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[177Lu]Lu-EB-DOTA-(PEG28)2-A20FMDV2
- Development stage
- Preclinical
- Lead developer
- Washington University School of Medicine
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
[177Lu]Lu-EB-DOTA-(PEG28)2-A20FMDV2 is a targeted radiopharmaceutical therapy designed for the treatment of cancers overexpressing the integrin αvβ6 receptor. The drug consists of the A20FMDV2 peptide, a 20-amino-acid sequence derived from the foot-and-mouth disease virus that specifically binds to αvβ6, conjugated to a DOTA chelator for radiolabeling with the beta-emitting radionuclide Lutetium-177. To improve its pharmacokinetic profile, the construct incorporates an Evans Blue (EB) moiety that reversibly binds to serum albumin, extending its blood circulation half-life and enhancing tumor accumulation. Additionally, bi-terminal PEGylation (PEG28) is utilized to further stabilize the peptide and optimize biodistribution. Preclinical studies conducted at Washington University School of Medicine have demonstrated that this agent provides significant tumor growth inhibition in pancreatic cancer models, although its clinical utility may be limited by high renal uptake and associated toxicity.
- Other names
- 177Lu-EB-DOTA-(PEG28)2-A20FMDV2EB-DOTA-(PEG28)2-A20FMDV2
02
Targets
αVβ6 (Integrin αVβ6)
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