Learning from the In Vitro Biological Activity Data of Current Antiviral
Medicines for the Successful Development of New Antiviral Drug
Candidates

Murilo   Barboza   Fontoura; Fernando      Fumagalli

doi:10.2174/1570180819666220928151734

Abstract

Background: Although evaluating in vitro biological activity is an important part of the drug discovery process, few publications discuss the ideal inhibitory activity in these tests.

Objective: To analyze the in vitro biological activity data from antiviral drugs to establish parameters that could increase success in developing new antiviral drug candidates.

Methods: Information from in vitro tests for each antiviral medicine was obtained from the Thomson Reuters Integrity platform for antiviral drugs approved by FDA between 1963 and 2020 (35 years). The inhibitory activity data was collected from three references using the same determination method, and the values were reported as means.

Results: 82 antiviral drugs were found to treat 11 different viruses. Most of these drugs were developed to treat HIV infections (33 of 82), followed by anti-HCV medicines (20 of 82). The anti-HIV phenotypic activities of most HIV-approved drugs had an IC₅₀ < 50 nM; for the anti-HCV it was verified as IC₅₀ < 0.2 μM. Combining the data for all drugs analyzed, the antiviral phenotypic activity in most cases exhibited an IC₅₀ < 0.2 μM.

Conclusion: The limited availability of antiviral drugs and in vitro activity data imposed limitations on this study. However, it could be inferred that an antiviral drug candidate would have more success in drug development when the IC₅₀ was in the range of low micromolar. Ultimately, in vitro activity must be considered in combination with other factors in drug development processes.

Keywords: drug development, drug discovery, in vitro, pandemic, virus, new chemical entities

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DOI https://dx.doi.org/10.2174/1570180819666220928151734	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X

Letters in Drug Design & Discovery

Learning from the In Vitro Biological Activity Data of Current Antiviral Medicines for the Successful Development of New Antiviral Drug Candidates

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Letters in Drug Design & Discovery

Learning from the In Vitro Biological Activity Data of Current Antiviral Medicines for the Successful Development of New Antiviral Drug Candidates

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