Table 2.
Comparison of relative levels (expressed as percentage) of NVP metabolites in clinical, pre-clinical and in vitro studies.
| Study Type | Sample | 2-OH-NVP * | 12-OH-NVP * | 3-OH-NVP * | 8-OH-NVP * | Ref. |
|---|---|---|---|---|---|---|
| Clinical, 2 weeks of NVP treatment | Human plasma | 13 | 43 | 39 | 2.0 | [40] |
| Clinical, 4 weeks of NVP treatment | Human plasma | 15 | 43 | 42 | 2.0 | [40] |
| Clinical, Steady state NVP treatment | Human urine | 23 | 33 | 33 | 1.0 | [14] |
| Clinical, Steady state NVP treatment | Human plasma | 13 | 80 | 6.0 | 0.0 | [41] |
| Clinical, Steady state NVP treatment | Human plasma | 16 | 75 | 7.0 | 2.0 | [42] |
| Clinical, Single Dose NVP treatment | Human plasma | 32 | 52 | 16 | 0.0 | [38] |
| Clinical, Steady state NVP treatment | Human plasma | 5 | 51 | 9 | 35 | [38] |
| In vitro, spheroids of freshly isolated rat primary hepatocytes, exposed to NVP for 11 days | Cell culture supernatant of rat hepatocytes | 25 | 57 | 18 | 0.0 | [6] |
| In vitro, human cryopreserved microsomal preparations | Microsomes, reaction buffer | 39 | 27 | 27 | 7.0 | [16] |
| In vitro, HLC spheroids exposed to NVP for 10 days | Human cell culture supernatant | 60 | 28 | 10 | 2.0 | Present study |
* the relative amounts of NVP metabolites were collected from the literature considering total amounts of metabolites, including Phase II metabolites that were incorporated as their Phase I form.