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⁶⁸Ga-DOTA-SIGMA-3
- Development stage
- Preclinical
- Lead developer
- Air Force Military Medical University
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
⁶⁸Ga-DOTA-SIGMA-3 is a novel gallium-68 labeled radiopharmaceutical and PET imaging probe designed to target the sigma-2 receptor (σ₂ receptor / TMEM97), a well-established biomarker for tumor proliferation. Developed by Xijing Hospital (Fourth Military Medical University), the probe utilizes a structure-guided optimization strategy where a DOTA chelator is conjugated to a σ₂ receptor-targeting scaffold, with lipophilicity modulated via a glycine-based spacer. In preclinical models of glioblastoma, ⁶⁸Ga-DOTA-SIGMA-3 demonstrated high specificity, rapid tumor uptake, and favorable imaging contrast with significantly reduced hepatic and intestinal accumulation compared to older fluorine-18 or technetium-99m labeled analogs. It is currently in preclinical development for tumor proliferation imaging, particularly in glioblastoma.
- Other names
- Ga-68-DOTA-SIGMA-3Ga68-DOTA-SIGMA-3Ga 68-DOTA-SIGMA-3
02
Targets
TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))
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