TABLE 1.
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 |
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.
Data represent mean values ± standard deviations from at least 2 independent experiments.