Drug intelligence / Profile preview

lufotrelvir

Development stage
Phase 3
Lead developer
Pfizer
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Lufotrelvir (PF-07304814) is an investigational antiviral drug developed by Pfizer. It is a phosphate prodrug that, after intravenous administration, is cleaved in vivo to yield the active compound PF-00835231. The active moiety selectively inhibits the 3CL protease (also known as Mpro or main protease), a critical enzyme required for coronavirus replication. By inhibiting this protease, lufotrelvir blocks the proteolytic cleavage of viral polyproteins necessary for producing functional viral proteins and enzymes, thereby preventing viral transcription and replication. Lufotrelvir has demonstrated potent and broad-spectrum inhibitory activity against multiple coronavirus 3CL proteases—including those from SARS-CoV-2—and has been evaluated in clinical trials for the treatment of COVID-19 in hospitalized patients. Unlike some related drugs such as nirmatrelvir, lufotrelvir is not orally bioavailable and must be administered intravenously[1][2][3][4][6].

Other names
PF-07304814PF07304814PF 07304814lufotrelvir
02

Targets

Mpro (3C-like proteinase of SARS-CoV-2)

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