Results 21 to 30 of about 809 (101)

Quantitative efficacy paradigms of the influenza clinical drug candidate EIDD-2801 in the ferret model. [PDF]

Transl Res, 2020
Seasonal influenza viruses cause major morbidity and mortality worldwide, threatening in particular older adults and the immunocompromised. Two classes of influenza therapeutics dominate current disease management, but both are compromised by pre-existing or rapidly emerging viral resistance.
Toots M, Yoon JJ, Hart M, Natchus MG, Painter GR, Plemper RK.   +5 more
europepmc   +4 more sources

Progress Towards a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from Cytidine [PDF]

ACS Omega, 2021
Molnupiravir (MK-4482, EIDD-2801) is a promising orally bioavailable drug candidate for treatment of COVID-19. Herein we describe a supply-centered and chromatography-free synthesis of molnupiravir from cytidine, consisting of two steps: a selective enzymatic acylation followed by transamination to yield the final drug product.
Ahlqvist GP, McGeough CP, Senanayake C, Armstrong JD, Yadaw A, Roy S, Ahmad S, Snead DR, Jamison T.   +8 more
europepmc   +7 more sources

A Concise Route to MK-4482 (EIDD-2801) [PDF]

Nucleosides, Nucleotides & Nucleic Acids, 2020
A two-step route to MK-4482 (EIDD-2801, 1 ) was developed consisting of an esterification and hydroxamination of cytidine. The reactions can be conducted in either order with overall yields of 67% (first step—esterification) and 37% (first step—hydroxamination). Selective esterification of the
Natarajan Vasudevan, Grace P. Ahlqvist, Catherine P. McGeough, Dinesh J. Paymode, Flavio S. P. Cardoso, Tobias Lucas, Jule-Phillip Dietz, Till Opatz, Timothy F. Jamison, B. Frank Gupton, David Snead   +10 more
openaire   +3 more sources

Therapeutic MK-4482/EIDD-2801 Blocks SARS-CoV-2 Transmission in Ferrets [PDF]

, 2020
Abstract The COVID-19 pandemic is having a catastrophic impact on human health. Widespread community transmission has triggered stringent distancing measures with severe socioeconomic consequences. Gaining control of the pandemic will depend on interruption of transmission chains until protective herd immunity arises.
Plemper R, Cox R, Wolf J.
europepmc   +3 more sources

Accelerated First-in-Human Clinical Trial of EIDD-2801/MK-4482 (molnupiravir), a Ribonucleoside Analogue with Potent Antiviral Activity Against SARS-CoV-2 [PDF]

Trials, 2021
Abstract A recently published article described the safety, tolerability and pharmacokinetic profile of molnupiravir, a novel antiviral agent with potent activity against SARS-CoV-2, the causative agent of COVID-19. Here, we report an unprecedented collaboration between sponsor, contract research organization (CRO) and regulatory authorities ...
Cohen O, Holman W, Holman W, Painter W, McIntosh S, Painter G, Bush J.   +6 more
europepmc   +4 more sources

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

Synlett, 2020
A new route to MK-4482 ( 1 ) was developed. The route replaces uridine with the more available and less expensive cytidine. Low cost, simple reagents are used for the chemical transformations and the yield is improved from 17% to 44%.
Snead, David R., Gopalsamuthiram, Vijayagopal, Williams, Corshai, Noble, Jeffrey, Jamison, Timothy F., Gupton, B. Frank   +5 more
openaire   +3 more sources

Unlicensed Molnupiravir is an Effective Rescue Treatment Following Failure of Unlicensed GS-441524-like Therapy for Cats with Suspected Feline Infectious Peritonitis

Pathogens, 2022
Feline infectious peritonitis (FIP) is a complex and historically fatal disease, though recent advances in antiviral therapy have uncovered potential treatments.
Meagan Roy, Nicole Jacque, Wendy Novicoff, Emma Li, Rosa Negash, Samantha J. M. Evans   +5 more
doaj   +1 more source

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

Molecules, 2021
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,
Mohd. Imran, Mandeep Kumar Arora, Syed Mohammed Basheeruddin Asdaq, Shah Alam Khan, Saleh I. Alaqel, Mohammed Kanan Alshammari, Mohammed M. Alshehri, Ahmed Subeh Alshrari, Alreshidi Mateq Ali, Ahmed Muteb Al-shammeri, Bushra Dhuhayyan Alhazmi, Aishah Ali Harshan, Md. Tauquir Alam, Abida   +13 more
doaj   +1 more source

Molnupiravir—A Novel Oral Anti-SARS-CoV-2 Agent

Antibiotics, 2021
Since December 2019, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has rapidly resulted in a global pandemic with approximately 4 million deaths.
Ching-Chi Lee, Chih-Chia Hsieh, Wen-Chien Ko   +2 more
doaj   +1 more source

Acute SARS-CoV-2 Infection is Highly Cytopathic, Elicits a Robust Innate Immune Response and is Efficiently Prevented by EIDD-2801 [PDF]

, 2020
Abstract All known recently emerged human coronaviruses likely originated in bats. Here, we used a single experimental platform based on human lung-only mice (LoM) to demonstrate efficient in vivo replication of all recently emerged human coronaviruses (SARS-CoV, MERS-CoV, SARS-CoV-2) and two highly relevant endogenous pre-pandemic SARS-like ...
Wahl A, Gralinski L, Johnson C, Yao W, Kovarova M, Dinnon K, Liu H, Madden V, Krzystek H, De C, White K, Schäfer A, Zaman T, Leist S, Grant P, Gully K, Askin F, Browne E, Jones C, Pickles R, Baric R, Garcia JV.   +21 more
europepmc   +3 more sources