Competitor Analysis: TGF-beta/Receptor Inhibitors

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-β) and TGF-β 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-β) is of particular importance. In mammals three TGF-β isoforms are described (TGF-β1, 2, and 3) which are the primary mediators of TGF-β 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-β 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-β inhibition as a potential therapeutic target, monoclonal antibodies against all three isoforms of TGF-β, as well as TGF-βR 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-β 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-β/R inhibitors for treatment of fibrosis and cancer, respectively. In addition, the report lists company-specific R&D pipelines of TGF-β and TGF-β 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.