drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An antibody–drug conjugate administered as monotherapy; a tumor‑antigen–binding monoclonal antibody delivers an intracellular topoisomerase I–inhibitor cytotoxic payload. After receptor‑mediated internalization and lysosomal release, the payload inhibits Top1, induces DNA damage, and triggers apoptosis, with potential bystander effects.
nci_thesaurus_concept_id
C200143
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) CD44 variant 9 (CD44v9), linked to the topoisomerase I inhibitor (TOP1i) and belotecan derivative KL610023 via a hydrolysable linker, with potential antineoplastic activity. Upon intravenous administration of anti-CD44v9 ADC AMT-116, the monoclonal antibody moiety targets and binds to CD44v9 expressed on tumor cells. Upon binding and internalization, KL610023 is released. KL610023 targets and binds to DNA topoisomerase I, thereby inhibiting DNA replication and killing the CD44v9-expressing cancer cells. CD44v9, a splicing variant of CD44 overexpressed in numerous cancer cell types, is associated with tumorigenicity and cancer treatment resistance.
drug_mesh_term
Antibody-Drug Conjugates
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
AMT-116 is a humanized IgG1 antibody–drug conjugate targeting CD44v9 on tumor cells. After antigen binding and receptor-mediated internalization, a hydrolysable linker is cleaved in lysosomes to release the belotecan-derived topoisomerase I inhibitor KL610023. The payload inhibits Top1, causing replication-associated DNA damage and apoptosis, with potential bystander killing of nearby tumor cells.
drug_name
AMT-116
nct_id_drug_ref
NCT06782334