Tosposertib

**Semantic type:** Pharmacologic Substance

**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.

**Synonyms:** - NCE 401 - NCE-401 - NCE401 - TGF-beta Inhibitor TU2218 - TGFb Inhibitor TU2218 - TGFbeta Antagonist TU2218 - TGFbeta Inhibitor TU2218 - TOSPOSERTIB - TU 2218 - TU-2218 - TU2218