Drug intelligence / Profile preview

AGS67E

Development stage
Phase 1
Lead developer
Astellas Pharma
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

AGS67E is an antibody-drug conjugate (ADC) developed for the treatment of hematologic malignancies, particularly B-cell and T-cell cancers such as non-Hodgkin lymphoma (NHL), chronic lymphocytic leukemia (CLL), and acute myeloid leukemia (AML). It consists of a fully human monoclonal IgG2 antibody targeting CD37, a tetraspanin protein highly expressed on malignant B cells and also present in T-cell lymphomas and AML. The antibody component (AGS67C) is conjugated via a protease-cleavable linker to monomethyl auristatin E (MMAE), a potent microtubule-disrupting agent. Upon binding to CD37-expressing cells, AGS67E is internalized, releasing MMAE inside the cell to inhibit tubulin polymerization, leading to cell cycle arrest and apoptosis. Preclinical studies demonstrated cytotoxicity against NHL, CLL, T-cell lymphoma, and AML models. Clinical development included phase 1 trials in relapsed/refractory NHLs and CLL.

02

Targets

TUBB (Tubulin (alpha and beta subunits))CD37

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