Polymorphs, Particle Size, and a Pandemic: Development of a Scalable Crystallization Process for Molnupiravir, an Antiviral for the Treatment of COVID-19-Reference-Cited by-同舟云学术

Polymorphs, Particle Size, and a Pandemic: Development of a Scalable Crystallization Process for Molnupiravir, an Antiviral for the Treatment of COVID-19

Published:2023-10-20 Issue:11 Volume:27 Page:2100-2110
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Bade Rachel¹^ORCID,Bothe Jameson R.²^ORCID,Sirota Eric¹^ORCID,Brunskill Andrew P. J.²,Newman Justin A.²^ORCID,Zhang Yongqian²,Tan Melissa²,Zheng Michelle¹,Brito Gilmar¹,Poirier Marc¹,Fier Patrick S.¹^ORCID,Xu Yingju¹,Ward Michael D.³,Stone Kevin¹^ORCID,Lee Ivan H.¹,Gmitter Andrew J.⁴,Bernardoni Frank²,Zompa Michael A.²^ORCID,Luo Hanlin²,Patel Sanjaykumar²,Masiuk Tina²,Mora Jeff²,Ni Tong³,Okoh Grace A.⁵,Tarabokija James⁵,Liu Jiaying⁵^ORCID,Lowinger Michael B.²,Mahmood Tariq⁶

Affiliation:

1. Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States

2. Analytical Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States

3. Small Molecule Science and Technology, Merck & Co., Inc., Rahway, New Jersey 07065, United States

4. Small Molecule Science and Technology, Merck & Co., Inc., West Point, Pennsylvania 19486, United States

5. Pharmaceutical Sciences and Clinical Supply, Merck & Co., Inc., Rahway, New Jersey 07065, United States

6. Regulatory Affairs CMC, Merck & Co., Inc., Rahway, New Jersey 07065, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.3c00268

Reference34 articles.

1. An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice

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

3. A phase 2a clinical trial of molnupiravir in patients with COVID-19 shows accelerated SARS-CoV-2 RNA clearance and elimination of infectious virus

4. Molnupiravir for Oral Treatment of Covid-19 in Nonhospitalized Patients

5. Molnupiravir plus usual care versus usual care alone as early treatment for adults with COVID-19 at increased risk of adverse outcomes (PANORAMIC): an open-label, platform-adaptive randomised controlled trial