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

Xuanyi Li1, Ziang Ding1, Zixuan Wu1

  • 1Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, China.

Abstract

Insights

Fibrosis affects multiple organs and is difficult to treat. Targeting the transforming growth factor-beta (TGF-β) signaling pathway, a critical factor in fibrosis, offers promising new antifibrotic drug development strategies.

Area of Science:

  • Fibrosis research
  • Drug development
  • Molecular signaling pathways

Background:

  • Fibrosis is a severe condition affecting vital organs like the kidney, liver, and lung, often leading to organ failure and death.
  • The complex mechanisms of fibrosis present significant challenges for antifibrotic drug development.
  • The transforming growth factor-beta (TGF-β) signaling pathway is a critical and universally recognized pathway in virtually all types of fibrosis.

Purpose of the Study:

  • To review patents on active molecules targeting the TGF-β signaling pathway for potential antifibrotic therapies.
  • To explore strategies for inhibiting TGF-β signaling at various stages, from activation to downstream effects.

Main Methods:

  • Discussion of patents related to molecules that target TGF-β pathway activation.
  • Overview of strategies to prevent signal propagation, including TGF-β antibodies, ligand traps, and receptor kinase inhibitors.
  • Description of molecules affecting downstream targets in both canonical and noncanonical TGF-β signaling.

Main Results:

  • Patents indicate a growing interest in targeting TGF-β signaling for fibrosis treatment.
  • Multiple molecular strategies exist to inhibit TGF-β signaling comprehensively.
  • Emerging patents support the potential of TGF-β pathway inhibition as an effective therapeutic approach.

Conclusions:

  • Targeting the TGF-β signaling pathway is a highly anticipated strategy for effective fibrosis treatment.
  • The pathway can be inhibited comprehensively, from TGF-β activation to downstream signaling.
  • Inhibiting TGF-β signaling holds promise for developing more effective antifibrotic therapies.

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