Pharmacokinetic summary for patients treated with KW-2449
| Dose level . | Daily dose, mg . | No. of patients . | KW-2449, 2 hours, nM . | M1, 2 hours, nM . | KW-2449, 12 hours, nM . | M1, 12 hours, nM . |
|---|---|---|---|---|---|---|
| 1 | 25 | 6 | 20.5 | 165.7 | 1.2 | 76.1 |
| 2 | 50 | 7 | 24.5 | 204.4 | 2.5 | 68.6 |
| 3 | 100 | 9 | 74.1 | 693 | 7.1 | 241.4 |
| 4 | 200 | 3 | 111.3 | 593.2 | 12.6 | 290.3 |
| 5 | 300 | 3 | 264 | 1865 | 17.6 | 413.8 |
| 6 | 400 | 3 | 387.2 | 2130 | 21.1 | 491.7 |
| 7 | 500 | 5 | 515.0 | 2867 | 102.5 | 420.3 |
| Dose level . | Daily dose, mg . | No. of patients . | KW-2449, 2 hours, nM . | M1, 2 hours, nM . | KW-2449, 12 hours, nM . | M1, 12 hours, nM . |
|---|---|---|---|---|---|---|
| 1 | 25 | 6 | 20.5 | 165.7 | 1.2 | 76.1 |
| 2 | 50 | 7 | 24.5 | 204.4 | 2.5 | 68.6 |
| 3 | 100 | 9 | 74.1 | 693 | 7.1 | 241.4 |
| 4 | 200 | 3 | 111.3 | 593.2 | 12.6 | 290.3 |
| 5 | 300 | 3 | 264 | 1865 | 17.6 | 413.8 |
| 6 | 400 | 3 | 387.2 | 2130 | 21.1 | 491.7 |
| 7 | 500 | 5 | 515.0 | 2867 | 102.5 | 420.3 |
Mean levels of KW-2449 and the metabolite, M1, are shown at 2 and 12 hours after dosing on day 1. The daily dose shown was administered in 2 divided doses, 12 hours apart (ie, 25 mg = 12.5 mg twice daily).