[68Ga]Ga-DOTA-Trip5

`[68Ga]Ga-DOTA-Trip5` (also referred to as `68Ga-Trip-5`) is a novel gallium-68 labeled peptide-based radiopharmaceutical designed for positron emission tomography (PET) imaging of prostate cancer. It specifically targets the six-transmembrane epithelial antigen of the prostate 2 (STEAP2), a cell-surface antigen highly overexpressed in prostate cancer. Developed by researchers at Peking University Cancer Hospital & Institute, the probe was created using a molecular docking-guided drug repurposing strategy starting from the GnRH agonist triptorelin. Triptorelin was structurally optimized via acetylation, PEG extension, and 4-iodophenylbutyric acid conjugation to enhance in vivo stability and pharmacokinetics. Preclinical evaluations in 22Rv1 prostate cancer xenograft models demonstrate high targeting affinity, specificity, and favorable tumor-to-background contrast, suggesting significant potential for the non-invasive diagnostic detection of STEAP2-positive prostate cancers, particularly in patients with low or absent PSMA expression.

Other names

68Ga-Trip-568Ga-Trip5DOTA-Trip5DOTA-Trip-5DOTA-Trip 5Trip-5Trip5Trip 5