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drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An intravenous anti-CD19 antibody-drug conjugate (ADC) that delivers a pyrrolobenzodiazepine (PBD) dimer payload via a cleavable linker; after CD19 binding and internalization, it releases the payload to induce DNA interstrand cross-links, leading to cell-cycle arrest and apoptosis in malignant B cells.
nci_thesaurus_concept_id
C125549
nci_thesaurus_preferred_term
Loncastuximab Tesirine
nci_thesaurus_definition
An antibody-drug conjugate (ADC) consisting of an anti-CD19 humanized monoclonal antibody conjugated, via a cleavable linker comprised of valine-alanine and maleimide, to a cytotoxic, cross-linking agent pyrrolobenzodiazepine (PBD) dimer, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the monoclonal antibody portion of loncastuximab tesirine targets the cell surface antigen CD19 on various cancer cells. Upon antibody/antigen binding and internalization, the cytotoxic PBD moiety is released. The imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA and inhibits DNA replication, which inhibits the proliferation of CD19-overexpressing tumor cells. CD19, a transmembrane receptor and tumor-associated antigen (TAA), is expressed on a number of B-cell-derived cancers.
drug_mesh_term
loncastuximab tesirine
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Humanized anti-CD19 monoclonal antibody linked via a cleavable linker to a pyrrolobenzodiazepine (PBD) dimer payload; upon CD19 binding and internalization in malignant B cells, the payload is released to create DNA interstrand cross-links in the minor groove, inhibiting DNA replication and triggering cell-cycle arrest and apoptosis.
drug_name
Loncastuximab Tesirine
nct_id_drug_ref
NCT05660395