Kinase inhibitors: 20 years of success and many new challenges and recent trends in their patents

ABSTRACT

Introduction

Protein kinases (PKs) play key roles in cellular signaling and regulation cascades and therefore are listed among the most investigated enzymes with the intent to develop drugs that are able to modulate their catalytic features. Specifically, PKs are involved in chronic diseases of large impact in the society such as cancers and neurodegeneration. Since the approval of Fasudil for the management of cerebral vasospasm, frantic efforts are currently ongoing for the development of selective PK-modulating agents.

Areas covered

A selection of the most relevant patents in the European Patent Office for biomedical innovation and/or industrial development covering the years 2020–2023 on PK modulators either of the antibody and small-molecule type is reported. In addition to the examined patents, we also reported the contributions claiming the use of antibody-targeted PKs for lab bench identification kits.

Expert opinion

The field of PK modulators for biomedical purposes is particularly crowded with contributions, making it rich in valuable information for the development of potential drugs. An emerging frontier is represented by PK activators that aims to complement the use of PK inhibitors with the final intent of finely adjusting any PK-related disruption responsible for triggering any disease.

KEYWORDS:

• Protein kinases (PKs)
• protein kinase inhibitors (PKIs)
• small-molecule protein kinases inhibitors (SMPKIs)
• PK-targeted antibodies
• anticancer drugs

Article highlights

• PKs are among the most exploited enzymes in the biomedical field.

• To date, 101 drugs are PK-directed, of which 74 are SMPKIs and the remaining are mAbs.

• PKA is an emerging frontier to complement PKIs.

• Specific PK modulators and their applications (i.e. anticancer, glaucoma, and macular degeneration) will be detailed.

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.

Author contribution statement

All authors discussed and contributed to the final manuscript. M. A. M. Aboul-Soud and F. C. did wrote the manuscript.

Additional information

Funding

This paper was not funded.