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Competitor Analysis: TGF-beta/Receptor Inhibitors

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  • 59 Pages
  • September 2019
  • Region: Global
  • La Merie Publishing
  • ID: 4848789
This Competitive Intelligence report about TGF-beta/Receptor Inhibitors evaluates the landscape of investigational new molecular entities targeting transforming growth factor-beta (TGF-ß) and TGF-ß receptor kinase for the treatment of cancer or fibrosis as of September 2019.

Several cytokines and growth factors are involved in the tight regulation of either antitumor immunity or immunosuppressive tumor-promoting inflammation within the tumor microenvironment (TME), of which transforming growth factor-beta (TGF-ß) is of particular importance. In mammals, three TGF-ß isoforms are described (TGF-ß1, 2, and 3) which are the primary mediators of TGF-ß cell transduction. All isoforms are synthesised as propeptides that form dimers which require maturation before being able to bind to their receptors. These dimers are composed of the C-terminal TGF-ß ligand as well as an N-terminal latency-associated propeptide (LAP), with which the complex gets sequester to proteins of the extracellular matrix (ECM).

As preclinical studies implicate the use of TGF-ß inhibition as a potential therapeutic target, monoclonal antibodies against all three isoforms of TGF-ß, as well as TGF-ßR inhibitors, are currently tested in various solid cancers. As the response to anti-PD-1 monotherapy appears to be mainly limited by the number of preexisting cytotoxic T cells, concurrent TGF-ß inhibition provides a powerful strategy to (a) improve T cell priming within the lymph nodes, (b) enhance cytotoxic destruction of tumor cells, and (c) reduce the appearance of immune-suppressive immune cells.

The report includes a compilation of currently active projects in research and development of TGF-ß/R inhibitors for the treatment of fibrosis and cancer, respectively. In addition, the report lists company-specific R&D pipelines of TGF-ß and TGF-ß receptor kinase inhibitors. Competitor projects are listed in a tabular format providing information on:

  • Drug Codes
  • Target/Mechanism of Action
  • Class of Compound
  • Company
  • Product Category
  • Indication
  • R&D Stage and
  • additional comments with a hyperlink leading to the source of information.

Table of Contents

1) Cancer Indications

  • Indirect TGF-β Inhibition
  • Selective TGF-β1 Inhibition
  • Selective TGF-β2 Inhibition
  • Dual and Pan-TGF-β Inhibition
  • Bispecific TGF-β Inhibition
  • Cell Therapeutics with TGF-β Inhibition

2) Non-Cancer Indications with TGF-β Inhibition

3) Corporate RORgamma Antagonist & Agonist R&D Pipelines