Table 2.
TEAEs in safety population (n = 40).
| Preferred term | Dose-escalation | Dose-expansion | All (n = 40) | ||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 mg/kg (n = 1) | 3 mg/kg (n = 6) | 10 mg/kg (n = 6) | 20 mg/kg (n = 3) | 30 mg/kg (n = 6) | 1200 mg (n = 18) | All grades | Grade ⩾3 | All grades | Grade ⩾3 | All grades | Grade ⩾3 | All grades | Grade ⩾3 | All grades | Grade ⩾3 | All grades | Grade ⩾3 | All grades | Grade ⩾3 | ||||||||||
| TEAE | 1 (100) | 1 (100) | 6 (100) | 3 (50.00) | 6 (100) | 1(16.67) | 3 (100) | 3 (100) | 6 (100) | 3 (50.00) | 18 (100) | 7 (38.39) | 40 (100) | 18 (45.00) | |||||||||||||||
| Treatment-related TEAE | 1 (100) | 1 (100) | 6 (100) | 2 (33.33) | 6 (100) | 0 | 3 (100) | 3 (100) | 6 (100) | 2 (33.33) | 16 (88.89) | 3 (16.67) | 38 (95.00) | 11 (27.50) | |||||||||||||||
| SAE | 1 (100) | 0 | 2 (33.33) | 0 | 1 (16.67) | 0 | 2 (66.67) | 0 | 1 (16.67) | 0 | 4 (22.22) | 0 | 11 (27.50) | 0 | |||||||||||||||
| Treatment-related SAE | 1 (100) | 0 | 2 (33.33) | 0 | 0 | 0 | 2 (66.67) | 0 | 1 (16.67) | 0 | 0 | 0 | 6 (15.00) | 0 | |||||||||||||||
| AESI | 1 (100) | 0 | 6 (100) | 3 (50.00) | 6 (100) | 1 (16.67) | 3 (100) | 2 (66.67) | 6 (100) | 2 (33.33) | 18 (100) | 2 (11.11) | 40 (100) | 10 (25.00) | |||||||||||||||
| Treatment-related AESI | 1 (100) | 0 | 5 (83.30) | 1 (16.67) | 6 (100) | 0 | 3 (100) | 2 (66.67) | 4 (66.67) | 1 (16.67) | 10 (55.56) | 0 | 29 (72.50) | 4 (10.00) | |||||||||||||||
| Treatment-related TEAEs (⩾10% incidence) | Creatinine increased | 1 (100) | 0 | 1 (16.67) | 0 | 1 (16.67) | 0 | 1 (33.33) | 0 | 1 (16.67) | 0 | 2 (11.11) | 0 | 7 (17.50) | 0 | ||||||||||||||
| Serum amylase increased | 0 | 0 | 3 (50.00) | 1(16.67) | 0 | 0 | 1 (33.33) | 1 (33.33) | 0 | 0 | 3 (16.67) | 1 (5.56) | 7 (17.50) | 3 (7.50) | |||||||||||||||
| AST increased | 0 | 0 | 3 (50.00) | 1(16.67) | 3 (50.00) | 0 | 1 (33.33) | 1 (33.33) | 1 (16.67) | 0 | 4 (22.22) | 0 | 12 (30.00) | 2 (5.00) | |||||||||||||||
| γ-Glutamyltransferase increased | 1 (100) | 0 | 3 (50.00) | 0 | 2 (33.33) | 0 | 1 (33.33) | 1 (33.33) | 0 | 0 | 2 (11.11) | 0 | 9 (22.50) | 1 (2.50) | |||||||||||||||
| Thyroid-stimulating hormone increased | 0 | 0 | 3 (50.00) | 0 | 3 (50.00) | 0 | 0 | 0 | 1 (16.67) | 0 | 2 (11.11) | 0 | 9 (22.50) | 0 | |||||||||||||||
| Blood alkaline phosphatase increased | 1 (100) | 0 | 2 (33.33) | 0 | 0 | 0 | 1 (33.33) | 1 (33.33) | 0 | 0 | 2 (11.11) | 1 (5.56) | 6 (15.00) | 2 (5.00) | |||||||||||||||
| ALT increased | 0 | 0 | 2 (33.33) | 0 | 1 (16.67) | 0 | 1 (33.33) | 1 (33.33) | 0 | 0 | 4 (22.22) | 0 | 8 (20.00) | 1 (2.50) | |||||||||||||||
