AEs reported by ≥ 20% of patients overall (in either part A or B) split by maximum grade achieved
| . | Patients with AEs, n (%) . | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Part A barasertib dose . | Part B barasertib dose . | ||||||||
| 50 mg (n = 3) . | 100 mg (n = 3) . | 200 mg (n = 3) . | 400 mg (n = 4) . | 800 mg (n = 7) . | 1200 mg (n = 6) . | 1600 mg (n = 6) . | Total (n = 32) . | 1200 mg (n = 32) . | |
| Any event | 3 (100) | 3 (100) | 3 (100) | 4 (100) | 7 (100) | 6 (100) | 6 (100) | 32 (100) | 32 (100) |
| Grade ≥ 3 | 3 (100) | 1 (33) | 3 (100) | 4 (100) | 7 (100) | 5 (83) | 5 (83) | 28 (88) | 24 (75) |
| Febrile neutropenia* | 13 (41) | 15 (47) | |||||||
| Grade 1/2 | 0 | 0 | 1 (33) | 0 | 0 | 0 | 1 (17) | 2 (6) | 2 (6) |
| Grade ≥ 3 | 0 | 0 | 0 | 4 (100) | 2 (29) | 2 (33) | 3 (50) | 11 (34) | 13 (41) |
| Stomatitis/mucosal inflammation events | 12 (38) | 22 (69) | |||||||
| Grade 1/2 | 0 | 0 | 1 (33) | 0 | 2 (28) | 2 (33) | 0 | 5 (16) | 13 (41) |
| Grade ≥ 3 | 0 | 0 | 0 | 1 (25) | 1 (14) | 2 (33) | 3 (50) | 7 (22) | 9 (28) |
| Pyrexia | 13 (41) | 14 (44) | |||||||
| Grade 1/2 | 1 (33) | 0 | 2 (67) | 1 (25) | 3 (43) | 4 (67) | 0 | 11 (34) | 12 (38) |
| Grade ≥ 3 | 0 | 1 (33) | 0 | 0 | 1 (14) | 0 | 0 | 2 (6) | 2 (6) |
| Nausea | 13 (41) | 12 (38) | |||||||
| Grade 1/2 | 0 | 1 (33) | 1 (33) | 2 (50) | 3 (43) | 3 (50) | 3 (50) | 13 (41) | 11 (34) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 (3) |
| Fatigue | 10 (31) | 15 (47) | |||||||
| Grade 1/2 | 0 | 1 (33) | 0 | 1 (25) | 2 (29) | 4 (67) | 2 (33) | 10 (31) | 12 (38) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 3 (9) |
| Diarrhea | 9 (28) | 17 (53) | |||||||
| Grade 1/2 | 0 | 0 | 1 (33) | 0 | 1 (14) | 4 (67) | 2 (33) | 9 (28) | 17 (53) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Constipation | 11 (34) | 5 (15) | |||||||
| Grade 1/2 | 0 | 1 (33) | 1 (33) | 1 (25) | 2 (29) | 4 (67) | 1 (17) | 10 (31) | 5 (15) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 1 (14) | 0 | 0 | 1 (3) | 0 |
| Vomiting | 8 (25) | 9 (28) | |||||||
| Grade 1/2 | 1 (33) | 0 | 0 | 0 | 3 (43) | 2 (33) | 2 (33) | 8 (25) | 9 (28) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Peripheral edema | 9 (28) | 7 (22) | |||||||
| Grade 1/2 | 2 (67) | 1 (33) | 0 | 1 (25) | 1 (14) | 1 (17) | 2 (33) | 8 (25) | 6 (19) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 1 (17) | 0 | 1 (3) | 1 (3) |
| Headache | 4 (13) | 9 (28) | |||||||
| Grade 1/2 | 1 (33) | 1 (33) | 0 | 0 | 0 | 1 (17) | 0 | 3 (9) | 9 (28) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 1 (17) | 1 (3) | 0 |
| Alopecia | 5 (16) | 8 (25) | |||||||
| Grade 1/2 | 0 | 0 | 0 | 1 (25) | 3 (43) | 0 | 1 (17) | 5 (16) | 8 (25) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Epistaxis | 5 (16) | 8 (25) | |||||||
| Grade 1/2 | 0 | 0 | 0 | 1 (33) | 1 (14) | 1 (17) | 1 (17) | 4 (13) | 7 (22) |
| Grade ≥ 3 | 1 (33) | 0 | 0 | 0 | 0 | 0 | 0 | 1 (3) | 1 (3) |
