Descriptive statistics for pharmacokinetic parameter estimates of AMG 557 after subcutaneous or intravenous administration of AMG 557 to subjects with systemic lupus erythematosus
| SAD | MAD | |||||
|---|---|---|---|---|---|---|
| Dose (mg) | tmax* (day) | Cmax† (µg/mL) | AUCinf†‡ (µg. day/mL) | tmax* (day) | Cmax† (µg/mL) | AUC0–14† (µg. day/mL) |
| 1.8 | 4.2 (4.0–7.3) | 0.0285 (0.00531) | NR | – | – | – |
| 6 | 6.9 (2.9–7.0) | 0.0819 (0.0428) | 1.59 (NR) | 7.0 (7.0–8.0) | 0.101 (0.0335) | 1.06 (0.358) |
| 18 | 5.0 (2.0–7.3) | 0.816 (0.487) | 8.08 (3.70) | 7.0 (6.9–7.0) | 1.63 (1.07) | 18.5 (12.9) |
| 18§ | 0.7 (0.5–0.7) | 6.75 (0.940) | 31.6 (9.83) | – | – | – |
| 30 | – | – | – | 7.0 (6.9–7.0) | 3.34 (1.46) | 37.6 (15.7) |
| 45 | – | – | – | 7.0 (0–8.0) | 6.71 (1.85) | 78.6 (20.7) |
| 60 | 3.0 (0.2–7.3) | 6.57 (3.07) | 94.6 (35.6) | – | – | – |
| 70 | – | – | – | 7.0 (6.1–7.1) | 20.2 (8.81) | 243 (109) |
| 140 | 3.1 (3.0–7.1) | 14.4 (6.70) | 352 (225) | 7.0 (4.9–8.1) | 36.0 (14.5) | 467 (191) |
| 210 | 3.9 (3.0–7.0) | 20.7 (6.04) | 505 (193) | 7.6 (7.1–8.0) | 72.7 (14.2) | 940 (191) |
MAD: AMG 557 was given every other week ×7. The pharmacokinetic parameter estimates for the seventh dose were shown.
SAD: n=3–7 for each dose cohort. MAD: n=3–6 for each dose cohort.
AUCinf, or AUC0–14, area under the concentration–time curve from time zero extrapolated to infinity, or from time zero to 14 days during a dosing interval; Cmax, maximum observed concentration; tmax, time at which maximum concentration occurred.
*tmax was reported as median (range); tmax for intravenous cohort reflects time post end of infusion.
†Cmax and AUC were reported as mean (SD).
‡AUCinf NR for subjects if AUC extrapolation exceeded 20%; 6 mg subcutaneous SAD data reported for one subject only.
§Intravenous administration. All other dose cohorts received subcutaneous administration(s).
AUC, area under the curve; MAD, multiple-ascending dose; NR, not reported; SAD, single-ascending dose.