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Competitor Analysis - Sphingosine-1-Phosphate (S1P)

La Merie Publishing, Nov 2010, Pages: 26


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The present Competitive Intelligence Report about Sphingosine-1-Phosphate (S1P) provides a competitor evaluation in the field of molecules interacting with the sphingosine-1-phosphate pathway as of November 2010. Among these molecules are S1P and selective S1P1 receptor agonists or S1P lyase inhibitors for treatment of inflammatory disease such as multiple sclerosis, psoriasis, asthma and rheumatoid arthritis. S1P inhibitors and S1P receptor antagonists and inhibitors of sphingosine kinase have promise for treatment of cancer. Purchase of the downloadable pdf report includes a 6-month online access to the data of the report and any updates since the publication date. Credentials to access the database will be sent by e-mail and allow online work with the project data to print or export an individual report.

Sphingosine-1-phospate (S1P) is a phospholipid released by platelets, mast and other cells. It is now known that S1P stimulates at least five different G-protein coupled receptors (GPCRs): S1P1, S1P2, S1P3, S1P4, and S1P5. Activation of these GPCRs mediates a complex variety of biological responses, such as lymphocyte migration, endothelial cell proliferation, blood vessel constriction, heart rate modulation and others. Selective S1P1 receptor agonists inhibit lymphocyte migration out of lymphoid tissue into the lymphatic and blood circulation, thereby reducing peripheral lymphocyte counts and preventing lymphocyte recruitment to sites of inflammation.

This lymphatic tissue specific mechanism of action offers potential advantages over existing therapies. Sequestration of T cells in lymphoid organs is expected to prevent the processes that contribute to inflammatory diseases – such as tissue invasion, local cytokine release, macrophage recruitment, and direct cell killing – while sparing functions that do not rely on homing mechanisms. These include antibody generation by B lymphocytes, first line immunological protection by neutrophils and monocytes, and antigen-dependent T cell activation and expansion. While a first generation, not specific S1P receptor agonist has advanced in development for multiple sclerosis until phase III, the next generation S1P1 specific receptor agonists have the promise of reduced side effects, e.g. bradycardia via S1P3. Inhibition of S1P lyase in mice caused the concentration of S1P to rise in lymphoid tissues, thereby causing lymphocytes to be retained in the lymphoid tissues. Thus, S1P agonism holds promise for treatment of inflammatory and autoimmune diseases such as multiple sclerosis, psoriasis, asthma, rheumatoid arthritis and transplantation.

In contrast, reducing levels of S1P may have anti-tumor effects because S1P promotes tumor growth by stimulating cell proliferation, metastasis, and cell survival. Corresponding therapeutic approaches are neutralization of S1P levels or inhibition of sphingosine-1-kinase.

The report includes a compilation of currently active projects in research and development of the sphingosine-1-phosphate (S1P) targeting antibodies and small molecules. In addition, the report lists company-specific S1P R&D pipelines. 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.


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