drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An intravenous antibody–drug conjugate (ADC) composed of an anti–Nectin-4 monoclonal antibody that binds Nectin-4 (PVRL4) on tumor cells, is internalized, and releases an intracellular cytotoxic payload to kill Nectin-4–expressing cells, with potential bystander effect.
nci_thesaurus_concept_id
C204904
nci_thesaurus_preferred_term
Anti-nectin-4 Antibody-drug Conjugate LY4101174
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 (IgG1) Fcg-silent monoclonal antibody directed against the cell surface adhesion molecule and tumor-associated antigen (TAA) nectin-4 (PVRL4) conjugated, via maleimide-beta-glucuronide poly-sarcosine linkers, to the camptothecin analog and topoisomerase 1 inhibitor exatecan, with potential antineoplastic activity. Upon administration of the anti-nectin-4 ADC LY4101174, the anti-nectin-4 antibody targets and binds to nectin-4 expressed on tumor cells. Upon binding and internalization, exatecan is released. Exatecan inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of nectin-4-expressing tumor cells. Nectin-4, a TAA belonging to the nectin family, is overexpressed in a variety of cancers.
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
LY4101174 is an intravenous anti–Nectin-4 IgG1 antibody–drug conjugate that binds Nectin-4 (PVRL4) on tumor cells, is internalized, and releases the topoisomerase I inhibitor exatecan via a cleavable linker, causing inhibition of DNA replication, cell‑cycle arrest, and apoptosis of Nectin‑4–expressing cells, with potential bystander effect.
drug_name
LY4101174
nct_id_drug_ref
NCT06238479