Drug intelligence / Profile preview

DOTA-FAPI-04

Development stage
Unknown
Lead developer
The First Hospital of Fujian Medical University
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

DOTA-FAPI-04 is a quinoline-based fibroblast activation protein (FAP) inhibitor that serves as a radiotracer for positron emission tomography (PET) imaging. It is typically labeled with the radioisotope gallium-68 ([^68^Ga]), resulting in [^68^Ga]Ga-DOTA-FAPI-04. This compound targets FAP, which is highly expressed on cancer-associated fibroblasts in the tumor microenvironment and upregulated during tissue fibrosis. By binding to FAP with high affinity and rapid blood clearance, DOTA-FAPI-04 enables non-invasive visualization of tumors and fibrotic processes using PET/CT or PET/MRI imaging. It has demonstrated superior sensitivity compared to standard tracers like [^18F]FDG for detecting certain metastases (e.g., bone and peritoneal), as well as potential utility in monitoring liver fibrosis[1][5][6][8][9].

Other names
gallium Ga 68-DOTA-FAPI-04[^68^Ga]Ga-DOTA-FAPi-04
02

Targets

FAP (Fibroblast activation protein alpha)

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