Evaluation of molnupiravir (EIDD-2801) efficacy against SARS-CoV-2 in the rhesus macaque model

Johnson, Dylan M.; Brasel, Trevor; Massey, Shane; Garrón, Tania; Grimes, Michael D.; Smith, Jeanon; Torres, Maricela; Wallace, Shannon M.; Villasante‐Tezanos, Alejandro; Comer, Jason E.

doi:10.1016/j.antiviral.2022.105492

Cited by 13 publications

(13 citation statements)

References 53 publications

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“…Molnupiravir is a prodrug. 28 Through an ester cleavage, it is converted into the active form N 4 -hydroxy-cytidine. 29 This compound had already been identified as a substrate for hmARC in our laboratory previously.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

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New Design of an Activity Assay Suitable for High-Throughput Screening of Substrates and Inhibitors of the Mitochondrial Amidoxime Reducing Component (mARC)

Klopp,

Struwe,

Plieth

et al. 2023

Anal. Chem.

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The mitochondrial amidoxime-reducing component (mARC) is one of the simplest molybdenum-containing enzymes. mARC is among a few known reducing enzymes playing an important role in drug metabolism in mammals. Here, an assay based on the fluorescence of NADH is reported for the rapid detection of substrates and potential inhibitors of mARC. So far unknown inhibitors might be useful for the development of drugs assigned to nonalcoholic fatty liver disease (NAFLD) and similar diseases. Kinetics of reactions catalyzed by mARC can be recorded with high sensitivity and precision. On a microtiter plate scale, the assay presented could be applied for highthroughput screening of substance libraries and detection of novel mARC substrate candidates. For instance, molnupiravir was also identified as a new substrate by this assay. For better comparison for such substances, the inhibitor or substrate-to-BAO ratio was introduced. After normalization of enzyme activities to the standard benzamidoxime, substrates can reproducibly be classified.

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Section: ■ Results and Discussionmentioning

confidence: 99%

“…As an example, we tested the potential SARS-CoV2-virustaticum molnupiravir (Lagevrio). Molnupiravir is a prodrug . Through an ester cleavage, it is converted into the active form N 4 -hydroxy-cytidine .…”

Section: Resultsmentioning

confidence: 99%

New Design of an Activity Assay Suitable for High-Throughput Screening of Substrates and Inhibitors of the Mitochondrial Amidoxime Reducing Component (mARC)

Klopp,

Struwe,

Plieth

et al. 2023

Anal. Chem.

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show abstract

“…MOV is rapidly and extensively converted by host esterases to NHC, then to an active ribonucleotide analog, NHC-triphosphate, within cells. This pathway is more active in rodents, so the doses used are proportionally higher than in ferrets [ 17 ], rhesus macaques [ 46 ] and humans [ 47 ]. We determined trough plasma and lung concentrations to ensure that animals were properly exposed to MOV.…”

Section: Discussionmentioning

confidence: 99%

Further preclinical characterization of molnupiravir against SARS-CoV-2: Antiviral activity determinants and viral genome alteration patterns

Petit,

Touret,

Driouich

et al. 2024

Heliyon

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“…Remdesivir, as a prodrug, could selectively inhibit RNA-dependent RNA polymerase (RdRp), then delay viral RNA chain termination, and finally inhibit viral replication 8 . Molnupiravir and its metabolites can also inhibit SARS-CoV-2 transmission by targeting RdRp 9 .…”

Section: Introductionmentioning

confidence: 99%

Potential herb–drug interactions between anti-COVID-19 drugs and traditional Chinese medicine

Ye¹,

Fan²,

Zhao³

et al. 2023

Acta Pharmaceutica Sinica B

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Evaluation of molnupiravir (EIDD-2801) efficacy against SARS-CoV-2 in the rhesus macaque model

Cited by 13 publications

References 53 publications

New Design of an Activity Assay Suitable for High-Throughput Screening of Substrates and Inhibitors of the Mitochondrial Amidoxime Reducing Component (mARC)

New Design of an Activity Assay Suitable for High-Throughput Screening of Substrates and Inhibitors of the Mitochondrial Amidoxime Reducing Component (mARC)

Further preclinical characterization of molnupiravir against SARS-CoV-2: Antiviral activity determinants and viral genome alteration patterns

Potential herb–drug interactions between anti-COVID-19 drugs and traditional Chinese medicine

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