drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate (ADC)
drug_description
HER2-targeted antibody-drug conjugate linking trastuzumab to the microtubule inhibitor DM1; after HER2 binding and internalization, DM1 disrupts microtubules while trastuzumab retains HER2 blockade and ADCC.
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
HER2-targeted antibody–drug conjugate linking trastuzumab to the microtubule inhibitor DM1 via a nonreducible linker. After HER2 binding and internalization, intracellular DM1 disrupts microtubule dynamics to inhibit cell division and induce apoptosis, while the trastuzumab component blocks HER2 signaling and mediates Fc-dependent ADCC.
drug_name
Trastuzumab emtansine
nct_id_drug_ref
NCT06313086