Table 2. Pharmacokinetic Profile of ML352.
| MW | 387.2 | |
| cLogP | 3.37 | |
| TPSA | 76.8 |
| in vitro PK parameters | human | rat |
|---|---|---|
| CLint (mL/min/kg) | 10.4 | 95.0 |
| CLhep (mL/min/kg) | 6.9 | 40.3 |
| PPB (Fu) | 0.67 | 0.35 |
| PBS solubility | 98.2 ± 1.1 μM | |
| P450 1A2 | >30 μM | |
| P450 2C9 | >30 μM | |
| P450 2D6 | >30 μM | |
| P450 3A4 | >30 μM |
| in vitro PK parameters (Sprague–Dawley rats) | ||
|---|---|---|
| IV (1 mg/kg) | ||
| CL (mL/min/kg) | 107 | |
| t1/2 (min) | 33 | |
| Vss (L/kg) | 3.2 | |
| AUC | 150 | |
| PO (2.3 mg/kg) | ||
|---|---|---|
| Cmax (ng/mL) | 32.6 | |
| Tmax (h) | 0.25 | |
| AUC (ng h/mL) | 77.5 | |
| F (%) | 22 |
| tissue distribution (IV, 1 mg/kg, 0.25 h) | ||
|---|---|---|
| plasma (ng/mL) | 129 | |
| brain (ng/g) | 23.4 | |
| CSF (ng/g) | 11.8 | |
| Kp,brain | 0.2 | |