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drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
Anti-HER2 antibody–drug conjugate carrying the microtubule inhibitor DM1, causing microtubule disruption.
nci_thesaurus_concept_id
C82492
nci_thesaurus_preferred_term
Trastuzumab Emtansine
nci_thesaurus_definition
An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers.
drug_mesh_term
Ado-Trastuzumab Emtansine
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Anti-HER2 monoclonal antibody (trastuzumab) conjugated to the microtubule inhibitor DM1 via a nonreducible linker. The antibody binds HER2 on tumor cells and is internalized; intracellular DM1 binds tubulin, disrupting microtubule dynamics to cause mitotic arrest and cell death. The trastuzumab component also inhibits HER2 signaling and can mediate ADCC.
drug_name
Trastuzumab emtansine
nct_id_drug_ref
NCT06324357