Targeting the TGF-β signaling pathway for fibrosis therapy: a patent review (2015–2020)

Fibrosis is a serious disease that occurs in many organs, such as kidney, liver and lung. The deterioration of these organs ultimately leads to death. Due to the complex mechanisms of fibrosis, research and development of antifibrotic drugs is difficult. One solution is to focus on core pathways, one of which is the TGF-β signaling pathway. In virtually every type of fibrosis, TGF-β signaling is recognized as a critical pathway.This review discusses patents on active molecules related to the TGF-β signaling. Molecules targeting components related to the activation of TGF-β are introduced. Several strategies preventing signal propagation from active TGF-β to downstream targets are also introduced, including TGF-β antibodies, TGF-β ligand traps, and inhibitors of TGF-β receptor kinases. Finally, molecules affecting downstream targets in both canonical and noncanonical TGF-β signaling pathways are described.Since the approval of pirfenidone, targeting TGF-β signaling has been anticipated as an effective therapy for fibrosis. The potential of this therapy has been further supported by emerging patents on the TGF-β signaling. This pathway can be entirely inhibited, from the activation of TGF-β to downstream signaling. Inhibiting TGF-β signaling is expected to provide more effective treatments for fibrosis.