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M-GB
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
M-GB is a modified small molecule inhibitor of cysteine cathepsins, specifically designed to serve as a payload for antibody-drug conjugates (ADCs). It is a derivative of the broad-spectrum cathepsin inhibitor GB111-NH2, modified with a maleimide linker to enable site-specific conjugation to antibodies. While M-GB itself has poor cell permeability, its conjugation to a targeting antibody (such as an anti-CD74 antibody) allows for selective internalization into malignant cells. Once inside the cell, M-GB inhibits cathepsin activity, which induces apoptosis and activates caspase-3. This therapeutic approach is primarily investigated for B-cell malignancies, including diffuse large B-cell lymphoma (DLBCL) and chronic lymphocytic leukemia (CLL), and is intended to address treatment resistance in these conditions.
- Other names
- maleimide-modified GB111-NH2modified GB111-NH2
02
Targets
CTSS (Cathepsin S)CTSB (Cathepsin B)CTSL (Cathepsin L)
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