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Competitor Analysis: FGF-R Agonists and Antagonists
La Merie, Nov 2009, Pages: 37


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The present Competitive Intelligence Report about FGF-R agonists and antagonists provides a competitor evaluation in the field of fibroblast growth factor receptor (FGF-R) or PDGF targeting molecules for wound healing, cardiac tissue repair, bone formation or treatment of cancer as of November 2009. 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.

The family of fibroblast growth factors (FGFs) regulates a plethora of developmental processes, including brain patterning, branching morphogenesis and limb development. The fibroblast growth factor receptors consist of an extracellular ligand domain composed of three immunoglobulin-like domains, a single transmembrane helix domain, and an intracellular domain with tyrosine kinase activity. These receptors bind fibroblast growth factors, members of the largest family of growth factor ligands, comprising 22 members.

FGF/FGFR signalling is important in tumour angiogenesis but studies in the last few years have uncovered increasing evidence that FGFRs are driving oncogenes in certain cancers and act in a cell autonomous fashion to maintain the malignant properties of tumour cells. These observations make FGFRs increasingly attractive as targets for therapeutic intervention in cancer. There is a range of therapeutic strategies currently employed or in development to antagonise de-regulated FGFRs including antibodies and small molecule tyrosine kinase inhibitors.

Quite a number of FGF-R agonists are in development or even marketed in a range of different indications of tissue repair:

Cardiovascular Diseases:

Fibroblast growth factor-2 (FGF-2 has been shown over the years to exert acute and direct pro-survival effects, irrespectively of whether it is administered before, during or after an ischemic insult to the heart. FGF-2 is also a potent angiogenic protein and a crucial agent for the proliferation, expansion, and survival of several cell types including those with stem cell properties. Human clinical trials have pointed to a good safety record for this protein.

Wound Healing:

Wound healing is an evolutionarily conserved, complex, multicellular process that, in skin, aims at barrier restoration. This complex process is executed and regulated by an equally complex signaling network involving numerous growth factors, cytokines and chemokines. Of particular importance is the epidermal growth factor (EGF) family, transforming growth factor beta (TGF-beta) family, fibroblast growth factor (FGF) family, vascular endothelial growth factor (VEGF), granulocyte macrophage colony stimulating factor (GM-CSF), platelet-derived growth factor (PDGF), connective tissue growth factor (CTGF), interleukin (IL) family, and tumor necrosis factor-alpha family. Currently, patients are treated by three growth factors: PDGF-BB, bFGF, and GM-CSF.

Dental and Bone Tissue Repair:

The role of growth factors (GF) in bone repair is widely recognised, particularly for bone morphogenetic proteins (BMPs), fibroblast growth factor (FGF), insulin-like growth factors (IGFs), platelet-derived growth factor (PDGF), transforming growth factor-beta (TGF-beta) and vascular endothelial growth factor (VEGF). GF are usually stored in the extracellular matrix (ECM), but after injury are actively released by ECM, cells and platelets.

The report includes a compilation of current active projects in research and development of molecules targeting FGF or the FGF receptor. In addition, the report lists company-specific R&D pipelines of FGF /-R targeting small molecules, antibodies, proteins, peptides, medical devices and DNA. 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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