Aurora kinase inhibitors: a patent review (2014-2020)

ABSTRACT

Introduction: Aurora kinases are a family of serine/threonine kinases, and promote mitotic spindle assembly by regulating centrosome duplication and separation. Aurora kinases are overexpressed in a variety of tumor cell lines, thus, the use of Aurora kinase small-molecule inhibitors has become a potential treatment option for cancer.

Areas covered: As a continuing review of Aurora kinase inhibitors and their patents published in 2009, 2011 and 2014. Herein, we updated the information for Aurora kinase inhibitors in clinical trials and the patents filed from 2014 to 2020. PubMed, Scopus, SciFinder, and www.clinicaltrials.gov databases were used for searching the clinical information and patents of Aurora kinase inhibitors.

Expert opinion: Even though Aurora A or B selective as well as pan inhibitors show preclinical and clinical efficacy, so far, no Aurora kinase inhibitor has been approved for clinical use. Preliminary evidence suggested that highly selective Aurora kinase or multi-target inhibitors as a single agent as well as in combination therapy are still the current main development trend of Aurora kinase inhibitors.

KEYWORDS:

• anticancer
• aurora kinase
• clinical trials
• combination therapy
• inhibitor
• patent

Article highlights

• MLN8237 was still the most advanced one among the Aurora kinase inhibitors in clinic with 32 clinical trials, in addition, ABT-348, CS2164, LY3295668/AK-01 and TT00420 first entered clinical trials since 2014.

• 43 patents about new structure were applied during 2014 to present worldwide and pyrimidine was the most effective core.

• High selective Aurora kinase or multi-target inhibitors as a single agent as well as combination therapy are the current main development trend of Aurora kinase inhibitors.

This box summarizes the 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.

Reviewer disclosures

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

Additional information

Funding

This paper was funded by The National Natural Science Foundation of China (No. 21672093).