Table 2.
Summary of Crenolanib Pharmacokinetic Parameters for Patients With Newly Diagnosed DIPG (stratum A)
Dosage (mg/m2) | Subgroup | Day | N | T MAX (h) | C MAX (nM) | a AUC0–T (h·nM) | CL/F (L/h/m2) | Half-life (h) |
---|---|---|---|---|---|---|---|---|
100 | A1 | D1 | 5 | 4 (2–8) | 645 (558–1690) | 8683 (4566–15 895) | 26.2 (14.3–49.7) | 8.5 (6.6–10.9) |
D28 | 4 | 6 (2–8) | 750 (298–981) | 7340 (3551–11 022) | 27.5 (17.6–59.9) | 4.9 (3.6–8.0) | ||
A2 | D1 | 6 | 2 (2–4) | 692 (297–2450) | 7397 (3759–16 455) | 32.9 (11.9–66.6) | 6.8 (5.7–12.8) | |
D28 | 5 | 4 (2–8) | 651 (200–1320) | 6945 (2774–13 864) | 32.6 (14.4–68.0) | 5.1 (5.0–8.0) | ||
130 | D1 | 6 | 2 (1–8) | 733 (273–2240) | 5951 (2675–15 291) | 52.1 (20.6–111) | 7.3 (2.2–8.2) | |
D28 | 6 | 4 (2–8) | 1110 (273–1860) | 14 212 (3936–19 795) | 17.6 (13.9–59.3) | 6.1 (3.9–10.8) | ||
170 | D1 | 6 | 4 (1–8) | 1240 (494–1880) | 14 989 (6187–25 360) | 25.4 (15.0–62.8) | 8.5 (6.0–9.2) | |
D28 | 6 | 3 (1–4) | 2010 (1300–4210) | 24 522 (12 548–52 999) | 13.2 (6.4–27.5) | 7.2 (4.4–14.2) | ||
220 | D1 | 7 | 4 (2–8) | 1890 (431–5970) | 22 060 (4826–64 870) | 21.6 (7.9–98.4) | 6.75 (5.4–8.3) | |
D28 | 6 | 2 (1–8) | 2270 (1030–9620) | 28 394 (7914–105 521) | 13.7 (4.3–60.4) | 5.5 (4.5–7.6) |
aOn day 1, AUC0–T corresponds to AUC0–∞. On day 28, AUC0–T corresponds to AUC0–24h.