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Drug Virus In vitro efficiacy (µmol/L) In vivo concentration (µmol/L) IC50 (µmol/L) Cmax Unbound Cmax Cmin Unbound Cmin Lopinavir SARS-CoV-2 7.79–12.01 13.5b 0.2c 5.3d 0.08d HIV 0.004–0.011a Ritonavir SARS-CoV-2 11.68–19.88 0.15e 0.002 0.038e 0.0006 HIV 0.022–0.16e Unbound Cmax and unbound Cmin represent the free plasma concentration after protein-binding correction. Protein bindings of lopinavir and ritonavir are 98%–99%. 98.5% were used here to calculate the unbound values.
In vitro anti-HIV activity values used here obtained from the in vitro activity study absence of human albumin.
aData obtained from Abbott Laboratories and European Medicines Agency.
bData obtained from http://www.fda.gov/cder/foi/nda/2000/21-226_Kaletra_biopharmr_P1.pdf.
cData obtained from referenceGulati et al. (2009) .
dData obtained from referenceMurphy et al. (2001) .
eData obtained from reference Cvetkovic and Goa (2003).Table 1. Comparation of lopinavir and ritonavir in vitro antiviral efficacy against SARS-CoV-2 or HIV and in vivo plasma exposures.
Figure 5 个
Table 1 个