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Drug intelligence / Profile preview
[68Ga]Ga-CTR-FAPI-30
- Development stage
- Unknown
- Lead developer
- Peking-Tsinghua Center for Life Sciences
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[68Ga]Ga-CTR-FAPI-30 is a gallium-68 labeled covalent targeted radioligand (CTR) designed to inhibit fibroblast activation protein (FAP). Unlike conventional FAP inhibitors (FAPIs) that bind reversibly to the target, CTR-FAPI-30 utilizes a covalent binding mechanism to form a stable, irreversible bond with the FAP enzyme. This approach is intended to enhance tumor retention and improve the target-to-background ratio in positron emission tomography (PET) imaging. It is primarily being developed as a diagnostic imaging agent for the precise localization of malignant lesions in medullary thyroid carcinoma (MTC), facilitating staging and surgical planning. Clinical data suggests it offers superior diagnostic accuracy, sensitivity, and specificity compared to conventional imaging modalities like CT and ultrasound.
- Other names
- Gallium-68 CTR-FAPI-30Gallium68 CTR-FAPI-30Gallium 68 CTR-FAPI-3068Ga-labeled covalent FAP inhibitor 30
02
Targets
FAP (Fibroblast activation protein alpha)
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