Vactosertib
Oral, potent and selective TGFBRI (ALK5) inhibitor.
Target and Technology
TGF-β1 inhibits cell proliferation and induces apoptosis in normal cells but in the tumor microenvironment, TGF-βsuppresses immunity, promotesmetastasis and induces anti-cancer drug resistance. TGF-βalso promotes fibroblast proliferation around cancerous tissue to produce large quantities of substrate that builds up a 'wall' around the tumor to prevent immune cells from penetrating the tumor.
Vactosertib(TEW-7197), a TGF-β1 kinase inhibitor, promotes the cancer cell killing activity of immune cells, and inhibits proliferation of cancer stem cells, angiogenesis and metastasis. In addition, vactosertib can support various cancer treatments to attack cancer cells by suppressing stroma formation.
Currently, combination trials with various anti-cancer treatments such as immunotherapy, targeted therapy and chemotheraphy are underway.
TGF-β1 is secreted by cancer cells in large quantities
TGF-β1 inhibits immunity, promotes cancer cell metastasis and plays a major role in the development of anticancer drug resistance.
Main Functions of Vactosertib
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01
Promotes tumor cell killing activity by immune cells
- Activates cytotoxic function of T- and NK cells
- Inhibits activity of regulatory T-cells
- Prevents T-cell exhaustion
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02
Inhibits Metastasis
- Inhibits epithelial-mesenchymal transition (EMT), cell migration and metastasis
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03
Inhibits cancer stem cell production
- Suppresses TGF-β1-induced generation of cancer stem cells (cause of drug resistance to various anti-cancer drugs such as Gleevec, a treatment for CML, and paclitaxel)
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04
Inhibits angiogenesis
