Engineered Ribosyl-1-Kinase Enables Concise Synthesis of Molnupiravir, an Antiviral for COVID-19

Article Chemistry, Organic

A Concise Route to MK-4482 (EIDD-2801) from Cytidine: Part 2

Vijayagopal Gopalsamuthiram et al.

Summary: A new synthesis route for MK-4482 has been developed, utilizing cytidine instead of uridine to improve yield and accessibility. It is expected to expand access to MK-4482 as a viable drug substance.

SYNLETT (2021)

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Article Microbiology

Therapeutically administered ribonucleoside analogue MK-4482/EIDD-2801 blocks SARS-CoV-2 transmission in ferrets

Robert M. Cox et al.

Summary: Treating SARS-CoV-2-infected ferrets with nucleoside analogue MK-4482/EIDD-2801 reduced viral load and suppressed virus spread. This therapeutic approach shows promise in breaking transmission chains of the COVID-19 pandemic.

NATURE MICROBIOLOGY (2021)

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Article Multidisciplinary Sciences

SARS-CoV-2 infection is effectively treated and prevented by EIDD-2801

Angela Wahl et al.

Summary: The study suggests that bats may be the source of coronaviruses that can be directly transmitted to humans. Using the LoM model, efficient replication of SARS-CoV, MERS-CoV, SARS-CoV-2, and two SARS-like bat coronaviruses in human lung tissue was demonstrated. Infection with SARS-CoV-2 predominantly targets human lung epithelial cells and induces a sustained inflammatory response. The broad-spectrum antiviral agent EIDD-2801 significantly inhibits SARS-CoV-2 replication in vivo, showing potential for prevention and treatment of COVID-19.

NATURE (2021)

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Article Chemistry, Multidisciplinary

Progress Toward a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from Cytidine

Grace P. Ahlqvist et al.

Summary: A supply-centered and chromatography-free synthesis of molnupiravir from cytidine has been successfully described, with an improved overall isolated yield compared to the patented route; this new route has the potential to reduce the production cost of the drug.

ACS OMEGA (2021)

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Review Microbiology

SARS-CoV-2 variants, spike mutations and immune escape

William T. Harvey et al.

Summary: The evolution of SARS-CoV-2 has been characterized by the emergence of mutations and variants that impact virus characteristics. Manufacturers are preparing for possible updates to vaccines in response to changes in the virus population, and it is crucial to monitor genetic and antigenic changes alongside experiments to understand the impacts of mutations.

NATURE REVIEWS MICROBIOLOGY (2021)

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Article Cell Biology