drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An antibody–drug conjugate targeting CD19; an anti-CD19 monoclonal antibody linked to the PBD-dimer cytotoxic payload tesirine that induces DNA interstrand crosslinks leading to apoptosis in CD19-positive 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
Anti-CD19 monoclonal antibody targets CD19 on B cells and is internalized; a cleavable linker releases the PBD-dimer payload (tesirine), which binds the DNA minor groove and forms interstrand crosslinks at guanine N2 positions, blocking DNA replication and triggering apoptosis in CD19-positive tumor cells.
drug_name
Loncastuximab tesirine
nct_id_drug_ref
NCT05672251