Drug intelligence / Profile preview

68Ga-FAPI-RGD

Development stage
Phase 2
Lead developer
Yantai Lannacheng Biotechnology
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

68Ga-FAPI-RGD is a dual-receptor targeting PET radiotracer that binds to both fibroblast activation protein (FAP) and integrin αvβ3. This heterodimeric radiotracer combines a fibroblast activation protein inhibitor (FAPI) with an Arg-Gly-Asp (RGD) peptide, radiolabeled with gallium-68. It demonstrates high specificity and rapid internalization into target cells, with improved tumor uptake and tumor-to-background ratio compared to conventional 18F-FDG PET/CT. The effective dose from 68Ga-FAPI-RGD PET/CT is approximately 1.01 × 10^-2 mSv/MBq, with the thyroid receiving the highest effective dose followed by the urinary bladder wall, liver, and lungs.

Other names
Gallium 68-labeled fibroblast activation protein inhibitor-RGDGallium68-labeled fibroblast activation protein inhibitor-RGDGallium-68-labeled fibroblast activation protein inhibitor-RGD
02

Targets

FAP (Fibroblast activation protein alpha)αVβ3 (Integrin αVβ3)

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