Small molecule
PubChem CID 155903259
Nirmatrelvir
Paxlovid
- Mechanism of action
- SARS-CoV-2 main protease (3CLpro) inhibitor
- In plain language
- Blocks a key enzyme the COVID-19 virus needs to cut its own proteins into working pieces, stopping the virus from multiplying in the body.
- How it works
- Nirmatrelvir is a peptidomimetic inhibitor of the SARS-CoV-2 main protease (Mpro, also called 3CL protease), an enzyme essential for viral replication. By binding the enzyme's active site, it prevents proteolytic processing of the viral polyproteins into the individual nonstructural proteins the virus needs, halting viral replication. Because nirmatrelvir is a CYP3A4 substrate with a short half-life, it is co-packaged with ritonavir, a pharmacokinetic booster that inhibits CYP3A-mediated metabolism and raises nirmatrelvir plasma concentrations to therapeutic levels; ritonavir itself has no direct antiviral activity against SARS-CoV-2.
- Therapeutic applications
- Paxlovid (nirmatrelvir/ritonavir) is FDA-approved for treatment of mild-to-moderate COVID-19 in adults at high risk of progression to severe disease. Treatment should be started as soon as possible after diagnosis and within 5 days of symptom onset. Not approved for pre-exposure or post-exposure prophylaxis, nor for initiating treatment in patients requiring hospitalization due to severe or critical COVID-19.
- Class
- Small molecule
- Therapeutic area
- Antiviral
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