Novel prostaglandin receptor modulators – Part II: EP receptor modulators; a patent review (2002 – 2012)

Abstract

Introduction: Prostaglandins and their G-protein–coupled receptors play numerous physiological and pathophysiological roles, especially in inflammation and its resolution. The variety of effects mediated by prostanoids makes prostanoid receptors valuable drug targets and the research on prostaglandin receptor modulators is intensive. The physiological and pathophysiological effects of prostaglandin E₂ are especially complex and numerous. The four subtypes of EP receptor have gained a lot of industrial and academic interest, in particular EP₂ and EP₄ for various indications.

Areas covered: Evaluation of the patent activity over the last decade (2002 – 2012) illustrates several potent compounds targeting the distinct prostaglandin E₂ receptors. Many novel methods for the use of EP receptor modulators have been developed, in addition to the classical indications for agents modulating the arachidonic acid cascade such as pain and inflammation.

Expert opinion: Several EP targeting agents with good potency and selectivity have been developed but their pharmacological use and utility has not yet been satisfactorily investigated. More research is necessary, and clinical use of these agents might therefore take some more time.

Keywords::

• arachidonic acid
• asthma
• cancer
• inflammatory disorders
• pain

Acknowledgments

The work has been supported by the Else Kröner-Fresenius Foundation (EKFS), Research Training Group Translational Research Innovation – Pharma (TRIP).

Notes

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