Varenicline Prevents SARS-CoV-2 Infection In Vitro And In Vivo (Medicine)

The SARS-CoV-2 is a novel strain of coronavirus that was first identified as an infectious agent in humans in 2019. It has resulted in a global pandemic, but an antiviral therapy for this novel strain does not currently exist. Now, Dr. Jeffrey Nau and colleagues investigated the antiviral potential of the Varenicline against SARS-CoV-2. They found that, it not only prevents SARS-CoV-2 infection In Vitro but also in Rhesus Macaques (In Vivo).

“To our knowledge these are the first in vitro and in vivo studies to show that Varenicline has antiviral activity against SARS-CoV-2.”

— Dr. Jeffrey Nau, President and CEO, Oyster Point Pharma, inc.

Varenicline is a prescription medication (FDA approved) used to treat tobacco use disorder. It both reduces craving for and decreases the pleasurable effects of nicotine from cigarettes and other tobacco products. It is a high-affinity partial agonist for the α4β2 nicotinic acetylcholine receptor subtype (nACh) that leads to the release of the neurotransmitter dopamine in the nucleus accumbens reward center of the brain when activated, and therefore, has the capacity to reduce the feelings of craving and withdrawal caused by smoking cessation.

Now, Dr. Jeffrey Nau and colleagues assessed the antiviral activity of varenicline tartrate against SARS-CoV-2 in Calu-3 and Caco-2 cells. It has been found that the, Varenicline tartrate reduced SARS-CoV-2 viral titers over a range of concentrations, with an IC50 of 0.3 μM and 0.5 μM in Calu-3 and Caco-2 cells, respectively. In addition, varenicline tartrate reduced SARS-CoV-2 alpha variant viral titers with an IC50 of 0.13µM in Calu-3 cells, and SARS-CoV-2-beta variant viral titers with an IC50 of 4µM in Calu-3 cells. Importantly, these in vitro conditions were not toxic and cell viability was maintained.

“Varenicline tartrate, over a wide range of concentrations, reduced the infectivity of SARS-CoV-2 wildtype, alpha and beta variants in Calu-3 cells and Caco-2 cells, with maintainance of cell viability.”

Moreover, they assessed the antiviral activity of varenicline against SARS-CoV-2 in rhesus macaques and found that, varenicline tartrate, administered as a nasal spray to rhesus macaques, reduced SARS-CoV-2 wildtype viral load and inhibited viral replication in the nasal mucosa and upper airway.

“Our study confirmed that the nAChR agonist, “Varenicline”, has the potential to interact with and inhibit SARS-CoV-2 infection and replication.”

— concluded authors of the study

Reference: Jeffrey Nau, Priya Luthra, Kathleen Lanzer, Frank Szaba, Tres Cookenham, Eric Carlson, “Varenicline Prevents SARS-CoV-2 Infection In Vitro and in Rhesus Macaques”, bioRxiv 2021.06.29.450426; doi:

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