Most commonly reported all-grade (≥10% of patients overall) and grade ≥3 (≥2 patients) drug-related AEs
| AE, n (%) . | Dose-escalation cohorts (n = 32) . | Expansion cohorts (n = 31*) . | Total (N = 60) . | |||
|---|---|---|---|---|---|---|
| All grades . | Grade ≥3 . | All grades . | Grade ≥3 . | All grades . | Grade ≥3† . | |
| Any | 26 (81) | 13 (41) | 28 (90) | 22 (71) | 51 (85) | 32 (53) |
| Thrombocytopenia | 14 (44) | 9 (28) | 14 (45) | 12 (39) | 26 (43) | 20 (33) |
| Diarrhea | 11 (34) | 4 (13) | 14 (45) | 7 (23) | 23 (38) | 10 (17) |
| Nausea | 11 (34) | 3 (9) | 13 (42) | 1 (3) | 23 (38) | 4 (7) |
| Fatigue | 12 (38) | 2 (6) | 13 (42) | 4 (13) | 22 (37) | 5 (8) |
| Vomiting | 9 (28) | 2 (6) | 13 (42) | 1 (3) | 21 (35) | 3 (5) |
| Decreased appetite | 5 (16) | 0 | 11 (35) | 4 (13) | 15 (25) | 4 (7) |
| Neutropenia | 4 (13) | 4 (13) | 10 (32) | 8 (26) | 13 (22) | 11 (18) |
| Skin/SC tissue disorders‡ | 3 (9) | 1 (3)§ | 11 (35) | 1 (3)|| | 13 (22) | 2 (3) |
| PN NEC¶ | 3 (9) | 0 | 10 (32) | 1 (3) | 12 (20) | 1 (2) |
| Anemia | 3 (9) | 2 (6) | 7 (23) | 2 (6) | 9 (15) | 4 (7) |
| Dehydration | 3 (9) | 1 (3) | 5 (16) | 1 (3) | 7 (12) | 2 (3) |
| Lymphopenia | 3 (9) | 3 (9) | 5 (16) | 3 (10) | 7 (12) | 5 (8) |
| Leukopenia | 2 (6) | 1 (3) | 5 (16) | 3 (10) | 6 (10) | 3 (5) |
| Pyrexia | 1 (3) | 0 | 5 (16) | 0 | 6 (10) | 0 |
| AE, n (%) . | Dose-escalation cohorts (n = 32) . | Expansion cohorts (n = 31*) . | Total (N = 60) . | |||
|---|---|---|---|---|---|---|
| All grades . | Grade ≥3 . | All grades . | Grade ≥3 . | All grades . | Grade ≥3† . | |
| Any | 26 (81) | 13 (41) | 28 (90) | 22 (71) | 51 (85) | 32 (53) |
| Thrombocytopenia | 14 (44) | 9 (28) | 14 (45) | 12 (39) | 26 (43) | 20 (33) |
| Diarrhea | 11 (34) | 4 (13) | 14 (45) | 7 (23) | 23 (38) | 10 (17) |
| Nausea | 11 (34) | 3 (9) | 13 (42) | 1 (3) | 23 (38) | 4 (7) |
| Fatigue | 12 (38) | 2 (6) | 13 (42) | 4 (13) | 22 (37) | 5 (8) |
| Vomiting | 9 (28) | 2 (6) | 13 (42) | 1 (3) | 21 (35) | 3 (5) |
| Decreased appetite | 5 (16) | 0 | 11 (35) | 4 (13) | 15 (25) | 4 (7) |
| Neutropenia | 4 (13) | 4 (13) | 10 (32) | 8 (26) | 13 (22) | 11 (18) |
| Skin/SC tissue disorders‡ | 3 (9) | 1 (3)§ | 11 (35) | 1 (3)|| | 13 (22) | 2 (3) |
| PN NEC¶ | 3 (9) | 0 | 10 (32) | 1 (3) | 12 (20) | 1 (2) |
| Anemia | 3 (9) | 2 (6) | 7 (23) | 2 (6) | 9 (15) | 4 (7) |
| Dehydration | 3 (9) | 1 (3) | 5 (16) | 1 (3) | 7 (12) | 2 (3) |
| Lymphopenia | 3 (9) | 3 (9) | 5 (16) | 3 (10) | 7 (12) | 5 (8) |
| Leukopenia | 2 (6) | 1 (3) | 5 (16) | 3 (10) | 6 (10) | 3 (5) |
| Pyrexia | 1 (3) | 0 | 5 (16) | 0 | 6 (10) | 0 |
PN NEC, peripheral neuropathy not elsewhere classified; SC, subcutaneous.
Includes 3 patients from the MTD dose-escalation cohort.
In addition, the following drug-related grade ≥3 AEs were reported in 1 patient each: hypocalcemia, hyperuricemia, hyponatremia, decreased platelet count, increased blood creatinine, decreased white blood cell count, dizziness, erythema multiforme, rash papular, cardiac failure congestive, pneumonia, renal failure acute, and orthostatic hypotension.
Skin/SC tissue disorders cover all AEs within this MedDRA system organ class; overall rate includes rash macular (n = 3, 5%), hyperhidrosis, exfoliative rash (each n = 2, 3%), acute febrile neutrophilic dermatosis, alopecia, erythema multiforme, night sweats, petechiae, rash, rash erythematous, rash papular, skin exfoliation, and an event coded as Stevens–Johnson syndrome with a clinical diagnosis of erythema multiforme (each n = 1, 2%).
DLT of grade 3 erythema multiforme.
Grade 3 rash papular.
PN NEC (high-level MedDRA term, including the preferred terms of “neuropathy peripheral,” “peripheral sensory neuropathy,” and “peripheral motor neuropathy”).