Pharmacokinetics of ß-d-N4-Hydroxycytidine, the Parent Nucleoside of Prodrug Molnupiravir, in Nonplasma Compartments of Patients With Severe Acute Respiratory Syndrome Coronavirus 2 Infection

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Abstract

ß-d-N4-hydroxycytidine (NHC), the parent nucleoside of molnupiravir, a COVID-19 antiviral, was quantified at SARS-CoV-2 transmission sites in 12 patients enrolled in AGILE Candidate-Specific Trial-2. Saliva, nasal, and tear NHC concentrations were 3%, 21%, and 22% that of plasma. Saliva and nasal NHC were significantly correlated with plasma (P < .0001).

Clinical Trials Registration. NCT04746183.

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  1. SciScore for 10.1101/2021.12.06.21267342: (What is this?)

    Please note, not all rigor criteria are appropriate for all manuscripts.

    Table 1: Rigor

    EthicsIRB: The study was approved by the UK Medicines and Healthcare product Regulatory Agency (MHRA; EudraCT 2020– 001860-27) and West Midlands Edgbaston Research Ethics Committee (20/ WM/0136) and all individuals provided written informed consent.
    Consent: The study was approved by the UK Medicines and Healthcare product Regulatory Agency (MHRA; EudraCT 2020– 001860-27) and West Midlands Edgbaston Research Ethics Committee (20/ WM/0136) and all individuals provided written informed consent.
    Field Sample Permit: All pharmacokinetic specimens were transported and processed on wet ice and stored at -80°C within 60 minutes of collection.
    Sex as a biological variablenot detected.
    RandomizationIn brief, eligible individuals were randomly assigned to one of three sequential dosing cohorts - molnupiravir dosed orally at 300, 600 and 800 mg twice daily.
    Blindingnot detected.
    Power Analysisnot detected.

    Table 2: Resources

    Software and Algorithms
    SentencesResources
    Data were log transformed and analysed using IBM SPSS Statistics (v. 25.0
    SPSS
    suggested: (SPSS, RRID:SCR_002865)

    Results from OddPub: We did not detect open data. We also did not detect open code. Researchers are encouraged to share open data when possible (see Nature blog).


    Results from LimitationRecognizer: We detected the following sentences addressing limitations in the study:
    There are a number of limitations. We utilised a sampling schedule for a truncated pharmacokinetic profile (0-4 hours) to limit infection risk. Missing samples led to a number of exclusions from the analysis, particularly for evaluation of RNP:P, contributed to data variability and limited data interpretation. Finally, the active triphosphate metabolite, EIDD-2061 was not quantified. Despite the limitations these data add to our understanding of NHC pharmacokinetics, principally at sites of COVID-19 infection. To our knowledge this is the first report describing significant accumulation of NHC in nasal secretions and tears, and to a lesser extent saliva. These data support the evaluation of molnupiravir as prophylaxis for SARS-CoV-2 infection.

    Results from TrialIdentifier: We found the following clinical trial numbers in your paper:

    IdentifierStatusTitle
    NCT04746183RecruitingAGILE (Early Phase Platform Trial for COVID-19)
    NCT04939428RecruitingStudy of MK-4482 for Prevention of Coronavirus Disease 2019 …


    Results from Barzooka: We did not find any issues relating to the usage of bar graphs.


    Results from JetFighter: We did not find any issues relating to colormaps.


    Results from rtransparent:
    • Thank you for including a conflict of interest statement. Authors are encouraged to include this statement when submitting to a journal.
    • Thank you for including a funding statement. Authors are encouraged to include this statement when submitting to a journal.
    • Thank you for including a protocol registration statement.

    Results from scite Reference Check: We found no unreliable references.


    About SciScore

    SciScore is an automated tool that is designed to assist expert reviewers by finding and presenting formulaic information scattered throughout a paper in a standard, easy to digest format. SciScore checks for the presence and correctness of RRIDs (research resource identifiers), and for rigor criteria such as sex and investigator blinding. For details on the theoretical underpinning of rigor criteria and the tools shown here, including references cited, please follow this link.