Nirmatrelvir is an oral protease inhibitor with emergency use authorization for the treatment of mild-to-moderate COVID-19. Nirmatrelvir (PF-07321332) is an orally bioavailable 3C-like protease (3CLPRO) inhibitor that is the subject of clinical trial NCT04756531.
- Mechanism
- Curator reviewed · 8 references
Nirmatrelvir is an inhibitor of a cysteine residue in the 3C-like protease (3CLPRO) of SARS-CoV-2. This cysteine is responsible to the activity of the 3CLPRO of SARS-CoV-2 and potentially other members of the coronavirus family. The 3CLPRO, also known as the main protease or non structural protein 5, is responsible for cleaving polyproteins 1a and 1ab. These polyproteins contain the 3CLPRO itself, a papain-like (PL) cysteine protease, and 14 other nonstructural proteins. Without the activity of the 3CLPRO, nonstructural proteins (including proteases) cannot be released to perform their functions, inhibiting viral replication.
- Primary indication
- In the US, Europe, and Canada, nirmatrelvir, in combination with ritonavir, is indicated for the treatment of mild-to-moderate coronavirus disease 2019 (COVID-19) in adults who are at high risk for progression to severe COVID-19, including...Curator reviewed · 1 structured indication
- Formula / weight
- C23H32F3N5O4 · 499.535 g/mol (avg)
- First approval
- Canada, 2022 · United States, 2023 · European Union, 2022
- Code names
- PF-07321332
- Brand names
Resolves to
LIENCHBZNNMNKG-OJFNHCPVSA-NSMILES[H][C@]12CN([C@H](C(=O)N[C@@H](C[C@]3([H])CCNC3=O)C#N)[C@@]1([H])C2(C)C)C(=O)[C@@H](NC(=O)C(F)(F)F)C(C)(C)CWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Nirmatrelvir, and which of those have an active Phase 3 trial?
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