Drug intelligence / Profile preview

depatuxizumab mafodotin

Development stage
Phase 3
Lead developer
AbbVie
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Depatuxizumab mafodotin is an antibody-drug conjugate (ADC) developed for the treatment of cancer, particularly glioblastoma and other solid tumors. It consists of a humanized IgG1 monoclonal antibody (depatuxizumab) targeting the epidermal growth factor receptor (EGFR), including tumor-specific EGFR epitopes and mutant forms such as EGFRvIII, conjugated via a stable maleimidocaproyl linker to the cytotoxic agent monomethyl auristatin F (MMAF), a tubulin inhibitor. Upon binding to EGFR-expressing tumor cells, the ADC is internalized and releases MMAF intracellularly, leading to inhibition of tubulin polymerization, mitotic arrest, apoptosis induction, and subsequent cell death. The drug was granted orphan drug status for glioblastoma but its development was discontinued after late-stage clinical trial failures[1][3][5][6].

Brand names
Depatux-M
Other names
depatuxizumab mafodotinABT-414ABT414ABT 414Depatux-M
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))EGFRvIII (Epidermal growth factor receptor variant III)

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