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[68Ga]Ga-FAPI-mFS
- Development stage
- Unknown
- Lead developer
- Peking University
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[68Ga]Ga-FAPI-mFS is a first-generation, covalent, fibroblast activation protein (FAP)-targeted radioligand developed by researchers at Peking University and collaborators. It is designed for positron emission tomography (PET) imaging of FAP-expressing tumors, such as medullary thyroid carcinoma (MTC) and pancreatic ductal adenocarcinoma (PDAC). Unlike conventional, reversible FAP inhibitors (such as FAPI-04) that suffer from rapid clearance and short tumor retention, [68Ga]Ga-FAPI-mFS incorporates an aryl-sulfone fluoride (FS) covalent warhead at the meta position. This warhead undergoes a sulfur(VI) fluoride exchange (SuFEx) reaction to form a stable, irreversible covalent bond with tyrosine residues (specifically Y450) in the FAP binding pocket. This covalent targeted radioligand (CTR) strategy significantly enhances tumor uptake and prolongs retention time while maintaining rapid clearance from healthy tissues, thereby improving diagnostic sensitivity and lesion detection.
- Other names
- 68Ga-FAPI-mFS[68Ga]Ga-FAPi-mFSFAPI-mFS
02
Targets
FAP (Fibroblast activation protein alpha)
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