Table 2.
Summary of pharmacokinetic parameters for surotomycin. Following administration of a single dose and following administration of a single dose (day 1) and multiple doses (day 14)
| Single ascending dose | Multiple ascending dose | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Day 1 | Day 14 | |||||||||
| Parameter | 500 mg | 1000 mg | 2000 mg | 4000 mg | 250 mg BID | 500 mg BID | 1000 mg BID | 250 mg BID | 500 mg BID | 1000 mg BID |
| Tmax, h (range) | 6.0 (4.0–8.0) | 10.0 (6.00–24.0) | 8.0 (4.00–12.0) | 12.0 (4.00–12.0) | 9.0 (6.0–12.0) | 6.0 (6.0–9.0) | 7.5 (6.0–9.0) | 4.5 (0.0–12.0) | 6.0 (0.0–9.0) | 1.8 (0.0–6.0) |
| Cmax, ng/mL (range) | 10.5 (5.1–30.1) | 21.5 (14.0–56.6) | 66.6 (36.9–137) | 86.7 (36.1–320) | 6.8 (3.4–13.8) | 11.0 (6.2–23.1) | 21.0 (15.2–27.3) | 25.5 (18.3–59.4) | 37.6 (16.5–106) | 93.5 (67.4–127) |
| AUC0–t, ng*h/mL (range) | 260 (116–531) | 664 (499–1648) | 1863 (862–3284) | 2481 (1419–6521) | 41.2 (28.2–101.2) | 49.4 (35.0–159) | 118 (75.1–157) | 274 (203–653) | 313 (141–913) | 771 (543–1029) |
| Half-life, h (range) | 18.3 (15.5–22.8) | 21.1 (14.7–32.5) | 16.3 (11.4–34.5) | 14.8 (10.4–21.5) | ND | ND | ND | ND | ND | ND |
| AUC0-∞, ng*h/mL (range) | 317 (147–565) | 702 (571–1754) | 2085 (905–3355) | 2572 (1507–6624) | ND | ND | ND | ND | ND | ND |
AUC Area under the concentration-time curve, AUC 0-t, AUC from 0 to last measurable plasma concentration; AUC 0-∞, AUC from 0 to infinity; BID Twice daily, C max Maximum plasma concentration, ND Not determined, T max Time to maximum plasma concentration