Table 4 Summary of H3B-8800 plasma PK parameters on Day 4 following once-daily dose regiments.

From: Phase I First-in-Human Dose Escalation Study of the oral SF3B1 modulator H3B-8800 in myeloid neoplasms

Statistical summary of plasma PK parameters on Day 1

Dose (mg)

n

Tmax (h)

Cmax (µg/L)

AUC0-24 (µg*h/L)

t1/2 (h)

1.0

3

2 (0.5–2)

0.835 (90.8)

4.89 (38.6)

5.1 (65.3)

2.0

7

2 (0.5–6)

1.09 (64.4)

8.39 (42.0)

5.4 (31.9)

3.5

6

1.5 (0.5–2)

2.78 (82.4)

15.6 (52.5)

5.4 (15.2)

5.0

9

1 (0.5–4)

3.94 (30.0)

24.5 (24.2)

5.8 (27.1)

7.0

19

1 (0.5–4)

9.61 (69.7)

39.4 (38.7)

5.3 (23.8)

10

7

1 (0.5–2)

12.7 (36.3)

51.0 (20.5)

5.5 (14.2)

12

5

2 (1–2)

12.2 (37.4)

64.7 (33.4)

5.4 (17.3)

14

10

1 (0.5–2)

25.6 (63.9)

108 (55.1)

5.1 (21.8)

20

8

0.75 (0.5–4)

33.6 (49.2)

142 (43.0)

5.1 (10.3)

30

4

1.25 (0.5–2)

34.4 (44.7)

159 (23.9)

5.3 (10.2)

40

6

0.5 (0.5–1)

73.3 (85.8)

265 (61.5)

4.5 (17.2)

  1. Median (min–max) for Tmax and geometric mean (CV%) for other parameters.