First in Class Science: Oral COVID-19 Protease Inhibitor
• HighSARS-CoV2 mutational rate, continued global impact & vaccine hesitancy creates likely sustained need for therapeutic
• Addressable market maybe up to 100s of millions of patients which include high risk, low risk and close contact
• Development plan for Pfizer’s protease inhibitor is designed to evaluate potential impact on these populations
•3CL protease is virally encoded protein that is essential to the viral lifecycle across a broad spectrum of coronaviruses with no close human analogue
• Goal to reduce SARS-CoV-2 viral load and decrease or prevent symptoms of COVID-19
• Oral Inhibitor exhibits potent in vitro antiviral activity against SARS-CoV-2(single and combo use)
‒ Anti-viral activity seen across multiple coronaviruses and potentially all known COVID-19 variants
• Oral inhibitor shows robust preclinical antiviral effect and good preclinical safety profile
• Enabled by >100x selectivity for coronavirus 3CL proteases vs human proteases
• Good tolerability, no safety findings up to dose of 500 mg twice a day with ritonavir / 10days in healthy volunteers
• Phase 1 pharmacokinetics studies indicate exposure >5xEC90 for antiviral effects
• Phase 2/3 study started Jul.2021; Potential US EUA submission Q4 2021
COVID-19: Coronavirus Disease 2019; SARS-CoV-2: Severe acute respiratory syndrome coronavirus 2; 3CL: 3C-like; EC90: 90% effective concentration