Preferred Label : Emiltatug Ledadotin;
NCIt synonyms : Anti-B7-H4 ADC XMT-1660; Anti-B7-H4 Antibody-drug Conjugate XMT-1660;
NCIt definition : An antibody-drug conjugate (ADC) composed of emiltatug, a human immunoglobulin G1
(IgG1) monoclonal antibody directed against the T-cell checkpoint ligand B7-H4 (V-set
domain-containing T-cell activation inhibitor 1; VTCN1; B7x; B7S1), site-specifically
conjugated to six cytotoxic auristatin derivative auristatin F-HPA (AF-HPA; auristatin
F-hydroxypropylamide) payloads per antibody, with potential antineoplastic activity.
Upon administration of emiltatug ledadotin, the anti-B7-H4 monoclonal antibody moiety
targets and binds to B7-H4 expressed on tumor cells. Upon binding, internalization
and linker cleavage, membrane permeating AF-HPA is metabolically converted to membrane
non-permeating auristatin F, which binds to tubulin and inhibits microtubule polymerization.
This results in G2/M phase arrest and the apoptosis of B7-H4-expressing tumor cells.
B7-H4, a member of the B7 family of immune modulators, is upregulated in a variety
of tumor cell types and tumor-associated macrophages (TAMs). It negatively regulates
T-cell immune responses. The metabolic conversion of membrane permeating AF-HPA to
membrane non-permeating auristatin F results in a controlled bystander effect, and
prevents or lessens neutropenia as an adverse effect of auristatin.;
UNII : PTB6AF3CSV;
CAS number : 2855974-40-0;
Molecule name : XMT 1660; XMT-1660;
NCI Metathesaurus CUI : CL1794137;
Origin ID : C189237;
UMLS CUI : C5706542;
Semantic type(s)
- concept_is_in_subset
- has_target
