Development of a Robust Manufacturing Route for Molnupiravir, an Antiviral for the Treatment of COVID-19
Patrick S. Fier, Yingju Xu, Marc Poirier, Gilmar Brito, Xue Zheng, Rachel S. Bade, E. B. Sirota, Kevin Stone, Lushi Tan, Guy R. Humphrey, Darryl Chang, Jameson R. Bothe, Yongqian Zhang, Frank Bernardoni, S. M. M. de Castro, Michael A. Zompa, J Taylor, Kevin M. Sirk, Anthony Diaz-Santana, Ike Diribe, Khateeta M. Emerson, B. Krishnamurthi, Ralph Zhao, Michael Ward, Chengqian Xiao, Honggui Ouyand, Jianfeng Zhan, William Morris
Abstract
Herein is described the development of a large-scale manufacturing process for molnupiravir, an orally dosed antiviral that was recently demonstrated to be efficacious for the treatment of patients with COVID-19. The yield, robustness, and efficiency of each of the five steps were improved, ultimately culminating in a 1.6-fold improvement in overall yield and a dramatic increase in the overall throughput compared to the baseline process.