Area under the concentration-time curve for erlotinib depletion and desmethyl erlotinib formation in primary cultures of human hepatocytes treated with vehicle (DMSO), ritonavir, or ketoconazole and incubated with erlotinib (5 μM)
| Treatment | Liver ID | AUC 0–48h | |
|---|---|---|---|
| Erlotinib | Desmethyl Erlotinib | ||
| μg⋅h/ml | μg⋅h/ml | ||
| DMSO | HH 2011 | 22.7 | 10.2 |
| Hu 1522 | 42.7 | 9.7 | |
| HH 2014 | 11.9 | 6.0 | |
| Hu 1594 | 25.3 | 4.1 | |
| H 1161 | 31.3 | 3.4 | |
| Hu 1595 | 23.7 | 3.2 | |
| Mean ± S.D. | 26.3 ± 10.2 | 6.1 ± 3.2 | |
| Ritonavir | HH 2011 | 102.2 | 3.3 |
| Hu 1522 | 190.8 | 4.4 | |
| HH 2014 | 85.7 | 1.7 | |
| Hu 1594 | 84.9 | 1.4 | |
| H 1161 | 80.3 | 1.1 | |
| Hu 1595 | 76.7 | 1.2 | |
| Mean ± S.D. | 103.4 ± 43.7* | 2.2 ± 1.4* | |
| Ratio to DMSO | 4.2 ± 1.6 | 0.4 ± 0.1 | |
| Ketoconazole | Hu 1594 | 58.9 | 3.9 |
| H 1161 | 61.0 | 4.1 | |
| Hu 1595 | 44.9 | 3.2 | |
| Mean ± S.D. | 55.0 ± 8.7 | 3.7 ± 0.5 | |
| Ratio to DMSO | 2.1 ± 0.2 | 1.1 ± 0.1 | |
↵* P < 0.05 versus DMSO; nonparametric Friedman analysis of variance followed by Dunn’s multiple comparison test.