Table 3.
Pharmacokinetic evaluation in male C57BL mice using doses of DQ derivatives of 20 mg/kg (oral) (n = 3) and 5 mg/kg (IV) (n = 3) [17].
| Parameters | IV | Oral | ||||
|---|---|---|---|---|---|---|
| RMB041 | RMB043 | RMB073 | RMB041 | RMB43 | RMB073 | |
| AUC (min. µmol/L) |
29,250.4 ± 309.0 | 10,068.4 ± 127.8 | 15,940.0 ± 400 | 25,012.2 ± 108.0 | 8915.7 ± 1017.0 | 3771.0 ± 296.0 |
| Cmax (µM) | - | - | - | 5.4 ± 0.4 | 5.6 ± 1.4 | 2.0 ± 0.3 |
| t1/2 (h) | 62.3 ± 6.7 | 8.6 ± 0.4 | 15.3 ± 3.2 | 23.4 ± 2.5 | 6.2 ± 0.8 | 11.6 ± 1.3 |
| CL tot (mL/h/kg) | 23.1 ± 0.3 | 70.5 ± 4.2 | 34.5 ± 1.3 | - | - | - |
| Vd (L/kg) | 1.2 ± 0.03 | 4.6 ± 1.6 | 3.9 ± 0.5 | - | - | - |
| Bioavailability | - | - | - | 21.4 ± 1.0 | 22.1 ± 2.2 | 5.9 ± 1.3 |