DC402234 (FB2001), an anti-SARS-CoV-2 drug candidate mainly developed by research team at the Shanghai Institute of Materia Medica (SIMM) of Chinese Academy of Sciences enters its Phase I clinical trial in the United States on March 15.
DC402234, a peptidomimetic compound, was designed and synthesized through analyzing the crystal structure of the coronaviruses Mpro.
Researchers found that DC402234 exhibits effective inhibitory activity against SARS-CoV-2 Mpro with IC50 values of 0.053 ± 0.005 μM, and vibrant anti-SARS-CoV-2-infection activity in cell culture (EC50 values of 0.42 ± 0.08 μM).
Furthermore, DC402234 shows good pharmacokinetic properties and safety in vivo.
Prof. Gregory Tarcey, main investigator of DC402234 from the US Frontage Phase I Research Center, will carry out the Phase I clinical trial in the United States.
The study was led by Professors LIU Hong, XU Yechun and JIANG Hualiang’s teams from SIMM, together with Professors YANG Haitao, RAO Zihe’s team from Shanghai Institute for Advanced Immunochemical Studies of ShanghaiTech University, and Professors ZHANG Lei-Ke, XIAO Gengfu’s team from Wuhan Institute of Virology of CAS.
The effective anti-SARS-CoV-2 in vitro activity of DC402234 will bring more research prospects. However, there is still a long way to go for DC402234 as a new drug, from entering the human clinical trial stage to final application and marketing in the future.
Reference: Dai W, Zhang B, Jiang X-M, et al. Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease. Science. 2020;368(6497):1331-1335. doi: 10.1126/science.abb4489
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