drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
An anti-HER2 antibody–drug conjugate (also known as RC48-ADC) consisting of a humanized IgG1 anti-HER2 antibody linked via a valine–citrulline linker to the cytotoxic payload monomethyl auristatin E (MMAE). It binds HER2 on tumor cells, is internalized, and releases MMAE to inhibit tubulin polymerization, causing mitotic arrest and apoptosis; may also exert Fc-mediated effects.
nci_thesaurus_concept_id
C169918
nci_thesaurus_preferred_term
Disitamab Vedotin
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of trastuzumab vedotin, the trastuzumab moiety targets and binds to HER2 on the surface of tumor cells. Following internalization, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Anti-HER2 IgG1 antibody–drug conjugate that binds HER2 (ERBB2) on tumor cells, is internalized, and—via a protease-cleavable valine–citrulline linker—releases monomethyl auristatin E (MMAE), which inhibits tubulin polymerization to induce G2/M arrest and apoptosis; the IgG1 may also engage Fc-mediated effector functions (e.g., ADCC).
drug_name
Disitamab vedotin
nct_id_drug_ref
NCT05785325