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 levelPatients (n = 39)DLTs in first cycleDose reductions (any cycle)Number of treatment days
NumberDescriptionNumberMedian (range)
0.025 mg30235 (35–98)
0.05 mg30299 (34–205)
0.10 mg302119 (65–253)
0.20 mg302281 (35–427)
0.40 mg301226 (97–268)
0.60 mg604185 (58–289)
0.90 mg61Grade 3 TCP5261 (30–1114)
1.00 mg605214 (84–960)
1.10 mg6a2Grade 3–4 TCP460 (14–196)
Adverse eventAll 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)
 Anemia25 (35)16 (23)
 TCP15 (21)13 (18)
 Neutropenia11 (15)7 (10)
Gastrointestinal disorders, n (%)27 (38)
 Nausea23 (32)
General disorders and administration site conditions, n (%)27 (38)2 (3)
 Fatigue26 (37)2 (3)
Skin and subcutaneous tissue disorders, n (%)19 (27)
 Alopecia14 (20)
  • Abbreviation: TCP, thrombocytopenia.

  • aOne patient discontinued from the trial on study day 21 for progressive disease, having received only 8 days of continuous dosing.