Table 2.
Effect of specific CYP inhibitors on maraviroc metabolism in human liver microsomes
| Inhibitor (CYP) | Inhibition (% of control activity remaining) | |
|---|---|---|
| UK-408,027 formation | Maraviroc depletion | |
| 30 µM furafylline (CYP1A2) | 85.0 ± 15.8 | ND |
| 10 µM sulphaphenazole (CYP2C9) | 108.1 ± 27.7 | 99.1 ± 5.3 |
| 10 µM benzylnirvanol (CYP2C19) | 85.4 ± 47 | ND |
| 1 µM quinidine (CYP2D6) | 102.2 ± 20.2 | 100.3 ± 16.0 |
| 1 µM ketoconazole (CYP3A4) | 16.1 ± 5.7* | 17.3 ± 3.4* |
*
P < 0.00001 compared with control activity. ND, not determined. Maraviroc concentrations were 50 µM and 1 µM for UK-408,027 formation and substrate depletion, respectively. Values are mean ± SD of quadruplicate determinations. Uninhibited control activities: UK-408,027 formation, 75.9 pmol mg−1 min−1; maraviroc depletion, 0.106 µl pmol−1 min−1.