Phospholipase A₂ inhibitors for the treatment of inflammatory diseases: a patent review (2010 – present)

Abstract

Introduction: Phospholipases A₂ have been implicated in various pathological conditions, such as rheumatoid arthritis, cardiovascular diseases, neurological disorders and cancer. The scientific community focuses on the search of potent and selective PLA₂ inhibitors of each PLA₂ class in order to identify novel medicinal agents. At present, only one lipoprotein-associated PLA₂ (LpPLA₂) inhibitor has reached Phase III clinical trials for the treatment of atherosclerosis.

Areas covered: This review article focuses on the role of the most important PLA₂s in inflammatory diseases and other severe pathological conditions presented in patent literature from June 2009 to September 2012.

Expert opinion: Even though the role of each PLA₂ in different diseases or pathological conditions is not yet definitively identified, the progress in the quest for potent and selective PLA₂ inhibitors is exciting and the use of such inhibitors as medicinal agent looks now more promising than ever.

Keywords::

• arthritis
• atherosclerosis
• cancer
• inflammation
• inhibitors
• multiple sclerosis
• phospholipase A₂

Notes

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