Lopinavir is an antiretroviral and selective HIV-1 protease inhibitor, used as a treatment for HIV-1 in combination with other antiretrovirals due to its poor bioavailability. An analogue of Ritonavir, it is a peptidomometic molecule that mimics the peptide linkage typically targeted by HIV-1 protease enzymes. Lopinavir is found to inhibit MERS-CoV replication in the low-micromolar range in cell cultures. Lopinavir with Ritonavir is currently being investigated as a potential drug target for the treatment of COVID-19.
References
[1] Sham, H.L., et al.: Antimicrob. Ag. Chemother., 42, 3218 (1998).
[2] Kumar, G.N., et al.: Drug Metab. Dispos., 27, 86 (1999).
[3]Murphy, R.L., et al.: Antiviral Ther., 4, Suppl. 3, 85 (1999).
[4]Cao B, Wang Y, Wen D, et al. A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19. N Engl J Med. 2020;382(19):1787-1799. doi:10.1056/NEJMoa2001282.
[5]Chan JF, Yao Y, Yeung ML, et al. Treatment With Lopinavir/Ritonavir or Interferon-β1b Improves Outcome of MERS-CoV Infection in a Nonhuman Primate Model of Common Marmoset. J Infect Dis. 2015;212(12):1904-1913. doi:10.1093/infdis/jiv392.
[6]Corrao S, Natoli G, Cacopardo B. A Trial of Lopinavir-Ritonavir in Covid-19. N Engl J Med. 2020;382(21):e68. doi:10.1056/NEJMc2008043.