Table 2.
Adverse events occurring in ≥ 20% of study participants in any dose level
| Adverse event | Level 1 (n = 6) | Level 2 (n = 12) | Total (n = 18) | |||
|---|---|---|---|---|---|---|
| All grades | Grade ≥ 3 | All grades | Grade ≥ 3 | All grades | Grade ≥ 3 | |
| Any adverse event | 6 (100.0) | 6 (100.0) | 12 (100.0) | 12 (100.0) | 18 (100.0) | 18 (100.0) |
| System organ class | ||||||
| Preferred term | ||||||
| Blood and lymphatic system disorders | ||||||
| Anemia | 3 (50.0) | 1 (16.7) | 7 (58.3) | 4 (33.3) | 10 (55.6) | 5 (27.8) |
| Febrile neutropenia | 0 | 0 | 3 (25.0) | 3 (25.0) | 3 (16.7) | 3 (16.7) |
| Gastrointestinal and related disorders | ||||||
| Constipation | 4 (66.7) | 0 | 3 (25.0) | 0 | 7 (38.9) | 0 |
| Diarrhoea | 1 (16.7) | 0 | 3 (25.0) | 0 | 4 (22.2) | 0 |
| Nausea | 6 (100.0) | 0 | 11 (91.7) | 0 | 17 (94.4) | 0 |
| Stomatitis | 3 (50.0) | 1 (16.7) | 7 (58.3) | 0 | 10 (55.6) | 1 (5.6) |
| Vomiting | 4 (66.7) | 0 | 8 (66.7) | 0 | 12 (66.7) | 0 |
| General disorders and administration site conditions | ||||||
| Fatigue | 2 (33.3) | 0 | 5 (41.7) | 0 | 7 (38.9) | 0 |
| Malaise | 2 (33.3) | 0 | 5 (41.7) | 0 | 7 (38.9) | 0 |
| Edema peripheral | 1 (16.7) | 0 | 3 (25.0) | 0 | 4 (22.2) | 0 |
| Pyrexia | 2 (33.3) | 0 | 2 (16.7) | 0 | 4 (22.2) | 0 |
| Infections and infestations | ||||||
| Upper respiratory tract infection | 3 (50.0) | 0 | 3 (25.0) | 0 | 6 (33.3) | 0 |
| Investigations | ||||||
| ALT increased | 4 (66.7) | 3 (50.0) | 12 (100.0) | 12 (100.0) | 16 (88.9) | 15 (83.3) |
| AST increased | 3 (50.0) | 2 (33.3) | 12 (100.0) | 12 (100.0) | 15 (83.3) | 14 (77.8) |
| Blood CPK increased | 0 | 0 | 6 (50.0) | 2 (16.7) | 6 (33.3) | 2 (11.1) |
| Blood LDH increased | 0 | 0 | 3 (25.0) | 0 | 3 (16.7) | 0 |
| GGT increased | 2 (33.3) | 1 (16.7) | 7 (58.3) | 3 (25.0) | 9 (50.0) | 4 (22.2) |
| Lymphocyte count decreased | 1 (16.7) | 1 (16.7) | 4 (33.3) | 4 (33.3) | 5 (27.8) | 5 (27.8) |
| Neutrophil count decreased | 6 (100.0) | 6 (100.0) | 11 (91.7) | 9 (75.0) | 17 (94.4) | 15 (83.3) |
| Platelet count decreased | 2 (33.3) | 1 (16.7) | 7 (58.3) | 3 (25.0) | 9 (50.0) | 4 (22.2) |
| White blood cell count decreased | 5 (83.3) | 5 (83.3) | 9 (75.0) | 8 (66.7) | 14 (77.8) | 13 (72.2) |
| Metabolism and nutrition disorders | ||||||
| Decreased appetite | 6 (100.0) | 1 (16.7) | 7 (58.3) | 0 | 13 (72.2) | 1 (5.6) |
| Musculoskeletal and connective tissue disorders | ||||||
| Myalgia | 1 (16.7) | 0 | 4 (33.3) | 0 | 5 (27.8) | 0 |
| Nervous system and psychiatric disorders | ||||||
| Headache | 2 (33.3) | 0 | 2 (16.7) | 0 | 4 (22.2) | 0 |
| Psychiatric disorders | ||||||
| Insomnia | 2 (33.3) | 0 | 3 (25.0) | 0 | 5 (27.8) | 0 |
| Skin and subcutaneous tissue disorders | ||||||
| Pigmentation disorder | 2 (33.3) | 0 | 0 | 0 | 2 (11.1) | 0 |
All data are expressed as n (%). Adverse events were coded according to preferred terms in the Medical Dictionary for Drug Regulatory Activities (MedDRA), version 22.1
ALT alanine aminotransferase, AST aspartate aminotransferase, CPK creatine phosphokinase, GGT gamma-glutamyltransferase, LDH lactate dehydrogenase