Table 2.
Part 1 dose escalation schema, DLTs, dose reductions, and common AEs (>15%) or grade 3 to 4 AEs (>4%) assessed by investigator as related at the recommended dose
| Dose level | Patients (n = 39) | DLTs in first cycle | Dose reductions (any cycle) | Number of treatment days | |
|---|---|---|---|---|---|
| Number | Description | Number | Median (range) | ||
| 0.025 mg | 3 | 0 | — | 2 | 35 (35-98) |
| 0.05 mg | 3 | 0 | — | 2 | 99 (34-205) |
| 0.10 mg | 3 | 0 | — | 2 | 119 (65-253) |
| 0.20 mg | 3 | 0 | — | 2 | 281 (35-427) |
| 0.40 mg | 3 | 0 | — | 1 | 226 (97-268) |
| 0.60 mg | 6 | 0 | — | 4 | 185 (58-289) |
| 0.90 mg | 6 | 1 | Grade 3 TCP | 5 | 261 (30-1114) |
| 1.00 mg | 6 | 0 | — | 5 | 214 (84-960) |
| 1.10 mg | 6a | 2 | Grade 3-4 TCP | 4 | 60 (14-196) |
| Adverse event | All grade (n = 71) | Grade 3-4 (n = 71) |
|---|---|---|
| Any treatment-emergent AE, n (%) | 55 (77) | 32 (45) |
|
| ||
| Blood and lymphatic system disorders,n (%) | 40 (56) | 30 (42) |
| Anemia | 25 (35) | 16 (23) |
| TCP | 15 (21) | 13 (18) |
| Neutropenia | 11 (15) | 7 (10) |
|
| ||
| Gastrointestinal disorders, n (%) | 27 (38) | — |
| Nausea | 23 (32) | — |
|
| ||
| General disorders and administration site conditions, n (%) | 27 (38) | 2 (3) |
| Fatigue | 26 (37) | 2 (3) |
|
| ||
| Skin and subcutaneous tissue disorders, n (%) | 19 (27) | — |
| Alopecia | 14 (20) | — |
Abbreviation: TCP, thrombocytopenia.
a
One patient discontinued from the trial on study day 21 for progressive disease, having received only 8 days of continuous dosing.