Drug intelligence / Profile preview

90Y-DOTA-αGPC3

Development stage
Preclinical
Lead developer
Stanford University
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**90Y-DOTA-αGPC3** is a radiopharmaceutical composed of the monoclonal antibody αGPC3, which targets glypican-3 (GPC3), a cell-surface proteoglycan highly expressed on hepatocellular carcinoma (HCC) cells. The antibody is conjugated via the chelator DOTA to the radioisotope yttrium-90 (90Y), a high-energy beta emitter. This agent is designed for radioimmunotherapy (RIT), enabling targeted delivery of cytotoxic radiation to GPC3-positive tumor cells while sparing normal tissues. Preclinical studies in orthotopic murine models of HCC demonstrate its ability to localize to tumors, induce tumor cell apoptosis, halt or reduce tumor growth, and significantly decrease serum alpha-fetoprotein (AFP), indicating reduction in tumor burden. The construct acts through dual mechanisms: antibody-mediated recognition and targeted radiotoxicity from the β-particle emission of 90Y. It is currently at the preclinical research stage; clinical trials have not been identified for this exact conjugate[1][3].

Other names
Yttrium-90-DOTA-αGPC3Y-90-GPC3Y90-GPC3Y 90-GPC3Yttrium-90 anti-glypican 3-DOTAYttrium90 anti-glypican 3-DOTAYttrium 90 anti-glypican 3-DOTA90Y-αGPC3
02

Targets

GPC3 (Glypican-3)

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