Preferred Label : Tosposertib;
NCIt synonyms : TGFbeta Antagonist TU2218; TGFb Inhibitor TU2218; TGF-beta Inhibitor TU2218; TGFbeta Inhibitor TU2218;
NCIt definition : An orally bioavailable inhibitor of transforming growth factor-beta (TGFb), with potential
antineoplastic and anti-fibrotic activities. Upon oral administration, tosposertib
specifically targets, binds to and inhibits TGFb, which prevents both the binding
of TGFb to its receptor TGFbR and TGFb-mediated signal transduction. This abrogates
TGFb-mediated fibrosis and immunosuppression, enhances anti-tumor immunity in the
tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated
immune response against tumor cells leading to tumor cell death. This may lead to
a reduction in TGFb-dependent proliferation of cancer cells. The TGFb signaling pathway
is often upregulated and activated in fibrotic diseases and deregulated in tumors
and plays a key role in the regulation of cell growth, differentiation, apoptosis,
motility, invasion, and angiogenesis. It plays a key role in immunosuppression in
the TME.;
UNII : UZ6A2QUZ5Z;
CAS number : 1418305-55-1;
Molecule name : TU-2218; NCE-401; TU 2218; NCE 401;
NCI Metathesaurus CUI : CL1778596;
Origin ID : C186379;
UMLS CUI : C5667061;
Semantic type(s)
- concept_is_in_subset
- has_target
