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68Ga-FAPI-RGD + 177Lu-FAPI-RGD
- Development stage
- Preclinical
- Lead developer
- Peking Union Medical College Hospital
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
68Ga-FAPI-RGD + 177Lu-FAPI-RGD is a dual-targeting theranostic radiopharmaceutical combination that targets both fibroblast activation protein (FAP) and integrin αvβ3. The 68Ga-labeled component serves as a diagnostic PET imaging agent, while the 177Lu-labeled component functions as a therapeutic radiopharmaceutical. This combination has shown promising results in enhancing immunogenicity and synergizing with PD-L1 inhibitors for improved antitumor efficacy. The heterodimeric peptide combines FAPI-02 and cyclo-RGD-d-Phe-Lys (c[RGDfK]) to simultaneously target both FAP-expressing cancer-associated fibroblasts and integrin αvβ3-expressing tumor cells or tumor endothelial cells. The 177Lu component demonstrates superior efficacy compared to 68Ga in therapeutic applications due to its longer half-life and greater tissue penetration range.
- Other names
- 68Ga/177Lu-DOTA-2P(FAPI)268Ga-DOTA-2P(FAPI)2 + 177Lu-DOTA-2P(FAPI)2DOTA-FAPI-RGD
02
Targets
FAP (Fibroblast activation protein alpha)αVβ3 (Integrin αVβ3)
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