Pharmacokinetic parameters of the disposition of staphylokinase-related antigen from plasma after bolus injection of PEGylated SakSTAR variants (100 μg/kg) in hamsters
| Compound . | C0 (μg/mL) . | A (μg/mL) . | B (μg/mL) . | t1/2 (α) (min) . | t1/2 (β) (min) . | VC (mL) . | AUC (μg · min · mL−1) . | Clp (mL · min−1) . |
|---|---|---|---|---|---|---|---|---|
| SakSTAR | 0.8 ± 0.1 | 0.6 ± 0.1 | 0.2 ± 0.0 | 2.8 | 7.0 | 13 ± 1.0 | 4.6 ± 0.4 | 2.2 ± 0.2 |
| SakSTAR(K96C-SP5) | 0.8 ± 0.0 | 0.6 ± 0.0 | 0.3 ± 0.0 | 4.4 | 16 | 12 ± 0.5 | 9.3 ± 0.4 | 1.1 ± 0.1 |
| SakSTAR(K102C-SP5) | 1.8 ± 0.2 | 1.3 ± 0.1 | 0.5 ± 0.0 | 4.4 | 25 | 5.8 ± 0.4 | 27 ± 2.2 | 0.4 ± 0.0 |
| SakSTAR(K109C-SP5) | 1.0 ± 0.1 | 0.6 ± 0.1 | 0.4 ± 0.0 | 5.6 | 21 | 11 ± 1.0 | 17 ± 1.6 | 0.6 ± 0.1 |
| SakSTAR(K135C-SP5) | 1.2 ± 0.1 | 0.8 ± 0.1 | 0.4 ± 0.0 | 4.8 | 18 | 8.7 ± 0.6 | 15 ± 1.0 | 0.7 ± 0.1 |
| SakSTAR(K96C-SP5, K135C-SP5) | 3.3 ± 0.4 | 2.6 ± 0.3 | 0.7 ± 0.1 | 8.4 | 90 | 3.1 ± 0.3 | 130 ± 15 | 0.1 ± 0.0 |
| SakSTAR(S3C-SP5) | 1.7 ± 0.1 | 1.3 ± 0.1 | 0.4 ± 0.0 | 4.0 | 32 | 5.9 ± 0.5 | 26 ± 1.9 | 0.4 ± 0.0 |
| SakSTAR(2SC-SP5, S3C-SP5) | 1.3 ± 0.1 | 0.5 ± 0.1 | 0.8 ± 0.1 | 7.0 | 36 | 7.9 ± 0.8 | 46 ± 4.0 | 0.2 ± 0.0 |
| SakSTAR(S3C-MP5) | 1.2 ± 0.1 | 1.1 ± 0.1 | 0.1 ± 0.0 | 5.0 | 15 | 8.5 ± 0.6 | 11 ± 0.8 | 0.1 ± 0.1 |
| SakSTAR(S3C-MP10) | 1.7 ± 0.1 | 1.3 ± 0.1 | 0.4 ± 0.0 | 10 | 53 | 5.9 ± 0.3 | 51 ± 2.7 | 0.2 ± 0.0 |
| SakSTAR(S3C-MP20) | 1.9 ± 0.2 | 0.8 ± 0.1 | 1.2 ± 0.1 | 20 | 96 | 5.4 ± 0.6 | 180 ± 16 | 0.1 ± 0.0 |
| Compound . | C0 (μg/mL) . | A (μg/mL) . | B (μg/mL) . | t1/2 (α) (min) . | t1/2 (β) (min) . | VC (mL) . | AUC (μg · min · mL−1) . | Clp (mL · min−1) . |
|---|---|---|---|---|---|---|---|---|
| SakSTAR | 0.8 ± 0.1 | 0.6 ± 0.1 | 0.2 ± 0.0 | 2.8 | 7.0 | 13 ± 1.0 | 4.6 ± 0.4 | 2.2 ± 0.2 |
| SakSTAR(K96C-SP5) | 0.8 ± 0.0 | 0.6 ± 0.0 | 0.3 ± 0.0 | 4.4 | 16 | 12 ± 0.5 | 9.3 ± 0.4 | 1.1 ± 0.1 |
| SakSTAR(K102C-SP5) | 1.8 ± 0.2 | 1.3 ± 0.1 | 0.5 ± 0.0 | 4.4 | 25 | 5.8 ± 0.4 | 27 ± 2.2 | 0.4 ± 0.0 |
| SakSTAR(K109C-SP5) | 1.0 ± 0.1 | 0.6 ± 0.1 | 0.4 ± 0.0 | 5.6 | 21 | 11 ± 1.0 | 17 ± 1.6 | 0.6 ± 0.1 |
| SakSTAR(K135C-SP5) | 1.2 ± 0.1 | 0.8 ± 0.1 | 0.4 ± 0.0 | 4.8 | 18 | 8.7 ± 0.6 | 15 ± 1.0 | 0.7 ± 0.1 |
| SakSTAR(K96C-SP5, K135C-SP5) | 3.3 ± 0.4 | 2.6 ± 0.3 | 0.7 ± 0.1 | 8.4 | 90 | 3.1 ± 0.3 | 130 ± 15 | 0.1 ± 0.0 |
| SakSTAR(S3C-SP5) | 1.7 ± 0.1 | 1.3 ± 0.1 | 0.4 ± 0.0 | 4.0 | 32 | 5.9 ± 0.5 | 26 ± 1.9 | 0.4 ± 0.0 |
| SakSTAR(2SC-SP5, S3C-SP5) | 1.3 ± 0.1 | 0.5 ± 0.1 | 0.8 ± 0.1 | 7.0 | 36 | 7.9 ± 0.8 | 46 ± 4.0 | 0.2 ± 0.0 |
| SakSTAR(S3C-MP5) | 1.2 ± 0.1 | 1.1 ± 0.1 | 0.1 ± 0.0 | 5.0 | 15 | 8.5 ± 0.6 | 11 ± 0.8 | 0.1 ± 0.1 |
| SakSTAR(S3C-MP10) | 1.7 ± 0.1 | 1.3 ± 0.1 | 0.4 ± 0.0 | 10 | 53 | 5.9 ± 0.3 | 51 ± 2.7 | 0.2 ± 0.0 |
| SakSTAR(S3C-MP20) | 1.9 ± 0.2 | 0.8 ± 0.1 | 1.2 ± 0.1 | 20 | 96 | 5.4 ± 0.6 | 180 ± 16 | 0.1 ± 0.0 |
Data are mean ± SEM of 4 experiments.