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Molecular Modeling and Preliminary Clinical Data Suggesting Antiviral Activity for Chlorpheniramine (Chlorphenamine) Against COVID-19

Black, S., Cureus, doi:10.7759/cureus.20980
Jan 2022  
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10th treatment shown to reduce risk in December 2020, now with p = 0.000063 from 16 studies.
Lower risk for mortality, recovery, cases, and viral clearance.
No treatment is 100% effective. Protocols combine treatments.
5,100+ studies for 112 treatments. c19early.org
In Silico study suggesting that the over-the-counter antihistamine chlorpheniramine may have antiviral activity against SARS-CoV-2. Using structural database searches and molecular modeling, authors found that chlorpheniramine shares similar structural features with chloroquine and hydroxychloroquine, including a chlorophenyl group, pyridine ring, alkyl sidechain, and terminal tertiary amine. Energy-minimized three-dimensional structures showed significant similarity between the drugs. In a preliminary retrospective study of 13 participants who took chlorpheniramine preventively or post-exposure, none were hospitalized or died from COVID-19. Authors propose that chlorpheniramine may prevent SARS-CoV-2 entry into cells in a similar manner as chloroquine and hydroxychloroquine.
12 preclinical studies support the efficacy of antihistamine H1RAs for COVID-19:
Black et al., 6 Jan 2022, peer-reviewed, 1 author. Contact: sblack@uttyler.edu.
In Silico studies are an important part of preclinical research, however results may be very different in vivo.
This PaperH1RAsAll
Molecular Modeling and Preliminary Clinical Data Suggesting Antiviral Activity for Chlorpheniramine (Chlorphenamine) Against COVID-19
Shaun D Black
Cureus, doi:10.7759/cureus.20980
Chlorpheniramine maleate, a widely used over-the-counter antihistamine, has been identified as a structural analog of aminoquinolines known to possess antiviral activity against the Betacoronavirus severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) that causes coronavirus disease 2019 (COVID-19). Structural similarities include the chlorophenyl group, pyridine ring, alkyl sidechain, and terminal tertiary amine; the comparison of aqueous energy-minimized structures indicates significant three-dimensional similarity as well. Preliminary clinical evidence supports these conclusions. The present study suggests that chlorpheniramine possesses antiviral activity against COVID-19.
Additional Information Disclosures Human subjects: Consent was obtained or waived by all participants in this study. Animal subjects: All authors have confirmed that this study did not involve animal subjects or tissue. Conflicts of interest: In compliance with the ICMJE uniform disclosure form, all authors declare the following: Payment/services info: All authors have declared that no financial support was received from any organization for the submitted work. Financial relationships: All authors have declared that they have no financial relationships at present or within the previous three years with any organizations that might have an interest in the submitted work. Other relationships: All authors have declared that there are no other relationships or activities that could appear to have influenced the submitted work.
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' 'Cureus. 2020, 12:e10501. 10.7759/cureus.10501', 'journal-title': 'Cureus'}], 'container-title': ['Cureus'], 'original-title': [], 'language': 'en', 'link': [ { 'URL': 'https://www.cureus.com/articles/81059-molecular-modeling-and-preliminary-clinical-data-suggesting-antiviral-activity-for-chlorpheniramine-chlorphenamine-against-covid-19', 'content-type': 'unspecified', 'content-version': 'vor', 'intended-application': 'similarity-checking'}], 'deposited': { 'date-parts': [[2022, 1, 6]], 'date-time': '2022-01-06T08:58:35Z', 'timestamp': 1641459515000}, 'score': 1, 'subtitle': [], 'short-title': [], 'issued': {'date-parts': [[2022, 1, 6]]}, 'references-count': 47, 'URL': 'http://dx.doi.org/10.7759/cureus.20980', 'relation': {}, 'ISSN': ['2168-8184'], 'issn-type': [{'value': '2168-8184', 'type': 'print'}], 'subject': ['Aerospace Engineering'], 'published': {'date-parts': [[2022, 1, 6]]}}
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