Preferred Label : Integrin AlphaVbeta3-targeted Small Molecule-drug Conjugate VIP236;
NCIt synonyms : Integrin AlphaVbeta3-targeted Topoisomerase I Inhibitor VIP236; Integrin AlphaVbeta3-targeted SMDC VIP236;
NCIt definition : A small molecule-drug conjugate (SMDC) composed of an integrin alphaVbeta3 binder
conjugated, via a cleavable linker, to a camptothecin-based topoisomerase I inhibitor,
with potential antineoplastic activity. Upon administration of integrin alphaVbeta3-targeted
SMDC VIP236, the integrin alphaVbeta3 binder targets and binds to integrin alphaVbeta3
expressed on tumor cells and tumor vessel endothelial cells. Upon binding and linker
cleavage by neutrophil elastase in the tumor microenvironment (TME), the camptothecin-based
topoisomerase I inhibitor is released. The topoisomerase I inhibitor inhibits DNA
topoisomerase I activity, thereby inhibiting DNA replication and generating DNA single-
and double-strand breaks, and leading to cell cycle arrest and apoptosis. This inhibits
the proliferation of integrin alphaVbeta3-expressing tumor cells, angiogenesis and
metastasis. Integrin alphaVbeta3, a cell adhesion and signaling receptor, is overexpressed
on the surface of tumor vessel endothelial cells, some tumor cells, and a number of
other cell types.;
Molecule name : VIP 236; VIP-236;
NCI Metathesaurus CUI : CL1907041;
Origin ID : C200199;
UMLS CUI : C5854494;
Semantic type(s)
- concept_is_in_subset
- has_target
