Summary of treatment-related AEs overall and by dose level (any-grade frequency ≥10%, grade 3 frequency of ≥5%, and all grade 4/5)
| Characteristics | Overall (N=33) (%) | Dose level 1 (n=3) (%) | Dose level 2 (n=30) (%) | |||
| All grades | Grade ≥3 | All grades | Grade ≥3 | All grades | Grade ≥3 | |
| Patients with AEs | 33 (100) | 19 (58) | 3 (100) | 1 (33) | 30 (100) | 18 (60) |
| Types of treatment-related AEs | ||||||
| Proteinuria | 20 (61) | 6 (18) | 0 | 0 | 20 (67) | 6 (20) |
| Hypertension | 18 (55) | 12 (36) | 0 | 0 | 18 (60) | 12 (40) |
| Diarrhea | 13 (39) | 1 (3) | 1 (33) | 1 (33) | 12 (40) | 0 |
| Fatigue | 10 (30) | 0 | 1 (33) | 0 | 9 (30) | 0 |
| Hoarseness | 9 (27) | 0 | 1 (33) | 0 | 8 (27) | 0 |
| Increased AST | 8 (24) | 0 | 0 | 0 | 8 (27) | 0 |
| Maculopapular rash | 8 (24) | 0 | 0 | 0 | 8 (27) | 0 |
| Increased amylase | 7 (21) | 2 (6) | 0 | 0 | 7 (23) | 2 (7) |
| Arthralgia | 7 (21) | 0 | 0 | 0 | 7 (23) | 0 |
| Limb edema | 6 (18) | 0 | 0 | 0 | 6 (20) | 0 |
| Headache | 6 (18) | 0 | 0 | 0 | 6 (20) | 0 |
| Dry mouth | 5 (15) | 0 | 1 (33) | 0 | 4 (13) | 0 |
| Increased ALP | 5 (15) | 0 | 0 | 0 | 5 (17) | 0 |
| Increased ALC | 5 (15) | 2 (6) | 0 | 0 | 5 (17) | 2 (7) |
| Acneiform rash | 5 (15) | 0 | 0 | 0 | 5 (17) | 0 |
| Hypothyroidism | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Nausea | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Vomiting | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Increased ALT | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Increased lipase | 4 (12) | 1 (3) | 0 | 0 | 4 (13) | 1 (3) |
| Thrombocytopenia | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Weight Loss | 4 (12) | 0 | 1 (33) | 0 | 3 (10) | 0 |
| Anorexia | 4 (12) | 0 | 1 (33) | 0 | 3 (10) | 0 |
| Myalgia | 4 (12) | 0 | 1 (33) | 0 | 3 (10) | 0 |
| Dizziness | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Hematuria | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Cough | 4 (12) | 0 | 0 | 0 | 4 (13) | 0 |
| Pneumonitis | 4 (12) | 1 (3) | 0 | 0 | 4 (13) | 1 (3) |
| Pain | 3 (9) | 0 | 0 | 0 | 3 (10) | 0 |
| Dehydration | 3 (9) | 1 (3) | 0 | 0 | 3 (10) | 1 (3) |
| Hypophosphatemia | 3 (9) | 1 (3) | 0 | 0 | 3 (10) | 1 (3) |
| Dysgeusia | 3 (9) | 0 | 1 (33) | 0 | 2 (7) | 0 |
| Peripheral sensory neuropathy | 3 (9) | 0 | 1 (33) | 0 | 2 (7) | 0 |
| Dyspnea | 3 (9) | 0 | 0 | 0 | 3 (10) | 0 |
| Voice alteration | 3 (9) | 0 | 0 | 0 | 3 (10) | 0 |
| Pruritus | 3 (9) | 0 | 0 | 0 | 3 (10) | 0 |
| Adrenal insufficiency | 1 (3) | 1 (3) | 0 | 0 | 1 (3) | 1 (3) |
| Small bowel obstruction | 1 (3) | 1 (3) | 0 | 0 | 1 (3) | 1 (3) |
| Hypercalcemia | 1 (3) | 1 (3) | 0 | 0 | 1 (3) | 1 (3) |
| Abdominal pain | 1 (3) | 1 (3) | 0 | 0 | 1 (3) | 1 (3) |
| Hyponatremia | 1 (3) | 1 (3) | 0 | 0 | 1 (3) | 1 (3) |
| Colitis | 2 (6) | 2 (6) | 0 | 0 | 2 (7) | 2 (7) |
| Cardiac arrest* | 1 (3) | 1 (3) | 0 | 0 | 1 (3) | 1 (3) |
*There was one treatment-related death due to cardiac arrest in a patient with colorectal cancer receiving dose level 2.
AE, adverse event; ALC, absolute lymphocyte count; ALP, alkaline phosphatase; ALT, alanine aminotransferase; AST, aspartate aminotransferase.