A patent review of myeloperoxidase inhibitors for treating chronic inflammatory syndromes (focus on cardiovascular diseases, 2013-2019)

ABSTRACT

Introduction

Myeloperoxidase (MPO) is an immune enzyme found in neutrophils and macrophages. It produces the highly oxidative compound HOCl from H₂O₂ and Cl⁻ ions inside the phagosome of the neutrophil. Leakage of the enzyme outside the cell causes oxidative damages for the biomolecules promoting many inflammatory diseases such as atherosclerosis. Thus, there is a real interest to develop potent inhibitors of MPO as non-steroidal anti-inflammatory agents. This review highlights the several published MPO inhibitors, their activity, and the challenges met during the development of these compounds.

Areas covered

This article covers the patent literature published on MPO inhibitors from 2013 to 2019, as well as the potential use of these compounds as therapeutics for inflammatory syndromes, especially that plays an important role in the initiation and progression of atherosclerosis.

Expert opinion

To date, many MPO inhibitors with different structures have been studied, many of which have prominent inhibitory activities. Furthermore, the specificity of these drugs offers hope for the targeted therapy of inflammatory syndromes. Although many data have proved that MPO can contribute to several chronic inflammatory syndromes, the usefulness of MPO inhibitors in preventing and treating inflammatory disorders is still under investigation.

KEYWORDS:

• Myeloperoxidase
• chronic inflammatory syndromes
• atherosclerosis
• oxidative damages

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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.

Article highlights

• MPO plays a significant role in atherosclerosis and other chronic inflammatory syndromes.

• The evidence which implicated MPO in atherosclerosis made the enzyme a promising target for treating and preventing CVD.

• Many new MPO inhibitors have been developed and approved, some of which have entered clinical trials.

• MPO inhibitors can have significant application prospects if their associated limitations are overcome.

This box summarizes key points contained in the article.

Additional information

Funding

This paper was funded by the Universite Libre de Bruxelles.