Recent progress in small molecule TBK1 inhibitors: a patent review (2015– 2020)

ABSTRACT

Introduction: TANK-binding kinase 1 (TBK1) is a key mediator of innate immunity processes and studies have reported on its role in inflammatory and autoimmune diseases. Moreover, several studies have also described the important role of TBK1 in cancer and metabolic disorders. Therefore, there is increasing interest in this noncanonical IKK serine/threonine kinase family member as a drug target in both the scientific community and the pharmaceutical industry as indicated by the growing number of patents reporting on these efforts.

Areas covered: This review covers the patent literature from 2015 to 2020 issued by the World, US and European patent offices on novel TBK1 small molecule inhibitors as well as patents claiming new applications of TBK1 inhibitors.

Expert opinion: The high complexity TBK1 biology greatly increases the challenge of pursuing it as a drug target. The recent discovery of several small molecule inhibitors, particularly those with high selectivity, will enable further exploration of TBK1s biological role and its validation as a drug target.

KEYWORDS:

• Cancer therapy
• inflammatory and autoimmune diseases
• metabolic disorders
• TBK1 inhibitors

Article highlights

• Modulation of TBK1 activity has been investigated for several disease indications including inflammatory, neuroinflammatory, autoimmune, neurodegenerative, metabolic disorders, and oncology.

• The key role of TBK1 in several biological processes has led to numerous research efforts from both academic groups and pharmaceutical industry.

• The patent literature on novel TBK1 inhibitors and their applications, from 2015 to present, is reviewed in this article.

This box summarizes key points contained in the article.

Declaration of interest

The authors are employees and shareholders of Cellzome GmbH, a GlaxoSmithKline company. The authors have no other 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 not funded.