Table 3.
Effect of COBI, emtricitabine, and elvitegravir on the cytotoxicity of TFV in HEK293T cells transiently expressing renal anion transporters
| Compound | CC50 [μM]a for: |
||
|---|---|---|---|
| Control | OAT1 | OAT1 + MRP4 | |
| Puromycin | 0.35 ± 0.02 | 0.21 ± 0.10 | 0.22 ± 0.06 |
| TFV | >2,000 | 78.7 ± 1.3 | 299.5 ± 81.3 |
| TFV + COBI (2 μM)b | >2,000 | 68.3 ± 0.4 | 230.9 ± 82.6 |
| TFV + COBI (2 μM) + elvitegravir (4.5 μM) + emtricitabine (8 μM)b | >2,000 | 68.0 ± 4.1 | 228.8 ± 51.2 |
a
The results represent means ± SD from 3 independent experiments performed in HEK293T cells. CC50 values were determined from cell viability (CellTiter Glo) readout.
b
The tested concentrations of COBI, elvitegravir, and emtricitabine correspond to peak plasma levels (Cmax) in HIV-infected patients treated with a clinical dose of each compound.