99mTc-CTR-FAPI

99mTc-CTR-FAPI is a novel, covalent-engineered radiopharmaceutical diagnostic imaging agent targeting fibroblast activation protein (FAP). Developed using proprietary Covalent Targeted Radioligand (CTR) technology, it incorporates a sulfur (VI)-fluoride exchange (SuFEx) chemistry-based linker that enables irreversible covalent binding to FAP. This covalent mechanism provides enhanced tumor uptake, superior imaging contrast, and prolonged retention compared to non-covalent FAP inhibitors. Labeled with the single-photon emitter technetium-99m (99mTc), 99mTc-CTR-FAPI is designed for single-photon emission computed tomography (SPECT/CT) imaging, offering a cost-effective, low-radiation, and widely accessible alternative to positron emission tomography (PET/CT) tracers. It is being clinically evaluated for the assessment of rheumatoid arthritis (to monitor synovial lesions and joint involvement) and the detection of solid tumors, including lung cancer.

Other names

99mTc-TCR-FAPItechnetium Tc 99m covalent targeted fibroblast activation protein inhibitor