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Chlorpheniramine Maleate Displays Multiple Modes of Antiviral Action Against SARS-CoV-2: A Mechanistic Study

Elshaier et al., bioRxiv, doi:10.1101/2023.08.28.554806
Aug 2023  
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10th treatment shown to reduce risk in December 2020, now with p = 0.00006 from 15 studies.
Lower risk for mortality, recovery, and cases.
No treatment is 100% effective. Protocols combine treatments.
5,100+ studies for 109 treatments. c19early.org
In Vitro study showing that chlorpheniramine maleate (CPM) inhibits SARS-CoV-2 infection by affecting viral adsorption, replication, and having a direct virucidal effect in Vero E6 cells. Molecular docking analysis revealed that CPM interacts with essential SARS-CoV-2 proteins, including the main protease receptor, spike protein receptor, and RNA polymerase, primarily through hydrophobic interactions and an additional hydrogen bond in the RNA polymerase active site. Authors suggest CPM has potential as a multitarget antiviral agent against SARS-CoV-2 and potentially other respiratory viruses.
12 preclinical studies support the efficacy of antihistamine H1RAs for COVID-19:
Elshaier et al., 29 Aug 2023, USA, preprint, 6 authors. Contact: rahaghf@ccf.org.
In Vitro studies are an important part of preclinical research, however results may be very different in vivo.
This PaperH1RAsAll
Chlorpheniramine Maleate Displays Multiple Modes of Antiviral Action Against SARS-CoV-2: A Mechanistic Study
Yaseen A M M Elshaier, Ahmed Mostafa, Fernando Valerio-Pascua, Mari L Tesch, Joshua M Costin, M.D, M.H.S Franck F Rahaghi
Chlorpheniramine Maleate (CPM) has been identified as a potential antiviral compound against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). In this study, we investigated the in vitro effects of CPM on key stages of the SARS-CoV-2 replication cycle, including viral adsorption, replication inhibition, and virucidal activity. Our findings demonstrate that CPM exhibits antiviral properties by interfering with viral adsorption, replication, and directly inactivating the virus. Molecular docking analysis revealed interactions between CPM and essential viral proteins, such as the main protease receptor, spike protein receptor, and RNA polymerase. CPM's interactions were primarily hydrophobic in nature, with an additional hydrogen bond formation in the RNA polymerase active site. These results suggest that CPM has the potential to serve as a multitarget antiviral agent against SARS-CoV-2 and potentially other respiratory viruses. Further investigations are warranted to explore its clinical implications and assess its efficacy in vivo.
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