Pharmacokinetic parameters of YM-64227 metabolites after a single oral administration of YM-64227
Each value represents the mean ± S.D.
Genotype | Analyte | Tmax | Cmax | AUCoral | T1/2 |
|---|---|---|---|---|---|
| h | ng/ml | h · ng/ml | h | ||
| C/C homo (n = 5) | MM-1 | 0.5 ± 0.0 | 12.4 ± 5.5 | 17.3 ± 10.1 | 0.6 ± 0.1 |
| MM-2 | 0.5 ± 0.0 | 73.2 ± 23.8 | 111.8 ± 33.1 | 0.8 ± 0.3 | |
| MM-3 | 0.4 ± 0.1 | 4.1 ± 2.1 | 3.2 ± 1.4 | 0.4 ± 0.0 | |
| MM-4 | 0.4 ± 0.1 | 4.3 ± 2.2 | 3.1 ± 1.5 | 0.3 ± 0.1a | |
| MM-5 | 0.4 ± 0.1 | 4.2 ± 2.6 | 3.1 ± 1.8 | 0.3 ± 0.0a | |
| C/T hetero (n = 5) | MM-1 | 0.6 ± 0.2 | 14.9 ± 6.8 | 23.4 ± 13.2 | 0.6 ± 0.1 |
| MM-2 | 0.6 ± 0.2 | 108.9 ± 54.5 | 186.7 ± 106.3 | 0.7 ± 0.1 | |
| MM-3 | 0.4 ± 0.1 | 8.6 ± 5.9 | 6.9 ± 4.4 | 0.3 ± 0.0 | |
| MM-4 | 0.4 ± 0.1 | 5.6 ± 2.9 | 4.1 ± 2.2 | 0.3 ± 0.1b | |
| MM-5 | 0.4 ± 0.1 | 10.9 ± 7.5 | 8.5 ± 5.5 | 0.3 ± 0.1a | |
| T/T homo (n = 5) | MM-1 | 1.8 ± 0.4** | 42.0 ± 9.0** | 355.4 ± 83.3** | 4.6 ± 0.6** |
| MM-2 | 0.6 ± 0.2 | 6.1 ± 1.3* | 15.9 ± 5.9 | 1.3 ± 0.2** | |
| MM-3 | 0.3 ± 0.1 | 7.9 ± 5.1 | 6.1 ± 4.1 | 0.3 ± 0.0 | |
| MM-4 | 0.4 ± 0.1 | 27.5 ± 14.9** | 35.4 ± 19.8** | 0.6 ± 0.1** | |
|
| MM-5 | 0.7 ± 0.3* | 136.8 ± 48.1** | 366.3 ± 191.5** | 1.1 ± 0.1** |
Statistically significant differences from the C/C type were determined using the Tukey test and are indicated as * P < 0.05 and ** P < 0.01.
↵ a n = 4 and bn = 3 because of plasma concentrations being less than the lower limit of detection (0.4 ng/ml) at many blood collection time points.