Drug intelligence / Profile preview

[18F]-FAPI-74

Development stage
Phase 3
Lead developer
SOFIE
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]-FAPI-74 is a fluorine-18 labeled fibroblast activation protein inhibitor (FAPI) developed as a diagnostic radiopharmaceutical for positron emission tomography (PET) imaging. It targets the fibroblast activation protein (FAP), which is overexpressed in cancer-associated fibroblasts within the tumor microenvironment of many epithelial cancers. By binding to FAP and being labeled with the positron-emitting isotope fluorine-18, [18F]-FAPI-74 enables high-resolution PET imaging of tumors expressing this target. Compared to earlier gallium-labeled FAPIs, it offers higher synthetic yield and better image resolution. Its primary clinical use under investigation is for detecting and staging various cancers—including gastrointestinal malignancies such as hepatocellular carcinoma, cholangiocarcinoma, gastric cancer, pancreatic cancer, colorectal cancer—as well as other solid tumors like lung and breast cancers. The agent has shown higher uptake in malignant lesions compared to nonmalignant tissue and may outperform standard tracers like [^18]FDG in certain settings[1][3][5]. It is currently being evaluated in Phase 2 clinical trials for its diagnostic performance.

Other names
18F-Fibroblast Activation Protein InhibitorFluorine F 18 FAPI-74Fibroblast activation protein inhibitor radiolabeled with [18F]
02

Targets

FAP (Fibroblast activation protein alpha)

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