Table 2.

AEs with frequency ≥15% irrespective of causality for Parts A and B in total or Part C in total

Parts A and BPart C
Schedule 1 (continuous)Schedule 2 (4/7)Schedule 2 (2/7)
80 mg160 mg240 mg320 mg400 mg480 mg600 mg480 mg640 mg640 mg800 mg480 mg bid;
bidbidbidbidbidbidbidbidbidbidbidTotal4/7
Number (%) of patients(n = 5)(n = 5)(n = 6)(n = 12)(n = 11)(n = 6)(n = 2)(n = 11)(n = 10)(n = 8)(n = 14)(N = 90)(n = 59)
Patients with any AE5 (100)5 (100)6 (100)12 (100)11 (100)6 (100)2 (100)11 (100)10 (100)8 (100)14 (100)90 (100)59 (100)
Diarrhea1 (20)1 (20)4 (67)11 (92)11 (100)6 (100)2 (100)9 (82)9 (90)4 (50)12 (86)70 (78)47 (80)
Nausea0 (0)2 (40)1 (17)8 (67)4 (36)5 (83)2 (100)5 (45)7 (70)3 (38)7 (50)44 (49)33 (56)
Vomiting0 (0)1 (20)2 (33)5 (42)4 (36)3 (50)1 (50)5 (45)5 (50)3 (38)6 (43)35 (39)26 (44)
Fatigue1 (20)2 (40)2 (33)5 (42)3 (27)2 (33)2 (100)3 (27)2 (20)4 (50)7 (50)33 (37)24 (41)
Decreased appetite1 (20)0 (0)1 (17)2 (17)5 (45)3 (50)0 (0)3 (27)5 (50)1 (13)5 (36)26 (29)25 (42)
Hyperglycemia2 (40)1 (20)0 (0)0 (0)4 (36)3 (50)1 (50)4 (36)4 (40)2 (25)5 (36)26 (29)24 (41)
Maculopapular rash1 (20)2 (40)1 (17)3 (25)3 (27)3 (50)2 (100)3 (27)1 (10)1 (13)4 (29)24 (27)15 (25)
Constipation1 (20)0 (0)2 (33)4 (33)4 (36)0 (0)0 (0)1 (9)1 (10)2 (25)2 (14)17 (19)10 (17)
Abdominal pain0 (0)0 (0)1 (17)5 (42)2 (18)2 (33)0 (0)2 (18)0 (0)3 (38)0 (0)15 (17)16 (27)
Pyrexia1 (20)1 (20)1 (17)2 (17)1 (9)3 (50)2 (100)1 (9)3 (30)0 (0)0 (0)15 (17)6 (10)
Headache0 (0)1 (20)1 (17)2 (17)1 (9)1 (17)0 (0)2 (18)1 (10)0 (0)0 (0)9 (10)15 (25)
Anemia0 (0)0 (0)1 (17)0 (0)1 (9)0 (0)0 (0)2 (18)1 (10)2 (25)0 (0)7 (8)12 (20)
Increased blood creatinine0 (0)1 (20)0 (0)1 (8)3 (27)0 (0)0 (0)0 (0)0 (0)1 (13)0 (0)6 (7)10 (17)
Proteinuria0 (0)0 (0)0 (0)0 (0)1 (9)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)1 (1)13 (22)
Asthenia0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)12 (20)
Hypomagnesemia0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)0 (0)9 (15)