Drug intelligence / Profile preview

225Ac-GT-008

Development stage
Preclinical
Lead developer
Pentixapharm
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

225Ac-GT-008 is a first-in-class, glycan-dependent radioimmunotherapeutic consisting of a humanized IgG1 monoclonal antibody (GT-008) conjugated to the alpha-emitting radionuclide actinium-225 (225Ac). GT-008 selectively targets a tumor-associated O-glycoform of the cell surface glycoprotein CD24 (specifically in the presence of Thomsen-Friedenreich [TF] core-1 glycosylation), which is highly expressed on various solid tumors but has limited abundance on healthy tissues. This glycoform-selective binding minimizes on-target/off-tumor toxicities on normal CD24-expressing cells, such as immune cells. Upon binding and internalization, the actinium-225 payload delivers high-energy alpha radiation directly to the cancer cells, causing lethal double-strand DNA breaks. Developed by Pentixapharm (originally originated from Glycotope's GlycoTarget platform), 225Ac-GT-008 is in preclinical development for the treatment of solid tumors, including female cancers such as breast, endometrial, and ovarian cancers.

Other names
225Ac-labeled GT-008actinium-225 GT-008actinium225 GT-008actinium 225 GT-008
02

Targets

CD24 (Cluster of Differentiation 24)DNA

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