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eFAP-6

Development stage: Preclinical
Lead developer: Erasmus MC
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration: Intravenous

Overview

eFAP-6 is a novel fibroblast activation protein (FAP)-targeting radioligand developed by Erasmus MC. Chemically, it is a DOTA-conjugated small molecule based on an 8-substituted (4-quinolinoyl)-glycyl-2-cyanopyrrolidine (8-QCP) core structure. eFAP-6 exhibits high affinity for FAP (IC50 of approximately 0.5–0.6 nM) and rapid internalization in FAP-expressing cells. When labeled with radionuclides such as indium-111 ([111In]In-eFAP-6) or lutetium-177 ([177Lu]Lu-eFAP-6), it demonstrates rapid tumor accumulation and fast renal clearance, making it a promising candidate for targeted radionuclide imaging of solid tumors.

Other names: DOTA-eFAP-6DOTA-eFAP6DOTA-eFAP 6[111In]In-eFAP-6[177Lu]Lu-eFAP-6

Targets

FAP (Fibroblast activation protein alpha)

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