Table 2. Most common TEAEs (⩾10% of all patients) for escalation and RP2D dose levels.
|
All subjects (n=80; %) |
||||||
|---|---|---|---|---|---|---|
| Preferred terms | 25 mg QOD–200 mg QD (N=29; %) | 250 mg QD and 325 mg QD (N=13; %) | 400 mg QD–425 mg QD (N=19) | 300 mg QD (N=19; %) | Grade ⩾3 | All grades |
| Any TEAE | 28 (97%) | 13 (100%) | 19 (100%) | 19 (100%) | 40 (50%) | 79 (99%) |
| Grade ⩾3 ARQ 087-related AEs | 3 (10%) | 3 (23%) | 6 (32%) | 2 (11%) | 14 (18%) | 70 (88%) |
| TEAE leading to treatment interruption | 10 (34%) | 7 (54%) | 11 (58%) | 3 (16%) | 20 (25%) | 31 (39%) |
| TEAE leading to dose reduction | 0 | 2 (15%) | 3 (16%) | 1 (5%) | 1 (5%) | 6 (8%) |
| TEAE leading to treatment discontinuation | 1 (3%) | 0 | 5 (26%) | 2 (11%) | 3 (4%) | 8 (10%) |
| Any SAE | 9 (31%) | 2 (15%) | 6 (32%) | 3 (16%) | 20 (25%) | 20 (25%) |
| Fatigue | 18 (62%) | 8 (62%) | 11 (58%) | 9 (47%) | 5 (6%) | 46 (58%) |
| Nausea | 14 (48%) | 8 (62%) | 13 (68%) | 8 (42%) | 1 (1%) | 43 (54%) |
| Aspartate aminotransferase increased | 7 (24%) | 7 (54%) | 10 (53%) | 5 (26%) | 12 (15%) | 29 (36%) |
| Diarrhoea | 6 (21%) | 5 (38%) | 9 (47%) | 3 (16%) | 0 | 23 (29%) |
| Decreased appetite | 11 (38%) | 3 (23%) | 6 (32%) | 3 (16%) | 1 (1%) | 23 (029%) |
| Vomiting | 10 (34%) | 2 (15%) | 7 (37%) | 3 (16%) | 1 (1%) | 22 (28%) |
| Constipation | 5 (17%) | 4 (31%) | 7 (37%) | 4 (21%) | 0 | 20 (25%) |
| Dry mouth | 3 (10%) | 1 (8%) | 6 (32%) | 4 (21%) | 0 | 14 (18%) |
| Alanine aminotransferase increased | 2 (7%) | 3 (23%) | 4 (21%) | 5 (26%) | 3 (4%) | 14 (18%) |
| Anaemia | 7 (24%) | 3 (23%) | 0 | 2 (11%) | 2 (3%) | 12 (15%) |
| Blood creatinine increased | 4 (14%) | 1 (8%) | 4 (21%) | 2 (11%) | 0 | 11 (14%) |
| Hypoalbuminaemia | 6 (21%) | 4 (31%) | 1 (5%) | 0 | 1 (1%) | 11 (14%) |
| Blood alkaline phosphatase increased | 8 (28%) | 2 (15%) | 1 (5%) | 0 | 1 (1%) | 11 (14%) |
| Blood lactate dehydrogenase increased | 5 (17%) | 2 (15%) | 3 (16%) | 0 | 1 (1%) | 10 (13%) |
| Dry skin | 2 (7%) | 2 (15%) | 5 (26%) | 0 | 0 | 9 (11%) |
| Dysgeusia | 3 (10%) | 3 (23%) | 3 (16%) | 0 | 0 | 9 (11%) |
| Anxiety | 4 (14%) | 3 (23%) | 2 (11%) | 0 | 0 | 9 (11%) |
| Dizziness | 1 (3%) | 1 (8%) | 5 (26%) | 1 (5%) | 0 | 8 (10%) |
| Dyspepsia | 3 (10%) | 0 | 3 (16%) | 2 (11%) | 0 | 8 (10%) |
| Dyspnoea | 6 (21%) | 0 | 2 (11%) | 0 | 3 (4%) | 8 (10%) |
Abbreviations: QD=daily; QOD=every other day; RP2D=recommended phase 2 dose; SAE=serious adverse event; TEAE=treatment-emergent adverse event.