.Pharmacolibrary.Drugs.ATC.J.J05AE30

Information

Nirmatrelvir and ritonavir is a combination antiviral therapy used primarily in the treatment of COVID-19. Nirmatrelvir is a SARS-CoV-2 3CL protease inhibitor, while ritonavir acts as a pharmacokinetic enhancer by inhibiting CYP3A-mediated metabolism, thereby increasing plasma concentrations of nirmatrelvir. This combination (marketed as Paxlovid) is approved for emergency use and treatment of COVID-19 in many countries.

Pharmacokinetics

Representative pharmacokinetic parameters for nirmatrelvir/ritonavir in healthy adult subjects after oral administration.

References

1. Hammond, J, et al., & Rusnak, JM (2022). Oral Nirmatrelvir for High-Risk, Nonhospitalized Adults with Covid-19. The New England journal of medicine 386(15) 1397–1408. DOI:10.1056/NEJMoa2118542 PUBMED:https://pubmed.ncbi.nlm.nih.gov/35172054

2. Gerhart, J, et al., & Damle, B (2024). A Comprehensive Review of the Clinical Pharmacokinetics, Pharmacodynamics, and Drug Interactions of Nirmatrelvir/Ritonavir. Clinical pharmacokinetics 63(1) 27–42. DOI:10.1007/s40262-023-01339-y PUBMED:https://pubmed.ncbi.nlm.nih.gov/38177893

3. Pagliano, P, et al., & Ascione, T (2023). Preclinical discovery and development of nirmatrelvir/ritonavir combinational therapy for the treatment of COVID-19 and the lessons learned from SARS-COV-2 variants. Expert opinion on drug discovery 18(12) 1301–1311. DOI:10.1080/17460441.2023.2248879 PUBMED:https://pubmed.ncbi.nlm.nih.gov/37614103

Revisions

• 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)