TABLE 5.
Comparisons of EBR plasma PK following coadministration of 50 mg EBR once daily and 300 mg ATV/100 mg RTV once daily, 400 mg LPV/100 mg RTV twice daily, or 600 mg DRV/100 mg RTV twice daily for 7 days versus administration of (200 mg) GZR once daily for 7 days to healthy adult participants (trial 3)
| PK parameter | GM (95% CI) | GM (95% CI) | GMR (90% CI) | Pseudo-within-subject CV (%)a |
|---|---|---|---|---|
| EBR/ATV/RTVb | EBR (n = 10) | EBR + ATV/RTV (n = 8)c | EBR + ATV/RTV vs EBR | |
| AUC0–24 (μM × h)d | 1.42 (1.04–1.96) | 6.77 (5.18–8.85) | 4.76 (4.07–5.56) | 16.9 |
| Cmax (nM)d | 97.5 (68.9–138) | 405 (317–516) | 4.15 (3.46–4.97) | 20.5 |
| C24 (nM)d | 37.9 (27.3–52.6) | 245 (181–330) | 6.45 (5.51–7.54) | 16.6 |
| Tmax (h)e | 4.09 (3.00–6.04) | 4.01 (3.01–8.01) | ||
| EBR/LPV/RTVf | EBR (n = 10) | EBR + LPV/RTV (n = 9)g | EBR + LPV/RTV vs EBR | |
| AUC0–24 (μM × h)d | 1.43 (1.11–1.83) | 5.29 (3.86–7.26) | 3.71 (3.05–4.53) | 22.4 |
| Cmax (nM)d | 109 (86.7–137) | 313 (225–434) | 2.87 (2.29–3.58) | 25.3 |
| C24 (nM)d | 40.6 (30.1–54.7) | 186 (136–254) | 4.58 (3.72–5.64) | 23.7 |
| Tmax (h)e | 5.00 (4.00–8.00) | 5.00 (4.00–6.00) | ||
| EBR/DRV/RTVh | EBR (n = 10) | EBR + DRV/RTV (n = 8)i | EBR + DRV/RTV vs EBR | |
| AUC0–24 (μM × h)d | 1.40 (0.972–2.00) | 2.32 (1.71–3.15) | 1.66 (1.35–2.05) | 22.4 |
| Cmax (nM)d | 96.4 (65.5–142) | 161 (114–228) | 1.67 (1.36–2.05) | 22.1 |
| C24 (nM)d | 38.4 (24.9–59.2) | 70.0 (47.8–102) | 1.82 (1.39–2.39) | 28.9 |
| Tmax (h)e | 4.50 (2.00–6.00) | 4.00 (2.01–5.00) |
Pseudo-within-subject percent CV = 100 × sqrt([σ2A + σ2B – 2σAB]/2), where σ2A and σ2B are the estimated variances on the log scale for the two treatments and σAB is the corresponding estimated covariance, each obtained from the linear mixed-effects model.
EBR plasma PK following EBR administration alone and coadministration with ATV/RTV.
One participant was discontinued by the investigator on day 13 of period 2, and one participant was discontinued by the investigator on day 7 of period 2.
Back-transformed least-squares mean (ratio) and CI from a linear mixed-effects model with natural-log-transformed values.
Median and range are reported for Tmax.
EBR plasma PK following EBR administration alone and coadministration with LPV/RTV.
One participant withdrew from the study on day 4 of period 2 (during the administration of LPV).
EBR plasma PK following EBR administration alone and coadministration with DRV/RTV.
One participant was discontinued from the study on day 11 of period 2, and one participant was discontinued from the study on day 13 of period 2.