drug_type
RELEVANT_DRUG
intervention_type
antibody‑drug conjugate (ADC)
drug_description
CD19‑directed antibody‑drug conjugate that delivers a pyrrolobenzodiazepine (PBD) cytotoxic payload to 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. After binding CD19 on B cells and internalization, the linker is cleaved to release the PBD payload, which binds the DNA minor groove and forms interstrand cross‑links (N2 of guanine), blocking DNA replication and inducing cytotoxicity in CD19‑expressing tumor cells.
drug_name
Loncastuximab tesirine
nct_id_drug_ref
NCT05991388