P2X receptor antagonists and their potential as therapeutics: a patent review (2010-2021)

Dane, Chianna, Stokes, Leanne ORCID: https://orcid.org/0000-0003-4013-6781 and Jorgensen, William T. (2022) P2X receptor antagonists and their potential as therapeutics: a patent review (2010-2021). Expert Opinion on Therapeutic Patents, 32 (7). pp. 769-790. ISSN 1354-3776

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Introduction: Purinergic receptors play a critical role in neurotransmission, and modulation of complex physiological functions and thus have implications in numerous disease states. The past decade has seen substantial progress in the design of novel chemical compounds that act on the P2X class of receptors and warrants an updated review of this field. Areas covered: This review provides a summary of the patent literature describing the discovery and clinical uses of P2X receptor antagonists published between 2010 and September 2021. The reader will gain information on structural claims, representative structures, and biological data of recently reported P2X antagonists. Expert opinion: Despite continual advancement in both crystallography and chemical biology strengthening our understanding of purinergic signalling, there remains an absence of clinically approved chemotypes. A testament to both the therapeutic potential and academic perseverance in purinergic research is the multitude of research initiatives that maintain active P2X receptor programs that have spanned decades. Very recently, the FDA declined Merck Pharmaceuticals application for Gefapixant, a P2X3 selective inhibitor as a treatment for chronic cough, requesting additional data. This unfortunate setback will ultimately be insignificant considering the long history of P2X investigation and the preclinical and clinical development that will undoubtedly occur over the next decade.

Item Type: Article
Additional Information: Funding Information: WT Jorgensen is recipient of a National Health and Medical Research Council Peter Doherty Fellowship (APP1157404).
Uncontrolled Keywords: drug discovery,p2x antagonists,inhibitors,purinergic,therapeutic applications,pharmacology,drug discovery ,/dk/atira/pure/subjectarea/asjc/3000/3004
Faculty \ School: Faculty of Science > School of Pharmacy
UEA Research Groups: Faculty of Science > Research Groups > Molecular and Tissue Pharmacology
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 07 Nov 2022 14:30
Last Modified: 07 Nov 2022 14:30
URI: https://ueaeprints.uea.ac.uk/id/eprint/89689
DOI: 10.1080/13543776.2022.2069010

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