Table 2.
(A) Grade 3 or 4 adverse events suspected to be related to study drug; (B) adverse events suspected to be related to study drug (all grades, in ≥ 10% of patients).
| 10 mg Reg 1 | 20 mgReg 1 | 40 mgReg 1 | 80 mgReg 1 | 150 mg Reg 1 | 300 mgReg 1 | 400 mgReg 1 | 300 mgReg 3 | 500 mgReg 3 | 700 mgReg 3 | All patients | |
|---|---|---|---|---|---|---|---|---|---|---|---|
| N = 3 | N = 4 | N = 4 | N = 4 | N = 4 | N = 7 | N = 5 | N = 8 | N = 6 | N = 6 | N = 51 | |
| (A) Preferred term, n % | |||||||||||
| Thrombocytopenia | 0 | 0 | 0 | 0 | 0 | 4 (57.1) | 4 (80.0) | 0 | 1 (16.7) | 3 (50.0) | 12 (23.5) |
| Lymphopenia | 1 (33.3) | 0 | 0 | 0 | 0 | 0 | 1 (20.0) | 1 (12.5) | 1 (16.7) | 1 (16.7) | 5 (9.8) |
| Neutropenia | 0 | 0 | 0 | 0 | 0 | 1 (14.3) | 1 (20.0) | 0 | 1 (16.7) | 3 (50.0) | 6 (11.8) |
| Lipase increased | 0 | 0 | 1 (25.0) | 0 | 0 | 1 (14.3) | 0 | 1 (12.5) | 1 (16.7) | 1 (16.7) | 5 (9.8) |
| Leukopenia | 0 | 0 | 0 | 0 | 0 | 1 (14.3) | 2 (40.0) | 0 | 0 | 1 (16.7) | 4 (7.8) |
| Anaemia | 0 | 0 | 0 | 0 | 0 | 2 (28.6) | 0 | 0 | 0 | 2 (33.3) | 4 (7.8) |
| White blood cell count decreased | 0 | 0 | 0 | 0 | 0 | 3 (42.9) | 1 (20.0) | 0 | 0 | 0 | 4 (7.8) |
| Granulocytopenia | 0 | 0 | 0 | 0 | 0 | 1 (14.3) | 0 | 0 | 0 | 0 | 1 (2.0) |
| Nausea | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 (12.5) | 1 (16.7) | 0 | 2 (3.9) |
| Lymphocyte count decreased | 0 | 0 | 0 | 0 | 0 | 1 (14.3) | 0 | 0 | 0 | 0 | 1 (2.0) |
| Neutrophil count decreased | 0 | 0 | 0 | 0 | 0 | 2 (28.6) | 0 | 0 | 0 | 0 | 2 (3.9) |
| Hyperlipasaemia | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 (16.7) | 1 (2.0) |
| Hyperlipidaemia | 0 | 0 | 0 | 0 | 0 | 1 (14.3) | 0 | 0 | 0 | 0 | 1 (2.0) |
| Proteinuria | 0 | 0 | 0 | 0 | 0 | 0 | 1 (20.0) | 0 | 0 | 0 | 1 (2.0) |
| (B) Preferred term, n % | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Thrombocytopenia | 0 | 0 | 0 | 0 | 1 (25.0) | 6 (85.7) | 5 (100.0) | 2 (25.0) | 4 (66.6) | 4 (66.6) | 22 (43) |
| Nausea | 0 | 0 | 0 | 0 | 0 | 5 (71.4) | 3 (60.0) | 5 (62.5) | 5 (83.3) | 4 (66.6) | 22 (43) |
| Leukopenia | 1 (33.3) | 0 | 1 (25.0) | 0 | 0 | 3 (42.8) | 4 (80.0) | 1 (12.5) | 1 (16.7) | 3 (50.0) | 14 (27) |
| Fatigue | 1 (33.3) | 0 | 1 (25.0) | 0 | 0 | 4 (57.1) | 1 (20.0) | 3 (37.5) | 2 (33.3) | 1 (16.7) | 13 (26) |
| Vomiting | 0 | 1 (25.0) | 0 | 0 | 0 | 2 (28.6) | 3 (60.0) | 3 (37.5) | 3 (50.0) | 2 (33.3) | 14 (27) |
| Diarrhoea | 0 | 1 (25.0) | 0 | 0 | 1 (25.0) | 2 (28.6) | 2 (40.0) | 2 (25.0) | 1 (16.7) | 2 (33.3) | 11 (22) |
| Neutropenia | 0 | 0 | 0 | 0 | 0 | 3 (42.8) | 3 (60.0) | 1 (12.5) | 1 (16.7) | 3 (50.0) | 11 (22) |
| Lymphopenia | 1 (33.3) | 0 | 1 (25.0) | 0 | 1 (25.0) | 1 (14.3) | 1 (20.0) | 2 (25.0) | 2 (33.3) | 1 (16.7) | 10 (20) |
| Decreased appetite | 0 | 0 | 0 | 0 | 0 | 3 (42.8) | 2 (40.0) | 1 (12.5) | 1 (16.7) | 2 (33.3) | 9 (18) |
| Anaemia | 0 | 0 | 0 | 1 (25.0) | 0 | 2 (28.6) | 3 (60.0) | 0 | 0 | 2 (33.3) | 8 (16) |
| Dysgeusia | 0 | 0 | 1 (25.0) | 0 | 0 | 0 | 0 | 2 (25.0) | 2 (33.3) | 2 (33.3) | 7 (14) |
| Abdominal pain upper | 0 | 0 | 0 | 0 | 0 | 1 (14.3) | 1 (20.0) | 1 (12.5) | 2 (33.3) | 1 (16.7) | 6 (12) |
| Asthenia | 1 (33.3) | 1 (25.0) | 0 | 0 | 1 (25.0) | 1 (14.3) | 1 (20.0) | 0 | 0 | 2 (33.3) | 7 (14) |
| Blood CPK increased | 0 | 0 | 1 (25.0) | 1 (25.0) | 0 | 2 (28.6) | 0 | 2 (25.0) | 0 | 0 | 6 (12) |
| Lipase increased | 0 | 0 | 1 (25.0) | 0 | 0 | 1 (14.3) | 1 (20.0) | 1 (12.5) | 1 (16.7) | 1 (16.7) | 6 (12) |
| ALT increased | 0 | 2 (50.0) | 0 | 0 | 0 | 1 (14.3) | 1 (20.0) | 0 | 0 | 1 (16.7) | 5 (10) |
| AST increased | 0 | 1 (25.0) | 0 | 0 | 1 (25.0) | 1 (14.3) | 1 (20.0) | 1 (12.5) | 0 | 0 | 5 (10) |
| Dizziness | 0 | 1 (25.0) | 0 | 0 | 0 | 1 (14.3) | 1 (20.0) | 1 (12.5) | 1 (16.7) | 0 | 5 (10) |
| Hypoalbuminemia | 0 | 0 | 0 | 0 | 2 (50.0) | 1 (14.3) | 1 (20.0) | 0 | 0 | 1 (16.7) | 5 (10) |
ALT alanine aminotransferase, AST aspartate amino transferase, CPK creatine phosphokinase.
Adverse events suspected to be related to study drug (all grades, in ≥10% of patients.
Reg 1: 3qw dosing, 4-week treatment cycle, continuous; Reg 3: 3qw dosing, 3-week treatment cycle; 2 weeks on treatment and 1 week off treatment.