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68Ga-FAPI + 177Lu-EB-FAPI

Development stage
Unknown
Lead developer
Jiangsu Institute of Nuclear Medicine
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

This is a combination of two radiopharmaceutical agents used in oncology for diagnosis and therapy targeting the fibroblast activation protein (FAP) expressed by cancer-associated fibroblasts (CAFs) in the tumor microenvironment. **68Ga-FAPI** is a positron emission tomography (PET) imaging agent that consists of a gallium-68 labeled fibroblast activation protein inhibitor. It enables non-invasive visualization of FAP-expressing tumors and metastases. **177Lu-EB-FAPI** is a therapeutic radioligand composed of lutetium-177 conjugated to an Evans Blue-modified FAP inhibitor via DOTA chelation. The Evans Blue moiety extends blood circulation time by binding to albumin, enhancing tumor uptake and retention. This agent delivers targeted beta radiation to FAP-expressing cells for internal radiotherapy ("theranostics"). The combination allows for both precise diagnostic imaging with 68Ga-FAPI PET/CT and subsequent targeted radionuclide therapy with 177Lu-EB-FAPI in patients with metastatic or advanced solid tumors[1][2][5]. Both agents are under clinical investigation.

Other names
68Ga-labeled fibroblast activation protein inhibitorGallium-68 FAPIGallium68 FAPIGallium 68 FAPILutetium-177 Evans Blue FAPILutetium177 Evans Blue FAPILutetium 177 Evans Blue FAPILutetium-177 DOTA-EB-FAPiLutetium177 DOTA-EB-FAPiLutetium 177 DOTA-EB-FAPi
02

Targets

FAP (Fibroblast activation protein alpha)

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