Drug intelligence / Profile preview

nirmatrelvir + ritonavir + dabigatran

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Nirmatrelvir + ritonavir + dabigatran is a combination of two antiviral agents and an oral anticoagulant. Nirmatrelvir is a peptidomimetic inhibitor of the SARS-CoV-2 main protease (Mpro, also known as 3CLpro or nsp5 protease), which blocks viral replication by preventing processing of viral polyproteins. Ritonavir, originally developed as an HIV protease inhibitor, acts here primarily as a pharmacokinetic enhancer by inhibiting CYP3A4 to boost plasma concentrations of nirmatrelvir. Dabigatran is a direct thrombin (Factor IIa) inhibitor that prevents thrombin-mediated activation in the coagulation cascade, thereby reducing blood clot formation. This combination may be encountered in patients with COVID-19 who are on chronic anticoagulation therapy and require antiviral treatment[6][5][8].

Brand names
Paxlovid (for nirmatrelvir + ritonavir)Pradaxa (for dabigatran)
Other names
nirmatrelvir + ritonavir + dabigatran
02

Targets

ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)F2 (Thrombin)Mpro (3C-like proteinase of SARS-CoV-2)

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