| Triiodothyronine decreased | 0 | 0 | 3 (50.00) | 0 | 3 (50.00) | 0 | 0 | 0 | 0 | 0 | 1 (5.56) | 0 | 7 (17.50) | 0 | |||||||||||||||
| Leukopenia | 0 | 0 | 1 (16.67) | 1 (16.67) | 0 | 0 | 1 (33.33) | 0 | 1 (16.67) | 1 (16.67) | 1 (5.56) | 0 | 4 (10.00) | 2 (5.00) | |||||||||||||||
| Serum amylase decreased | 0 | 0 | 1 (16.67) | 0 | 0 | 0 | 0 | 0 | 2 (33.33) | 0 | 2 (11.11) | 0 | 5 (12.50) | 0 | |||||||||||||||
| Free triiodothyronine decreased | 0 | 0 | 2 (33.33) | 0 | 3 (50.00) | 0 | 0 | 0 | 0 | 0 | 3 (16.67) | 0 | 8 (20.00) | 0 | |||||||||||||||
| Lipase increased | 0 | 0 | 0 | 0 | 1 (16.67) | 0 | 1 (33.33) | 1 (33.33) | 0 | 0 | 2 (11.11) | 2 (11.11) | 4 (10.00) | 3 (7.5) | |||||||||||||||
| Conjugated bilirubin increased | 0 | 0 | 1 (16.67) | 0 | 1 (16.67) | 0 | 1 (33.33) | 1 (33.33) | 1 (16.67) | 0 | 0 | 0 | 4 (10.00) | 1 (2.50) | |||||||||||||||
| Abnormal T wave on the ECG | 0 | 0 | 0 | 0 | 2 (33.33) | 0 | 2 (66.67) | 0 | 0 | 0 | 1 (5.56) | 0 | 5 (12.50) | 0 | |||||||||||||||
| Blood bilirubin increased | 0 | 0 | 1 (16.67) | 0 | 1 (16.67) | 0 | 1 (33.33) | 1 (33.33) | 2 (33.33) | 0 | 0 | 0 | 5 (12.50) | 1 (2.50) | |||||||||||||||
| Lipase decreased | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 2 (33.33) | 0 | 2 (11.11) | 0 | 4 (10.00) | 0 | |||||||||||||||
| Hyperuricemia | 1 (100) | 0 | 1 (16.67) | 0 | 2 (33.33) | 0 | 1 (33.33) | 0 | 1 (16.67) | 0 | 3 (16.67) | 0 | 9 (22.50) | 0 | |||||||||||||||
| Hypoalbuminemia | 1 (100) | 0 | 2 (33.33) | 0 | 0 | 0 | 1 (33.33) | 0 | 2 (33.33) | 0 | 0 | 0 | 6 (15.00) | 0 | |||||||||||||||
| Hyperglycemia | 0 | 0 | 1 (16.67) | 0 | 2 (33.33) | 0 | 1 (33.33) | 0 | 0 | 0 | 1 (5.56) | 0 | 5 (12.50) | 0 | |||||||||||||||
| Hyponatremia | 0 | 0 | 1 (16.67) | 1 (16.67) | 1 (16.67) | 0 | 1 (33.33) | 0 | 2 (33.33) | 0 | 0 | 0 | 5 (12.50) | 1 (2.50) | |||||||||||||||
| Hypochloremia | 1 (100) | 0 | 0 | 0 | 1 (16.67) | 0 | 0 | 0 | 2 (33.33) | 0 | 0 | 0 | 4 (10.00) | 0 | |||||||||||||||
| Proteinuria | 1 (100) | 0 | 1 (16.67) | 0 | 1 (16.67) | 0 | 1 (33.33) | 0 | 0 | 0 | 4 (22.22) | 0 | 8 (20.00) | 0 | |||||||||||||||
| Anemia | 1 (100) | 0 | 1 (16.67) | 1 (16.67) | 1 (16.67) | 0 | 1 (33.33) | 1 (33.33) | 3 (50.00) | 0 | 2 (11.11) | 0 | 9 (22.50) | 2 (5.00) | |||||||||||||||
| Arthralgia | 0 | 0 | 2 (33.33) | 0 | 1 (16.67) | 0 | 1 (33.33) | 0 | 0 | 0 | 1 (5.56) | 0 | 5 (12.50) | 0 | |||||||||||||||
| Pruritus | 0 | 0 | 1 (16.67) | 0 | 2 (33.33) | 0 | 1 (33.33) | 0 | 2 (33.33) | 0 | 0 | 0 | 6 (15.00) | 0 | |||||||||||||||
AESI, adverse events of special interest; ALT, alanine aminotransferase; AST, aspartate aminotransferase; ECG, electrocardiogram; SAE, serious adverse effects; TEAE, treatment-emergent adverse event.