Friday, August 26, 2022 2:21:29 PM
• Targeting the virus main protease (Mpro): interrupting virus replication
• STI-1558 is designed with the following properties:
• STI-1558 is a prodrug, and its active form AC1115 binds to Cys-145 of catalytic domain of Mpro , which is highly conserved in all SARS-CoV-2 variants and achieves a broad-spectrum anti-SARS-CoV-2 activity, including against the original SARS-CoV-2 strain as well as the predominant variants of concern (VOCs), such as Delta and
Omicron.
• STI-1558 is also a Cathepsin L inhibitor, which may block effective viral entry into host cells without accelerating viral mutations.
• Oral bioavailability up to 85% with fast absorption and enhanced drug exposure in plasma allowing early treatment of COVID at home by oral administration.
• Avoids the use of a potent CYP3A4 inhibitor (e.g., ritonavir) as booster to increase the plasma exposure allowing for standalone treatment with low risk for drug interaction.
• A drug product with robust formulation, stability and large-scale drug substance manufacture with controlled cost allowing for global accessibility and application.
See: Jeong, G. U., et al. (2020). "Therapeutic Strategies Against COVID-19 and Structural Characterization of SARS-CoV-2: A Review." Frontiers in Microbiology 11(1723).
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