Table 1.
RG7116 pharmacokinetic parameters in FaDu-bearing SCID-beige mice by non-compartmental analysis treated with (A) weekly administration of RG7116 and (B) a single dose of RG7116
| Study | Dose (mg/kg) [no. of mice] | C min (µg/mL) | ||
|---|---|---|---|---|
| Day 7a | Day 14a | Day 21a | ||
| (A) Weekly administration PK | ||||
| FaDu_001 | 0.3 [n = 9] | 1.66 (15.0) | NM | 1.48 (53.4) |
| 1 [n = 10] | 5.12 (23.8) | NM | 10.4 (21.2) | |
| 3 [n = 10] | 17.8 (18.9) | NM | 36.7 (21.2) | |
| 10 [n = 10] | 58.3 (13.0) | NM | 102 (24.1) | |
| FaDu_008 | 0.3 [n = 15] | 0.79 (25.3) | 0.86 (55.8) | 1.26 (52.0) |
| 3 [n = 15] | 8.88 (15.6) | 13.5 (16.9) | 17.6 (23.7) | |
| Study | Dose (mg/kg) [no. of mice] | C max (µg/mL) | AUCinf (haµg/mL) | CLtotal (mL/h) | t 1/2 (h) |
|---|---|---|---|---|---|
| (B) Single-dose PK | |||||
| FaDu_006 | 0.3 [n = 35] | 2.55 | 192 | 0.0312 | 62.4 |
| 1 [n = 35] | 9.73 | 863 | 0.0232 | 94.2 | |
| FaDu_008 | 3 [n = 15] | 17.4 | 4811 | 0.0125 | 167 |
Data are mean (CV %)
AUC, area under the curve; CLtotal, total clearance; C max, peak plasma RG7116 concentration; CV %, coefficient of variation; NM, not measured; PK, pharmacokinetics; t 1/2, elimination half life
aDay since randomization/first dose. For all PK analyses, n = 5 mice were analyzed per time point