Drug intelligence / Profile preview

FAPI-46

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

Overview

FAPI-46 is a quinoline-based small molecule that acts as a fibroblast activation protein (FAP) inhibitor and is primarily used as a radiolabeled tracer for positron emission tomography (PET) imaging. When labeled with radioisotopes such as gallium 68 ([68Ga]Ga-FAPI-46), it enables the visualization of FAP-expressing cells, which are commonly found in cancer-associated fibroblasts within the tumor microenvironment. This makes it valuable for tumor detection, staging, and potentially therapy response assessment across various solid tumors. The compound has demonstrated high tumor retention and favorable tumor-to-background ratios in clinical studies, supporting its use in oncologic imaging[2][3][4][6][8][9][10]. Therapeutic versions using other isotopes (e.g., lutetium 177 or actinium 225) are also under investigation for targeted radiopharmaceutical therapy[5][7].

Other names
Actinium-225 FAPI-46Actinium225 FAPI-46Actinium 225 FAPI-46225Ac-labeled FAPI-46Actinium-225 fibroblast activation protein inhibitor-46Actinium225 fibroblast activation protein inhibitor-46Actinium 225 fibroblast activation protein inhibitor-46
02

Targets

FAP (Fibroblast activation protein alpha)

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