Table 2.

TRAEs in ≥10% of all patients treated with once-daily dosing

140 mg (n = 3)280 mg (n = 3)420 mg (n = 6)600 mg (n = 87)900 mg (n = 7)All patients (q.d.) (n = 106)
TRAEAnygradeGrade≥3AnygradeGrade≥3AnygradeGrade≥3AnygradeGrade≥3AnygradeGrade≥3AnygradeGrade ≥3
Any TRAE3 (100)1 (33)3 (100)1 (33)6 (100)5 (83)83 (95)36 (41)7 (100)3 (43)102 (96)46 (43)
Diarrhea1 (33)0 (0)3 (100)0 (0)5 (83)2 (33)63 (72)6 (7)6 (86)0 (0)78 (74)8 (8)
Nausea0 (0)0 (0)1 (33)0 (0)3 (50)0 (0)34 (39)2 (2)6 (86)0 (0)44 (42)2 (2)
Vomiting0 (0)0 (0)1 (33)0 (0)2 (33)0 (0)29 (33)4 (5)5 (71)0 (0)37 (35)4 (4)
ALT increased0 (0)0 (0)1 (33)0 (0)4 (67)2 (33)27 (31)10 (11)0 (0)0 (0)32 (30)12 (11)
AST increased0 (0)0 (0)1 (33)1 (33)4 (67)2 (33)24 (28)13 (15)0 (0)0 (0)29 (27)16 (15)
Fatigue1 (33)0 (0)1 (33)0 (0)0 (0)0 (0)19 (22)3 (3)4 (57)1 (14)25 (24)4 (4)
Blood bilirubin increased0 (0)0 (0)1 (33)0 (0)4 (67)1 (17)14 (16)3 (3)0 (0)0 (0)19 (18)4 (4)
Decreased appetite0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)14 (16)0 (0)4 (57)0 (0)18 (17)0 (0)
Abdominal pain1 (33)0 (0)1 (33)0 (0)1 (17)0 (0)7 (8)0 (0)4 (57)1 (14)14 (13)1 (1)
Blood ALP increased0 (0)0 (0)1 (33)0 (0)3 (50)1 (17)9 (10)3 (3)0 (0)0 (0)13 (12)4 (4)
Anemia1 (33)1 (33)1 (33)1 (33)1 (17)1 (17)8 (9)2 (2)0 (0)0 (0)11 (10)5 (5)
  • Abbreviations: ALP, alkaline phosphatase; ALT, alanine aminotransferase; AST, aspartate aminotransferase; q.d., once daily; TRAE, treatment-related adverse event.