Drug intelligence / Profile preview

68Ga-FAPI

Development stage
Phase 2
Lead developer
SOFIE
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Gallium-68-labeled fibroblast activation protein inhibitor (68Ga-FAPI) is a radiopharmaceutical used primarily for positron emission tomography (PET) imaging. It targets the fibroblast activation protein (FAP), which is highly expressed in cancer-associated fibroblasts within the tumor stroma of many epithelial cancers, as well as in sites of fibrosis and inflammation. The compound consists of a FAP-targeted small molecule inhibitor conjugated to the DOTA chelator, which binds gallium-68 for PET imaging. This enables rapid and specific accumulation in FAP-expressing tissues with low background uptake, providing high contrast images for detecting primary and metastatic tumors—especially those with strong desmoplastic reactions such as breast, colon, pancreatic cancers, peritoneal carcinomatosis—as well as non-oncologic conditions like fibrosis and rheumatoid arthritis. The DOTA chelator also allows coupling to therapeutic radionuclides (e.g., yttrium‑90 or lutetium‑177) for theranostic applications[3][4][5][8].

Other names
gallium Ga 68-DOTA-FAPI-04gallium Ga 68-labeled fibroblast activation protein inhibitor
02

Targets

FAP (Fibroblast activation protein alpha)

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