Table 2. Main adverse events that occurred in the trial.
| Variables | Any grade | Grade 1–2 | Grade 3 | Grade 4 | |
|---|---|---|---|---|---|
| Number | Percent | ||||
| 600 mg BID (N=6) | |||||
| Clinical | |||||
| Constipation | 4 [4] | 66.7% | 4 [4] | 0 | 0 |
| Myalgia | 3 [3] | 50.0% | 3 [3] | 0 | 0 |
| Dysgeusia | 2 [2] | 33.3% | 2 [2] | 0 | 0 |
| Oedema peripheral | 2 [2] | 33.3% | 2 [2] | 0 | 0 |
| Hepatic function abnormal | 2 [2] | 33.3% | 1 [1] | 1 [1]* | 0 |
| Cholangitis | 1 [1] | 16.7% | 0 | 1 [1] | 0 |
| Thromboembolic event | 1 [1] | 16.7% | 0 | 1 [1]* | 0 |
| Erythema multiforme | 1 [1] | 16.7% | 0 | 1 [1]* | 0 |
| Rash | 1 [1] | 16.7% | 0 | 1 [1]* | 0 |
| Laboratory | |||||
| Alkaline phosphatase increase | 2 [2] | 33.3% | 1[1] | 1[1] | 0 |
| Creatine phosphokinase increase | 2 [2] | 33.3% | 1[1] | 1[1]* | 0 |
| Creatinine increase | 2 [2] | 33.3% | 2[2] | 0 | 0 |
| Lymphocyte decrease | 1 [1] | 16.7% | 0 | 0 | 1 [1] |
| 450 mg BID (N=28; phase 1 N=3, phase 2 N=25) | |||||
| Clinical | |||||
| Constipation | 16 [12] | 57.1 [42.9]% | 16 [12] | 0 | 0 |
| Diarrhea | 3 [2] | 10.7 [7.1]% | 2 [2] | 1 [0] | 0 |
| Pneumonitis | 1 [0] | 3.6 [0.0]% | 0 | 1 [1] | 0 |
| Laboratory | |||||
| Creatine phosphokinase increase | 13 [13] | 46.4% | 12 [12] | 1 [1] | 0 |
| Aspartate aminotransferase increase | 9 [7] | 32.1 [25.0]% | 9 [7] | 0 | 0 |
| Creatinine increase | 8 [8] | 28.6% | 8 [8] | 0 | 0 |
| Bilirubin increase | 6 [6] | 21.4% | 5 [5] | 1 [1] | 0 |
| Hyponatraemia | 1 [1] | 3.6% | 0 | 1 [1] | 0 |
| Neutropenia | 1 [1] | 3.6% | 0 | 1 [1] | 0 |
Total number [ ] is assessed as causally related . *, dose limiting toxicities.