Table 2.

Toxicity

EKB-569 dose level
10 mg (n = 4)25 mg (n = 22), n (%)35 mg (n = 7)50 mg (mod)* (n = 4)50 mg (n = 7)75 mg (n = 3)Total (n = 47), n (%)
Number of DLTs (first 28 d)0012126
All grade toxicity
All adverse events, n (%)4 (100)22 (100)7 (100)4 (100)7 (100)3 (100)47 (100)
Diarrhea419 (86)747344 (94)
Asthenia320 (91)436238 (81)
Nausea417 (77)425133 (70)
Neutropenia211 (50)423224 (51)
Vomiting29 (41)224120 (43)
Anorexia210 (45)313120 (43)
Alopecia49 (41)211219 (40)
Stomatitis/mucositis47 (32)214119 (40)
Rash16 (27)234218 (38)
Abdominal pain17 (32)221215 (32)
Anemia06 (27)111110 (21)
Grade ≥3 toxicity
All grade ≥3 adverse events, n (%)3 (75)20 (91)6 (86)3 (75)4 (57)3 (100)39 (83)
Diarrhea04 (18)223314 (30)
Neutropenia15 (23)202010 (21)
Asthenia05 (23)11108 (17)
Hypertension02 (9)10104 (9)
Deep vein thrombosis02 (9)10104 (9)
Pulmonary embolism02 (9)10003 (6)
Hyperglycemia02 (9)00103 (6)
Nausea02 (9)00103 (6)
Infection01 (5)00012 (4)
Anemia02 (9)00002 (4)
  • * Modified FOLFIRI: 300 mg/m2 5-FU bolus instead of 400 mg/m2; 2,000 mg/m2 5-FU infusion instead of 2,400 mg/m2.

  • Regardless of causality, occurring in ≥20% of patients.

  • Occurring in >2.5% of patients.