A FGFR1 inhibitor patent review: progress since 2010

ABSTRACT

Introduction: FGFR1 is a well known molecular target for anticancer therapy. Many studies have proved that the regulation of FGFR1 activity is a promising therapeutic approach to treat a series of cancers. Therefore, the development of potent inhibitors has consequently become a key focus in the present drug discovery, and it is encouraging that several highly selective FGFR1 inhibitors have been identified from various sources in recent years.

Areas covered: This article reviews patents and patent applications related to selective FGFR1 inhibitors published from 2010 to 2016. This summary highlights about 15 patents from different pharmaceutical companies and academic research groups. We used Baidu and NCBI search engines to find relevant patents as a search term.

Expert opinion: In the past few years, considerable progress has been made in the identification and development of selective FGFR1 inhibitors in use. At present, at least 10 inhibitors of FGFR1 are in clinical trials, and several agents have shown encouraging results under experimental conditions. Given the fact that FGFR1 plays a crucial role in the regulation of cancer and other diseases, we hope that it will gain further attraction from pharmaceutical companies and encourage development of more novel, safe and efficient FGFR1 inhibitors in the future.

KEYWORDS:

• FGFR1 inhibitors
• cancer
• angiogenesis
• tyrosine kinase
• clinical evaluation
• drug discovery

Article highlights

• In the past seven years, more than 50 inhibitors selective to FGFR1 have been patented and are reviewed in this article.

• Among the chemical agents reviewed, an Imidazole derivative - compound 46 has shown the most potent FGFR1 inhibition at subnanomolar range (IC₅₀).

• A recently patented FGFR1 inhibitor, E7090 has shown promising therapeutic potential for treating various types of cancer.

• The utilization of different strategies to develop FGFR1 inhibitors could overcome several problems such as drug resistance.

This box summarizes key points contained in the article.

Declaration of interest

The authors have 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.

Additional information

Funding

This work was supported by National Natural Science Foundation of China (31501142) and China Postdoctoral Science Foundation (2016M590616).