Competitor Analysis: Ras-Raf-MEK-ERK Inhibitors

The present Competitive Intelligence report about Ras-Raf-MEK-ERK Inhibitors provides a competitor evaluation in the field of synthetic and biologic molecules targeting the Ras-Raf-MEK-ERK pathway for treatment of cancer as of June 2011.

Inhibitors of Raf and MEK (MAPK/ERK kinase) have gained great interest because they suppress growth of tumors with mutant B-Raf and some with mutant Ras which depend upon ERK signaling for proliferation. The selectivity of mutant B-Raf inhibitors lead to a broader therapeutic index and may explain the greater antitumor activity observed with mutant B-Raf inhibitors than with MEK inhibitors. In fact, the submission of a NDA for vemurafenib (RG7204, PLX4032) to the U.S. FDA for people with BRAF V600 mutation-positive metastatic melanoma, and simultaneously of a MAA to the EMA for vemurafenib in the same indication reflects the tremendous progress made in this area of cancer drug discovery and development. Roche also submitted an application for the cobas 4800 BRAF V600 Mutation Test, a companion diagnostic, highlighting another example of personalized cancer therapy.

Competitors for Roche and Daiichi Sankyo (acquired Plexxikon) are quite behind and mostly in phase I trials except one phase III program or even earlier, indicating that the field still offers opportunities for successful drug discovery and development. Creating dual B-Raf and MEK inhibitors in one molecules or combining B-Raf inhibitors with inhibitors of other members of the same Ras-Raf-MEK-ERK pathway or of other pathywas such as the PI3K-Akt-mTOR pathways. Combining a mutant B-Raf inhibitor with a targeted T-cell antibody, such as ipilimumab, may increase the so far low response rate of ipilimumab in melanoma, bring its life-prolonging effect in responders to more patients.

The report includes a compilation of current active projects in research and development of synthetic and biologic molecules targeting the Ras-Raf-MEK-ERK pathway. In addition, the report lists company-specific R&D pipelines of Ras-Raf-MEK-ERK targeting molecules. 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.