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Review
. 2021 Sep 24;26(19):5795.
doi: 10.3390/molecules26195795.

Discovery, Development, and Patent Trends on Molnupiravir: A Prospective Oral Treatment for COVID-19

Mohd Imran  1 , Mandeep Kumar Arora  2 , Syed Mohammed Basheeruddin Asdaq  3 , Shah Alam Khan  4 , Saleh I Alaqel  1 , Mohammed Kanan Alshammari  5 , Mohammed M Alshehri  6 , Ahmed Subeh Alshrari  7 , Alreshidi Mateq Ali  8 , Ahmed Muteb Al-Shammeri  9 , Bushra Dhuhayyan Alhazmi  10 , Aishah Ali Harshan  11 , Md Tauquir Alam  1 , Abida  1
Affiliations
Review

Discovery, Development, and Patent Trends on Molnupiravir: A Prospective Oral Treatment for COVID-19

Mohd Imran et al. Molecules. .

Abstract

The COVID-19 pandemic needs no introduction at present. Only a few treatments are available for this disease, including remdesivir and favipiravir. Accordingly, the pharmaceutical industry is striving to develop new treatments for COVID-19. Molnupiravir, an orally active RdRp inhibitor, is in a phase 3 clinical trial against COVID-19. The objective of this review article is to enlighten the researchers working on COVID-19 about the discovery, recent developments, and patents related to molnupiravir. Molnupiravir was originally developed for the treatment of influenza at Emory University, USA. However, this drug has also demonstrated activity against a variety of viruses, including SARS-CoV-2. Now it is being jointly developed by Emory University, Ridgeback Biotherapeutics, and Merck to treat COVID-19. The published clinical data indicate a good safety profile, tolerability, and oral bioavailability of molnupiravir in humans. The patient-compliant oral dosage form of molnupiravir may hit the market in the first or second quarter of 2022. The patent data of molnupiravir revealed its granted compound patent and process-related patent applications. We also anticipate patent filing related to oral dosage forms, inhalers, and a combination of molnupiravir with marketed drugs like remdesivir, favipiravir, and baricitinib. The current pandemic demands a patient compliant, safe, tolerable, and orally effective COVID-19 treatment. The authors believe that molnupiravir meets these requirements and is a breakthrough COVID-19 treatment.

Keywords: COVID-19; EIDD-1931; EIDD-2801; MK-4482; SARS-CoV-2; molnupiravir; patents.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Scheme 1
Scheme 1
Mechanism of action of RdRp inhibitors.
Figure 1
Figure 1
(A) Molnupiravir; (B) EIDD-1931; (C) EIDD-1931-triphopsphate.
Scheme 2
Scheme 2
Summary of the development of molnupiravir.
Scheme 3
Scheme 3
Methodology of patent searching.
Scheme 4
Scheme 4
The summary of the process of preparing molnupiravir provided in US2020276219A1.
Scheme 5
Scheme 5
Summary of the process of preparing molnupiravir provided in CN112552288A.
Scheme 6
Scheme 6
The summary of the process of preparing molnupiravir provided in CN112608357A.
Scheme 7
Scheme 7
The summary of the process of preparing molnupiravir provided in IN202141018775A.
Figure 2
Figure 2
Chemical structures of EIDD-02749, EIDD-02991, and EIDD-02947.
See this image and copyright information in PMC

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