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PF-07304814 is a small molecule prodrug that targets the 3CL protease (M, which is used by viruses like SARS-CoV-2 to assemble and multiply. Once administered through intravenous infusion, the compound is cleaved into PF-00835231 to exert its anti-viral effects. PF-07304814, developed by Pfizer, was first identified during the SARS outbreak in 2002-2003; it was subsequently shelved as the outbreak was controlled. Now, it is being tested regarding the novel SARS-CoV-2 virus, including studies in conjunction with Remdesivir to treat COVID-19 infection; in vitro data showed synergistic effects on articles published on preprint servers. Phase 1b studies are also exploring the safety and tolerability of PF-07304814 in COVID-19 patients who are hospitalized (NCT04535167).
PF-07304814 is a small molecule prodrug that targets the 3CL protease (M, which is used by viruses like SARS-CoV-2 to assemble and multiply. Once administered through intravenous infusion, the compound is cleaved into PF-00835231 to exert its anti-viral effects. PF-07304814, developed by Pfizer, was first identified during the SARS outbreak in 2002-2003; it was subsequently shelved as the outbreak was controlled. Now, it is being tested regarding the novel SARS-CoV-2 virus, including studies in conjunction with Remdesivir to treat COVID-19 infection; in vitro data showed synergistic effects on articles published on preprint servers. Phase 1b studies are also exploring the safety and tolerability of PF-07304814 in COVID-19 patients who are hospitalized (NCT04535167).
The structure of PF-07304814 contains a phosphate group, allowing the compound to be soluble and then subsequently cleaved in tissue by alkaline phosphatase. This step allows for the release of PF-00835231, which is the compound that exerts anti-viral activity against the 3CL protease of SARS-CoV-2. The active compound, PF-00835231, was shown to have potent and broad-spectrum inhibitory activity against numerous coronavirus 3CL proteases.
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