Definition

An orally bioavailable inhibitor of transforming growth factor-beta (TGFb), with potential antineoplastic and anti-fibrotic activities. Upon oral administration, TGFb inhibitor TU2218 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.