Table 1.
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 reference Gulati et al. (2009).
dData obtained from reference Murphy et al. (2001).
eData obtained from reference Cvetkovic and Goa (2003).