Table 2.
Treatment-emergent adverse events occurring in >10% of patients in total (safety analysis set) by CTCAE grade.
| AE | Dose escalation | Safety Expansion | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Cohort 1—250 mg/d BID | Cohort 2—500 mg/d BID | Cohort 3—1000 mg/d BID | Cohort 4—2000 mg/d BID | Cohort 5—4000 mg/d TID | Cohort 6—8000 mg/d BID | Cohort 7—16,000 mg/d BID | Cohort 30—4000 mg/d t.i.d. | Cohort 40—4000 mg/d t.i.d. | Total | ||
| Number of patients (% of total) | 3 (5.5%) | 4 (7.4%) | 3 (5.5%) | 4 (7.4%) | 3 (5.5%) | 8 (14.8%) | 7 (13%) | 12 (22.2%) | 10 (18.5%) | 54 (100%) | |
| G1-2 | G3-4 | ||||||||||
| Diarrhoea | 2 (50.0%) | 1 (33.3%) | 2 (50.0%) | 2 (66.7%) | 4 (50.0%) | 6 (85.7%) | 7 (58.3%) | 4 (40.0%) | 26 (48.1%) | 2 (3.7%) | |
| Nausea | 2 (50.0%) | 1 (25%) | 2 (66.7%) | 2 (25.0%) | 5 (71.4%) | 2 (16.7%) | 4 (40.0%) | 17 (31.5%) | 1 (1.9%) | ||
| Vomiting | 1 (25.0%) | 2 (66.7%) | 3 (37.5%) | 6 (85.7%) | 3 (30.0%) | 16 (29.6%) | 1 (1.9%) | ||||
| Decreased appetite | 2 (66.7%) | 1 (12.5%) | 3 (42.9%) | 2 (20.0%) | 8 (14.8%) | 0 (0.0%) | |||||
| Alanine aminotransferase increased | 1 (25.0%) | 1 (25.0%) | 1 (12.5%) | 3 (25.0%) | 6 (11.1%) | 0 (0.0%) | |||||
| Fatigue | 2 (28.6%) | 2 (16.7%) | 2 (20.0%) | 6 (11.1%) | 0 (0.0%) | ||||||
| Serious AEs | |||||||||||