drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
TROP2-directed antibody-drug conjugate composed of a human monoclonal antibody linked to the microtubule inhibitor prodrug MMAE; binds TROP2 on tumor cells, is internalized, and releases MMAE to disrupt microtubules and induce apoptosis.
nci_thesaurus_concept_id
C202102
nci_thesaurus_preferred_term
Anti-TROP-2/MMAE Antibody-drug Conjugate LCB84
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of Hu2G10, a humanized immunoglobulin G1 (IgG1) monoclonal antibody that targets the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1), conjugated via a beta-glucuronidase-cleavable linker to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of anti-TROP-2/MMAE ADC LCB84, the anti-TROP-2 antibody targets and binds to TROP-2 expressed on tumor cells. Upon binding and internalization, MMAE is released upon cleavage by the cancer-associated lysosomal enzyme beta-glucuronidase. MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. This induces cell death in TROP-2-expressing cancer cells. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
TROP2-targeted human IgG1 antibody-drug conjugate linked via a beta-glucuronidase-cleavable linker to the microtubule inhibitor MMAE. After binding TROP2 and internalization, linker cleavage releases MMAE, which binds tubulin, inhibits microtubule polymerization, causes G2/M arrest, and induces apoptosis (with potential bystander killing).
drug_name
LCB84
nct_id_drug_ref
NCT05941507