drug_type
RELEVANT_DRUG
intervention_type
Drug (antibody–drug conjugate)
drug_description
HER2-targeted antibody–drug conjugate (T-DM1) that delivers the maytansinoid microtubule inhibitor DM1.
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 nonreducible thioether (MCC) to the maytansinoid DM1; after binding HER2 and internalization, DM1 is released intracellularly to bind tubulin and disrupt microtubule dynamics, inhibiting cell division and inducing cancer cell death. Trastuzumab also inhibits HER2 signaling and can mediate Fc-dependent immune effector functions.
drug_name
Trastuzumab Emtansine
nct_id_drug_ref
NCT05408845