A patent review of RAF kinase inhibitors (2010–2018)

ABSTRACT

Introduction: RAF kinase inhibitors block and regulate RAS/RAF/MEK/ERK signaling, which is a key to tumor treatment. At present, although RAF kinase inhibitors have good efficacy, there are few such drugs with low toxicity, and thus, it is urgent to find novel RAF kinase inhibitors associated with higher activity and fewer adverse reactions. This review highlights the anti-tumor effects of several published RAF kinase inhibitors and might be helpful in providing new ideas for the development of novel drug candidates in the future.

Areas covered: This article covers the pertinent literature published on RAF kinase inhibitors from 2010 to 2018, as well as the potential use of these compounds as therapeutics for cancer.

Expert opinion: To date, many RAF kinase inhibitors with different structures have been studied, many of which have prominent inhibitory activities toward RAF kinase. Further, the specificity of these drugs offers hope for the targeted therapy of tumors. Although RAF kinase inhibition has achieved promising results for the treatment of many cancers, overcoming limitations associated with drug resistance and safety comprises a new direction for the optimization and improvement of RAF kinase inhibitors.

KEYWORDS:

• RAF kinase inhibitors
• chemical structure
• anti-tumor
• classification

Article highlights

• RAF kinase mediated RAS/RAF/MEK/ERK signaling plays a significant role in tumor development and metastasis, and is closely related to many growth factors.

• Currently, RAF kinase inhibitors play an important role in the design of anti-tumor strategies.

• Many new RAF kinase inhibitors have been developed and approved, some of which have entered clinical trials.

• Upon overcoming associated limitations, RAF kinase inhibitors will have significant application prospects.

This box summarizes key points contained in the article.

Declaration of interest

The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This work was supported by Guangxi University for Nationalities Research Funded Project (no. 2018KJQD13), Guangxi Minority Preparatory Education Base Research Project (no. 2017B002) and Guangxi Biological Polysaccharide Separation, Purification and Modification Research Platform (GKZY18076005).