Toxicity profile in phase Ib
| Phase Ib (n=16) | |||||
| Type of adverse event (n=16) | Any grade, n (%) | Grades 1–2, n (%) | Grade 3, n (%) | Grade 4, n (%) | Grade 5, n (%) |
| Hematological toxicity | |||||
| Leukopenia | 12 (75.0) | 11 (68.8) | 1 (6.3) | 0 | 0 |
| Neutropenia | 10 (62.5) | 7 (43.8) | 3 (18.8) | 0 | 0 |
| Thrombocytopenia | 9 (56.3) | 7 (43.8) | 2 (12.5) | 0 | 0 |
| Anemia | 8 (50.0) | 6 (37.5) | 2 (12.5) | 0 | 0 |
| Lymphopenia | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Febrile neutropenia | 1 (6.3) | 0 | 0 | 1 (6.3) | 0 |
| Non-hematological toxicity | |||||
| Fatigue | 14 (87.5) | 11 (68.8) | 3 (18.8) | 0 | 0 |
| Hypertension | 11 (68.8) | 10 (62.5) | 1 (6.3) | 0 | 0 |
| Diarrhea | 8 (50.0) | 8 (50.0) | 0 | 0 | 0 |
| Oral mucositis | 8 (50.0) | 7 (43.8) | 1 (6.3) | 0 | 0 |
| Increased AST | 7 (43.8) | 6 (37.5) | 1 (6.3) | 0 | 0 |
| Nausea | 6 (37.5) | 6 (37.5) | 0 | 0 | 0 |
| Increased ALT | 5 (31.3) | 4 (25.0) | 1 (6.3) | 0 | 0 |
| Anorexia | 4 (25.0) | 4 (25.0) | 0 | 0 | 0 |
| Constipation | 3 (18.8) | 3 (18.8) | 0 | 0 | 0 |
| Hyponatremia | 3 (18.8) | 3 (18.8) | 0 | 0 | 0 |
| Hypothyroidism | 3 (18.8) | 2 (12.5) | 1 (6.3) | 0 | 0 |
| Palmar-plantar erythrodysesthesia syndrome | 3 (18.8) | 3 (18.8) | 0 | 0 | 0 |
| Skin/subcutaneous tissue disorders | 3 (18.8) | 3 (18.8) | 0 | 0 | 0 |
| Stomach pain | 3 (18.8) | 3 (18.8) | 0 | 0 | 0 |
| Vomiting | 3 (18.8) | 3 (18.8) | 0 | 0 | 0 |
| Hypokalemia | 3 (18.8) | 2 (12.5) | 1 (6.3) | 0 | 0 |
| Increased ALP | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Infection | 2 (12.5) | 0 | 1 (6.3) | 1 (6.3) | 0 |
| Dysgeusia | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Epistaxis | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Fever | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Hypermagnesemia | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Periodontal disease | 2 (12.5) | 2 (12.5) | 0 | 0 | 0 |
| Arthralgia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Body pain | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Bronchopulmonary hemorrhage | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Renal function deterioration | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Dry mouth | 1 (6.3) | 0 | 1 (6.3) | 0 | 0 |
| Flatulence | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Headache | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Hiccups | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Hypercalcemia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Hypocalcemia | 1 (6.3) | 1 (6.3) | |||
| Hypernatremia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Hypomagnesemia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Hypophosphatemia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Myalgia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Odynophagia | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Tumor lesions bleeding | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Periorbital edema | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Proteinuria | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
| Thromboembolic event | 1 (6.3) | 0 | 0 | 1 (6.3) | 0 |
| Weight loss | 1 (6.3) | 1 (6.3) | 0 | 0 | 0 |
ALP, alkaline phosphatase; ALT, alanine aminotransferase; AST, aspartate aminotransferase.