Table 4.
Mean (SD) pharmacokinetic parameters of active moiety by CYP2C19 genotype following single (day 1) and multiple (day 4) dose administration of nelfinavir in healthy subjects
| Normal dose* | High dose* | ||||||
|---|---|---|---|---|---|---|---|
| Parameter (units) | Study day | *1*1†[n = 38] | *1*2†[n = 22] | *2*2†[n = 6] | *1*1 [n = 38] | *1*2 [n = 22] | *2*2 [n = 6] |
| Cmax (µg ml–1) | Day 1 | 10.4 (3.4) | 12.0 (2.2) | 9.0 (2.2) | 11.1 (3.3) | 10.8 (3.4) | 10.1 (3.4) |
| Day 4 | 13.0 (3.3) | 15.6 (4.2) | 14.5 (4.9) | 17.3 (4.4) | 21.9 (5.2) | 19.3 (3.6) | |
| AUC (µg h–1 ml–1) | Day 1 | 71.5 (26.3) | 85.5 (15.3) | 67.8 (22.5) | 75.1 (23.6) | 78.3 (27.4) | 76.5 (28.4) |
| Day 4 | 89.2 (26.6) | 115.2 (30.9) | 119.5 (43.0) | 120.0 (32.5) | 162.4 (35.8) | 161.9 (35.8) | |
*
Normal dose was 1250 mg nelfinavir q12h on days 1–3 and the morning dose of 1250 mg on day 4. High dose was 1250 mg nelfinavir q12h on days 1–3 and the morning dose of 3125 mg on day 4.
†
*1*1, *1*2 and *2*2 genotypes correspond to extensive metabolizer, heterozygous poor metabolizer, and homozygous poor metabolizer phenotypes, respectively.