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. 2015 Dec 31;60(1):316–322. doi: 10.1128/AAC.01834-15

TABLE 1.

Effect of HIV and HCV PIs, cobicistat, and inhibitors of host serine proteases on CatA-mediated activation of TAF in vitroa

Inhibitor class Compound IC50 (μM)b Cmax (μM)c
HIV PI Darunavir >50 8.9
Atazanavir >50 6.3
Lopinavir >50 15.2
Ritonavir >50 1.3
HCV PI Telaprevir 0.27 ± 0.17 5.2
Boceprevir 0.16 ± 0.02 3.3
Simeprevir >50 13.3
Faldaprevir 25 ± 7 20.0
MK-5172 >50 2.5
GS-9256 >50 10.6
GS-9451 >50 1.7
CYP3A Cobicistat >50 2.2
Factor Xa Apixaban >50 0.2
>50 0.3
Thrombin Argatroban >50 0.4
Dabigatran >50 0.4
DPP4 Sitagliptin >50 1.0
a

TAF (30 μM) was incubated with purified CatA in the presence of various protease inhibitors, and the rate of TFV-Ala conjugate formation was monitored by HPLC.

b

Data represent mean values ± standard deviations from at least 2 independent experiments.

c

Clinical peak plasma concentrations of the tested drugs (3946).