| . | Patients with AEs, n (%) . | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Part A barasertib dose . | Part B barasertib dose . | ||||||||
| 50 mg (n = 3) . | 100 mg (n = 3) . | 200 mg (n = 3) . | 400 mg (n = 4) . | 800 mg (n = 7) . | 1200 mg (n = 6) . | 1600 mg (n = 6) . | Total (n = 32) . | 1200 mg (n = 32) . | |
| Any event | 3 (100) | 3 (100) | 3 (100) | 4 (100) | 7 (100) | 6 (100) | 6 (100) | 32 (100) | 32 (100) |
| Grade ≥ 3 | 3 (100) | 1 (33) | 3 (100) | 4 (100) | 7 (100) | 5 (83) | 5 (83) | 28 (88) | 24 (75) |
| Febrile neutropenia* | 13 (41) | 15 (47) | |||||||
| Grade 1/2 | 0 | 0 | 1 (33) | 0 | 0 | 0 | 1 (17) | 2 (6) | 2 (6) |
| Grade ≥ 3 | 0 | 0 | 0 | 4 (100) | 2 (29) | 2 (33) | 3 (50) | 11 (34) | 13 (41) |
| Stomatitis/mucosal inflammation events | 12 (38) | 22 (69) | |||||||
| Grade 1/2 | 0 | 0 | 1 (33) | 0 | 2 (28) | 2 (33) | 0 | 5 (16) | 13 (41) |
| Grade ≥ 3 | 0 | 0 | 0 | 1 (25) | 1 (14) | 2 (33) | 3 (50) | 7 (22) | 9 (28) |
| Pyrexia | 13 (41) | 14 (44) | |||||||
| Grade 1/2 | 1 (33) | 0 | 2 (67) | 1 (25) | 3 (43) | 4 (67) | 0 | 11 (34) | 12 (38) |
| Grade ≥ 3 | 0 | 1 (33) | 0 | 0 | 1 (14) | 0 | 0 | 2 (6) | 2 (6) |
| Nausea | 13 (41) | 12 (38) | |||||||
| Grade 1/2 | 0 | 1 (33) | 1 (33) | 2 (50) | 3 (43) | 3 (50) | 3 (50) | 13 (41) | 11 (34) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 (3) |
| Fatigue | 10 (31) | 15 (47) | |||||||
| Grade 1/2 | 0 | 1 (33) | 0 | 1 (25) | 2 (29) | 4 (67) | 2 (33) | 10 (31) | 12 (38) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 3 (9) |
| Diarrhea | 9 (28) | 17 (53) | |||||||
| Grade 1/2 | 0 | 0 | 1 (33) | 0 | 1 (14) | 4 (67) | 2 (33) | 9 (28) | 17 (53) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Constipation | 11 (34) | 5 (15) | |||||||
| Grade 1/2 | 0 | 1 (33) | 1 (33) | 1 (25) | 2 (29) | 4 (67) | 1 (17) | 10 (31) | 5 (15) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 1 (14) | 0 | 0 | 1 (3) | 0 |
| Vomiting | 8 (25) | 9 (28) | |||||||
| Grade 1/2 | 1 (33) | 0 | 0 | 0 | 3 (43) | 2 (33) | 2 (33) | 8 (25) | 9 (28) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Peripheral edema | 9 (28) | 7 (22) | |||||||
| Grade 1/2 | 2 (67) | 1 (33) | 0 | 1 (25) | 1 (14) | 1 (17) | 2 (33) | 8 (25) | 6 (19) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 1 (17) | 0 | 1 (3) | 1 (3) |
| Headache | 4 (13) | 9 (28) | |||||||
| Grade 1/2 | 1 (33) | 1 (33) | 0 | 0 | 0 | 1 (17) | 0 | 3 (9) | 9 (28) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 1 (17) | 1 (3) | 0 |
| Alopecia | 5 (16) | 8 (25) | |||||||
| Grade 1/2 | 0 | 0 | 0 | 1 (25) | 3 (43) | 0 | 1 (17) | 5 (16) | 8 (25) |
| Grade ≥ 3 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Epistaxis | 5 (16) | 8 (25) | |||||||
| Grade 1/2 | 0 | 0 | 0 | 1 (33) | 1 (14) | 1 (17) | 1 (17) | 4 (13) | 7 (22) |
| Grade ≥ 3 | 1 (33) | 0 | 0 | 0 | 0 | 0 | 0 | 1 (3) | 1 (3) |
Febrile neutropenia was classed as CTCAE Grade ≥ 3, some febrile neutropenia events of Grade 1 and 2 were reported in error by the investigators.