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Competitor Analysis: TGF-beta/Receptor Inhibitors

September 2019 | 59 pages | ID: CD26ACA80C25EN
La Merie Publishing

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Competitor Analysis: TGF-beta/Receptor Inhibitors

This Competitive Intelligence report about TGF-beta/Receptor Inhibitors evaluates the landscape of investigational new molecular entities targeting transforming growth factor beta (TGF-?) and TGF-? receptor kinase for 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-?) is of particular importance. In mammals three TGF-? isoforms are described (TGF-?1, 2, and 3) which are the primary mediators of TGF-? 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-? 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-? inhibition as a potential therapeutic target, monoclonal antibodies against all three isoforms of TGF-?, as well as TGF-?R 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-? 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-?/R inhibitors for treatment of fibrosis and cancer, respectively. In addition, the report lists company-specific R&D pipelines of TGF-? and TGF-? 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.
About Competitor Analysis Series:

The Competitor Analysis Series delivers NO-FRILLS, but concise information about the pipeline of R&D projects for targets, diseases, technologies and companies. The information is provided in a tabular format and fully referenced.

Indirect TGF-? Inhibition
Selective TGF-?1 Inhibition
Selective TGF-?2 Inhibition
Dual and Pan-TGF-? Inhibition
Bispecific TGF-? Inhibition
Cell Therapeutics with TGF-? Inhibition



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