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. 2020 Sep 10;35(6):776–784. doi: 10.1007/s12250-020-00288-1

Table 1.

Comparation of lopinavir and ritonavir in vitro antiviral efficacy against SARS-CoV-2 or HIV and in vivo plasma exposures.

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).