title: A FGFR1 inhibitor patent review: progress since 2010.
abstract: 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.
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Tao
authors.initials: T
authors.lastname: Yu
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Yang
authors.affiliation: b Food and Drug Administration of Linyi City , Hedong District Branch , Linyi , People's Republic of China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Yinfeng
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: c Department of Orthodontics , Affiliated Hospital of Qingdao University , People's Republic of China.
authors.forename: Hong
authors.initials: H
authors.lastname: Xu
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Mengpeng
authors.initials: M
authors.lastname: Li
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Murugavel
authors.initials: M
authors.lastname: Ponnusamy
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Kun
authors.initials: K
authors.lastname: Wang
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Jian-Xun
authors.initials: JX
authors.lastname: Wang
authors.affiliation: a Institute for Translational Medicine , Qingdao University , Qingdao , People's Republic of China.
authors.forename: Pei-Feng
authors.initials: PF
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D051496:Receptor, Fibroblast Growth Factor, Type 1 / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; C496348:FGFR1 protein, human; D051496:Receptor, Fibroblast Growth Factor, Type 1
keywords: FGFR1 inhibitors; angiogenesis; cancer; clinical evaluation; drug discovery; tyrosine kinase