drug_type
RELEVANT_DRUG
intervention_type
Antibody–drug conjugate
drug_description
Intravenous antibody–drug conjugate (ado-trastuzumab emtansine, T-DM1) linking trastuzumab to the maytansinoid DM1 via a non-cleavable linker; binds HER2, inhibits signaling, mediates ADCC, and delivers DM1 to disrupt microtubules causing mitotic arrest and apoptosis, including activity in brain metastases.
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 monoclonal antibody (trastuzumab) linked via a non-cleavable linker to the maytansinoid DM1. Binds HER2 to inhibit signaling and mediate ADCC; after internalization, DM1 binds tubulin to disrupt microtubules, causing mitotic arrest and apoptosis in HER2-overexpressing tumor cells.
drug_name
Trastuzumab emtansine
nct_id_drug_ref
NCT05673928