| . | Dose escalation (n = 40) . | Dose expansion (12 mg, n = 8) . | Total (n = 48) . | |||
|---|---|---|---|---|---|---|
| Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | |
| Study drug-related TEAE | 33 (82.5) | 16 (40.0) | 8 (100) | 5 (62.5) | 41 (85.4) | 21 (43.8) |
| Study drug-related serious TEAE | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Common study drug-related TEAEa | ||||||
| Hypertension | 19 (47.5) | 9 (22.5) | 5 (62.5) | 4 (50.0) | 24 (50.0) | 13 (27.1) |
| Diarrhea | 15 (37.5) | 1 (2.5) | 1 (12.5) | 0 | 16 (33.3) | 1 (2.1) |
| Palmar-plantar erythrodysesthesia syndrome | 10 (25.0) | 1 (2.5) | 4 (50.0) | 0 | 14 (29.2) | 1 (2.1) |
| Stomatitis | 9 (22.5) | 2 (5.0) | 5 (62.5) | 0 | 14 (29.2) | 2 (4.2) |
| Nausea | 11 (27.5) | 1 (2.5) | 0 | 0 | 11 (22.9) | 1 (2.1) |
| Vomiting | 10 (25.0) | 0 | 0 | 0 | 10 (20.8) | 0 |
| Decreased appetite | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Blood thyroid-stimulating hormone increased | 4 (10.0) | 0 | 3 (37.5) | 0 | 7 (14.6) | 0 |
| Proteinuria | 6 (15.0) | 0 | 0 | 0 | 6 (12.5) | 0 |
| Alanine aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Aspartate aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Dry mouth | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
| Myalgia | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
| . | Dose escalation (n = 40) . | Dose expansion (12 mg, n = 8) . | Total (n = 48) . | |||
|---|---|---|---|---|---|---|
| Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | |
| Study drug-related TEAE | 33 (82.5) | 16 (40.0) | 8 (100) | 5 (62.5) | 41 (85.4) | 21 (43.8) |
| Study drug-related serious TEAE | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Common study drug-related TEAEa | ||||||
| Hypertension | 19 (47.5) | 9 (22.5) | 5 (62.5) | 4 (50.0) | 24 (50.0) | 13 (27.1) |
| Diarrhea | 15 (37.5) | 1 (2.5) | 1 (12.5) | 0 | 16 (33.3) | 1 (2.1) |
| Palmar-plantar erythrodysesthesia syndrome | 10 (25.0) | 1 (2.5) | 4 (50.0) | 0 | 14 (29.2) | 1 (2.1) |
| Stomatitis | 9 (22.5) | 2 (5.0) | 5 (62.5) | 0 | 14 (29.2) | 2 (4.2) |
| Nausea | 11 (27.5) | 1 (2.5) | 0 | 0 | 11 (22.9) | 1 (2.1) |
| Vomiting | 10 (25.0) | 0 | 0 | 0 | 10 (20.8) | 0 |
| Decreased appetite | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Blood thyroid-stimulating hormone increased | 4 (10.0) | 0 | 3 (37.5) | 0 | 7 (14.6) | 0 |
| Proteinuria | 6 (15.0) | 0 | 0 | 0 | 6 (12.5) | 0 |
| Alanine aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Aspartate aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Dry mouth | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
| Myalgia | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
Data are presented as No. (%).
Abbreviation: TEAE, treatment-emergent adverse event.
aDefined as any grade study drug-related TEAE occurring in ≥10% of the total study population. No grade 4 or 5 study drug-related TEAEs were reported.
| . | Dose escalation (n = 40) . | Dose expansion (12 mg, n = 8) . | Total (n = 48) . | |||
|---|---|---|---|---|---|---|
| Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | |
| Study drug-related TEAE | 33 (82.5) | 16 (40.0) | 8 (100) | 5 (62.5) | 41 (85.4) | 21 (43.8) |
| Study drug-related serious TEAE | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Common study drug-related TEAEa | ||||||
| Hypertension | 19 (47.5) | 9 (22.5) | 5 (62.5) | 4 (50.0) | 24 (50.0) | 13 (27.1) |
| Diarrhea | 15 (37.5) | 1 (2.5) | 1 (12.5) | 0 | 16 (33.3) | 1 (2.1) |
| Palmar-plantar erythrodysesthesia syndrome | 10 (25.0) | 1 (2.5) | 4 (50.0) | 0 | 14 (29.2) | 1 (2.1) |
| Stomatitis | 9 (22.5) | 2 (5.0) | 5 (62.5) | 0 | 14 (29.2) | 2 (4.2) |
| Nausea | 11 (27.5) | 1 (2.5) | 0 | 0 | 11 (22.9) | 1 (2.1) |
| Vomiting | 10 (25.0) | 0 | 0 | 0 | 10 (20.8) | 0 |
| Decreased appetite | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Blood thyroid-stimulating hormone increased | 4 (10.0) | 0 | 3 (37.5) | 0 | 7 (14.6) | 0 |
| Proteinuria | 6 (15.0) | 0 | 0 | 0 | 6 (12.5) | 0 |
| Alanine aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Aspartate aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Dry mouth | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
| Myalgia | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
| . | Dose escalation (n = 40) . | Dose expansion (12 mg, n = 8) . | Total (n = 48) . | |||
|---|---|---|---|---|---|---|
| Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | Any grade . | Grade ≥3 . | |
| Study drug-related TEAE | 33 (82.5) | 16 (40.0) | 8 (100) | 5 (62.5) | 41 (85.4) | 21 (43.8) |
| Study drug-related serious TEAE | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Common study drug-related TEAEa | ||||||
| Hypertension | 19 (47.5) | 9 (22.5) | 5 (62.5) | 4 (50.0) | 24 (50.0) | 13 (27.1) |
| Diarrhea | 15 (37.5) | 1 (2.5) | 1 (12.5) | 0 | 16 (33.3) | 1 (2.1) |
| Palmar-plantar erythrodysesthesia syndrome | 10 (25.0) | 1 (2.5) | 4 (50.0) | 0 | 14 (29.2) | 1 (2.1) |
| Stomatitis | 9 (22.5) | 2 (5.0) | 5 (62.5) | 0 | 14 (29.2) | 2 (4.2) |
| Nausea | 11 (27.5) | 1 (2.5) | 0 | 0 | 11 (22.9) | 1 (2.1) |
| Vomiting | 10 (25.0) | 0 | 0 | 0 | 10 (20.8) | 0 |
| Decreased appetite | 5 (12.5) | 0 | 2 (25.0) | 0 | 7 (14.6) | 0 |
| Blood thyroid-stimulating hormone increased | 4 (10.0) | 0 | 3 (37.5) | 0 | 7 (14.6) | 0 |
| Proteinuria | 6 (15.0) | 0 | 0 | 0 | 6 (12.5) | 0 |
| Alanine aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Aspartate aminotransferase increased | 4 (10.0) | 0 | 1 (12.5) | 0 | 5 (10.4) | 0 |
| Dry mouth | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
| Myalgia | 5 (12.5) | 0 | 0 | 0 | 5 (10.4) | 0 |
Data are presented as No. (%).
Abbreviation: TEAE, treatment-emergent adverse event.
aDefined as any grade study drug-related TEAE occurring in ≥10% of the total study population. No grade 4 or 5 study drug-related TEAEs were reported.
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