Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs

Abstract

Introduction: The identification of PGD₂ as the cognate ligand for the DP2 (formerly CRTH2) receptor and the apparent role of that receptor in allergic disease has led to considerable interest in the development of DP2 receptor antagonists for the treatment of asthma. Around 20 DP2 receptor antagonists have progressed into development.

Areas covered: The DP2 antagonists in clinical development and those whose development has been discontinued are discussed in detail. This article highlights the former and examines the available clinical data in respect of both groups of antagonists. It draws upon data that are available from clinical trial registries as well as data that have been presented.

Expert Opinion: The unpromising clinical outcomes obtained with setipiprant, vidupiprant and AZD-1981, and the reason why development of OC-459 appears stalled, are all considered. An assessment of the nine DP2 antagonists currently in clinical development highlights the apparent advantages of ADC-3680 and MK-1029. The scope for licensing opportunities in this field is also highlighted.

Keywords::

• ADC-3680
• ARRY-502
• Asthma
• BI-671800
• DP1 receptor
• DP2 receptor
• eosinophil
• inflammation
• MK-1029
• OC-459
• PGD₂
• setipiprant
• vidupiprant

Declaration of interest

The authors state no conflict of interest and have received no payment in preparation of this manuscript.

Notes

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