Journal
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Volume 538, Issue -, Pages 173-179Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2020.11.095
Keywords
Angiotensin converting Enzyme-2; Sigma-1 receptor; SARS-CoV-2; Repurposing; Docking
Categories
Funding
- University of Florida Clinical and Translational Science Institute
- NIH National Center for Advancing Translational Sciences [UL1TR001427]
- National Center for Advancing Translational Sciences [UL1TR001872]
- National Institutes of Health [R00HL119560, OT2OD026582, OT2OD023854]
- Center for Data Driven Insight and Innovation in the University of California Health
- UCSF Florida Clinical and Translational Science Institute
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The urgency to identify therapies that prevent SARS-CoV-2 infection and enhance COVID-19 outcomes is emphasized. The study identified potential repurposed antihistamine drugs with in vitro antiviral activity against SARS-CoV-2 through mining electronic health records. Clinical studies are recommended to evaluate the effectiveness of these antihistamines for disease prevention and treatment.
There is an urgent need to identify therapies that prevent SARS-CoV-2 infection and improve the outcome of COVID-19 patients. Although repurposed drugs with favorable safety profiles could have significant benefit, widely available prevention or treatment options for COVID-19 have yet to be identified. Efforts to identify approved drugs with in vitro activity against SARS-CoV-2 resulted in identification of antiviral sigma-1 receptor ligands, including antihistamines in the histamine-1 receptor binding class. We identified antihistamine candidates for repurposing by mining electronic health records of usage in population of more than 219,000 subjects tested for SARS-CoV-2. Usage of diphenhydramine, hydroxyzine and azelastine was associated with reduced incidence of SARS-CoV-2 positivity in subjects greater than age 61. We found diphenhydramine, hydroxyzine and azelastine to exhibit direct antiviral activity against SARS-CoV-2 in vitro. Although mechanisms by which specific antihistamines exert antiviral effects is not clear, hydroxyzine, and possibly azelastine, bind Angiotensin Converting Enzyme-2 (ACE2) and the sigma-1 receptor as off-targets. Clinical studies are needed to measure the effectiveness of diphenhydramine, hydroxyzine and azelastine for disease prevention, for early intervention, or as adjuvant therapy for severe COVID-19. (c) 2020 Elsevier Inc. All rights reserved.
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