability of [Ga]DP11 imaging in mice administered [Ga]DP11 or [Ga]DP11 (as a dilution tracer) using imaging and biodistribution studies.

Results: Region of interest (ROI) analysis of the [Ga]DP11 imaging study indicated that the uptake was constant on the same day or consecutive days.

Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.

Tyrosine kinases often play pivotal roles in the pathogenesis of cancer and are good candidates for therapeutic intervention and targeted molecular imaging. The precursor synthesis, radiosynthesis, and biological characterization of a fluorine-18 analog of dasatinib, a multitargeted kinase inhibitor, are reported. Compound 5 potently inhibits Abl, Src, and Kit kinases and inhibits K562 and M07e/p210bcr-abl human leukemic cell growth.