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177Lu-DOTA-EB-RGD2

Development stage: Phase 1
Lead developer: Beijing Tiantan Hospital
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration: Intravenous, Intratumoral

Overview

177Lu-DOTA-EB-RGD2 is an investigational radioligand therapy (RLT) consisting of the beta-emitting radioisotope Lutetium-177 conjugated to an Evans Blue (EB)-modified RGD2 peptide dimer. The RGD2 motif specifically targets integrin αvβ3, which is overexpressed in high-grade gliomas and tumor neovasculature. The Evans Blue modification allows for reversible binding to serum albumin, extending the drug's circulatory half-life and enhancing tumor accumulation and retention. Developed by Beijing Tiantan Hospital, it is currently being evaluated in Phase I clinical trials for the treatment of recurrent high-grade glioma via intravenous or locoregional administration.

Other names: Lutetium Lu 177 DOTA-EB-RGD2177Lu-EB-RGD2

Targets

αVβ3 (Integrin αVβ3)

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