Shanghai, February 20, 2024 - Shanghai Ark Biopharmaceutical Co., Ltd. (hereinafter referred to as "ArkBio") announced that the company, together with Tongji Medical College of Huazhong University of Science and Technology and Hubei CDC, has jointly published a paper titled "Novel small-molecule inhibitors of SARS-CoV-2 main protease with nanomolar antiviral potency" in the internationally renowned journal "Journal of Infection". This paper points out that in the field of COVID-19 therapeutics, targeting the main protease 3CLpro of SARS-CoV-2 is a promising new drug development direction. This article details six potential 3CLpro inhibitors with completely independent intellectual property rights of ArkBio and explores the interactions between them and 3CLpro from a structural biology perspective. The co-corresponding authors of this paper are Professor Li Yan from Tongji Medical College of Huazhong University of Science and Technology, Researcher Cai Kun from Hubei CDC, and Dr. Song Guowei from ArkBio.

Since the outbreak of the COVID-19 pandemic, the virus has spread globally, causing severe impacts. Although several vaccines have been approved and marketed, the constant mutation of the virus, limitations in vaccine efficacy, and potential antigenic and toxic changes continue to necessitate the development of innovative antiviral drugs. 3CLpro, a crucial cysteine protease in the SARS-CoV-2 virus, is an attractive target for antiviral drug development. Currently approved drugs like Paxlovid™ include Nirmatrelvir, an efficient 3CLpro covalent inhibitor. However, reports have shown that some patients experience symptom recurrence and viral rebound after discontinuing Paxlovid™. Therefore, optimizing Nirmatrelvir to enhance its therapeutic effect is crucial.

The paper introduced ArkBio's proprietary 3CLpro inhibitors, showing that these inhibitors exhibited stronger antiviral activity than Nirmatrelvir in inhibiting 3CLpro enzyme activity and in cell infection models for both HCoV-OC43 and SARS-CoV-2. The team also used microscale thermophoresis (MST) and NMR spectroscopy to analyze the compound-3CLpro NTD interaction and detailed the mechanisms of these interactions. This structure-driven drug development research, integrating biochemistry, biophysics, and structural biology, offers valuable insights into the inhibition mechanism of SARS-CoV-2 and opens the path for developing next-generation antiviral drugs.

About ArkBio·

ArkBio is a global biotech company focusing on discovery and development of innovative drugs for unmet medical needs, especially in the therapeutic areas of respiratory, infectious and pediatric diseases. Since its inception in 2014, the company has established core technology platforms and built an innovative and highly differentiated R&D pipeline through in-house R&D efforts and external collaborations. This strong R&D pipeline program includes innovative clinical and pre-clinical stage drug candidates with first- or best-in-class potential for global clinical development. As one of the core assets, ziresovir is the first direct-acting RSV antiviral drug that has been developed by ArkBio. 

ArkBio has established strategic partnerships with several global pharmaceutical companies and academic institutes, including Roche, Genentech, the Scripps Research Institute, the Institute of Microbiology of Chinese Academy of Sciences, domestic and international biotechnology companies, as well as venture investment institutions. 

For more information about the company, please visit our website: www.arkbiosciences.com

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