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Drug intelligence / Profile preview
cetuximab + monomethyl auristatin E
- Development stage
- Preclinical
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Cetuximab + monomethyl auristatin E (CTX-MMAE) is an antibody-drug conjugate (ADC) that targets the epidermal growth factor receptor (EGFR). It consists of the chimeric monoclonal antibody cetuximab linked to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline-p-aminobenzyloxycarbonyl (vc-PAB) linker. The ADC is designed to bind to EGFR-expressing tumor cells, undergo internalization, and release MMAE in the lysosomal compartment through cathepsin B-mediated cleavage. Released MMAE inhibits tubulin polymerization, leading to G2/M phase cell cycle arrest and subsequent apoptosis. CTX-MMAE has shown preclinical activity in models of non-small cell lung cancer (NSCLC) and pancreatic cancer, including those with EGFR or KRAS mutations that may be resistant to cetuximab monotherapy.
- Other names
- cetuximab-vc-PAB-MMAEcetuximab-MMAEErbitux-MMAE
02
Targets
EGFR (Epidermal growth factor receptor)TUBB (Tubulin (alpha and beta subunits))
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