Preferred Label : Anti-B7-H4 Antibody-drug Conjugate XMT-1660;
NCIt synonyms : Anti-B7-H4 ADC XMT-1660;
NCIt definition : An antibody-drug conjugate (ADC) composed of XMT-1604, 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 anti-B7-H4 ADC XMT-1660, 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.;
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
