Table 4.
Summary of AEs in clinical trials of fostamatinib
| Disease | RA | RA | RA | RA | |||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Phase | Phase II | Phase II | Phase II | Phase III | |||||||
| Trial number | NCT00326339 | NCT00665925 | NCT01569074 | NCT01197521 | |||||||
| Trial name | TASKI-1 | TASKI-2 | OSKIRA-ASIA-1 | OSKIRA-1 | |||||||
| Dosage | 50 mg BID | 100 mg BID | 150 mg BID | 150 mg QD | 100 mg BID | 50 mg BID | 75 mg BID | 100 mg BID 150 mg QD |
100 mg BID | 100 mg BID 150 mg QD |
100 mg BID |
| Patients (%) | 46 | 49 | 47 | 152 | 152 | 33 | 33 | 33 | 31 | 304 | 310 |
| Any AE | 80.0 | 40.8 | 48.0 | 72.7 | 63.6 | 69.7 | 74.2 | 71.1 | 66.8 | ||
| Severe AE | 3.5 | 3.3 | 0.7 | 9.1 | 0.0 | 3.0 | 3.2 | 4.9 | 2.9 | ||
| Hypertension | 0.0 | 6.1 | 4.3 | 11.8 | 13.8 | 9.1 | 18.2 | 18.2 | 29.0 | 15.1 | 15.8 |
| Neutropenia | 2.2 | 10.2 | 29.8 | 15.2 | 12.1 | 6.1 | 12.9 | ||||
| ALT increase | 4.3 | 6.1 | 8.5 | 4.6 | 5.3 | 0.0 | 0.0 | 0.0 | 0.0 | 3.9 | 3.5 |
| URTI | 6.5 | 0.0 | 0.0 | 2.0 | 6.6 | 0.0 | 3.0 | 6.1 | 9.7 | 5.3 | 3.5 |
| Diarrhea | 10.9 | 16.3 | 44.7 | 11.8 | 19.1 | 3.0 | 6.1 | 18.2 | 16.1 | 15.1 | 13.9 |
| Nausea | 4.3 | 14.3 | 14.9 | 5.9 | 4.6 | 0.0 | 0.0 | 0.0 | 3.2 | 8.9 | 6.9 |
| Gastritis | 2.2 | 4.1 | 14.9 | 3.0 | 0.0 | 3.0 | 9.7 | ||||
| Dyspepsia | 2.2 | 10.2 | 6.4 | 1.6 | 3.2 | ||||||
| Abdominal pain | 0.0 | 4.1 | 6.4 | 5.3 | 3.9 | ||||||
| Headache | 13.0 | 2.0 | 6.4 | 6.6 | 5.9 | 0.0 | 3.0 | 6.1 | 3.2 | 6.3 | 3.2 |
| Dizziness | 4.3 | 8.2 | 10.6 | 3.0 | 3.0 | 0.0 | 3.2 | ||||
| Fatigue | 6.5 | 6.1 | 0.0 | ||||||||
| Edema | 2.2 | 2.0 | 8.5 | ||||||||
| Rash | 6.5 | 8.2 | 4.3 | 1.3 | 2.0 | ||||||
| Disease | RA | RA | RA | ITP | ITP | DLBCL | B-cell NHL | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Phase | Phase III | Phase III | Phase IIb | Phase III | Phase III | Phase II | Phase II | |||||
| Trial number | NCT01197534 | NCT01197534 | NCT01264770 |
NCT02076399 NCT02076412 |
NCT02077192 | NCT01499303 | NCT00446095 | |||||
| Trial name | OSKIRA-2 | OSKIRA-3 | OSKIRA-4 | FIT1, FIT2 | FIT3 | – | – | |||||
| Dosage | 100 mg BID 150 mg QD |
100 mg BID | 100 mg BID 150 mg QD |
100 mg BID | 100 mg BID 100 mg QD |
100 mg BID 150 mg QD |
100 mg BID | 100 mg BID 150 mg BID |
100 mg BID 150 mg BID |
100 mg BID | 200 mg BID | 200 mg BID |
| Patients (%) | 298 | 308 | 108 | 105 | 48 | 48 | 54 | 102 | 146 | 21 | 47 | 68 |
| Any AE | 51.0 | 55.2 | 45.4 | 48.6 | 59.6 | 60.4 | 72.2 | 83.0 | 86.0 | 62.0 | 72.0 | |
| Severe AE | 8.4 | 9.7 | 6.5 | 6.7 | 7.0 | 2.1 | 9.3 | 16.0 | 23.3 | 48.0 | 53.0 | |
| Hypertension | 18.5 | 22.1 | 13.9 | 13.3 | 8.8 | 6.3 | 13.0 | 28.0 | 21.0 | 4.8 | 10.6 | 24.0 |
| Neutropenia | 0.0 | 0.0 | 5.6 | 6.0 | 6.0 | 19.0 | 8.5 | 31.0 | ||||
| ALT increase | 4.7 | 6.8 | 3.5 | 2.1 | 5.6 | 11.0 | 10.0 | 10.0 | ||||
| URTI | 9.7 | 12.0 | 1.9 | 5.7 | 1.8 | 4.2 | 1.9 | 11.0 | 10.0 | |||
| Diarrhea | 15.8 | 14.3 | 26.9 | 20.0 | 21.1 | 27.1 | 16.7 | 31.0 | 35.0 | 0.0 | 29.8 | 41.0 |
| Nausea | 4.2 | 6.5 | 6.5 | 3.8 | 4.2 | 3.7 | 19.0 | 19.0 | 14.3 | 21.3 | 21.0 | |
| Gastritis | 1.9 | 5.7 | ||||||||||
| Dyspepsia | 1.8 | 0.0 | 0.0 | |||||||||
| Abdominal pain | 4.0 | 6.2 | 6.0 | 6.0 | 7.0 | |||||||
| Headache | 8.3 | 7.6 | 13.0 | 16.0 | ||||||||
| Dizziness | 5.6 | 6.7 | 11.0 | 11.0 | 10.0 | |||||||
| Fatigue | 0.0 | 0.0 | 6.0 | 9.0 | 14.3 | 19.1 | 41.0 | |||||
| Edema | ||||||||||||
| Rash | 9.0 | 6.0 | ||||||||||
AE adverse events, ALT alanine aminotransferase, BID twice daily, DLBCL diffuse large B-cell lymphoma, ITP immune thrombocytopenia, NHL non-Hodgkin lymphoma, QD once daily, RA rheumatoid arthritis, URTI upper respiratory tract infection