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-?) 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:
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.
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.
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.
1) CANCER INDICATIONS
Indirect TGF-? Inhibition
Selective TGF-?1 Inhibition
Selective TGF-?2 Inhibition
Dual and Pan-TGF-? Inhibition
Bispecific TGF-? Inhibition
Cell Therapeutics with TGF-? Inhibition
2) NON-CANCER INDICATIONS WITH TGF-? INHIBITION
3) CORPORATE RORGAMMA ANTAGONIST & AGONIST R&D PIPELINES
Indirect TGF-? Inhibition
Selective TGF-?1 Inhibition
Selective TGF-?2 Inhibition
Dual and Pan-TGF-? Inhibition
Bispecific TGF-? Inhibition
Cell Therapeutics with TGF-? Inhibition
2) NON-CANCER INDICATIONS WITH TGF-? INHIBITION
3) CORPORATE RORGAMMA ANTAGONIST & AGONIST R&D PIPELINES
