Table 2.
Pharmacokinetic assessment of AZD3293.
| Property | Model name | Predicted value |
|---|---|---|
| Absorption | Water solubility | −4.956 (log mol/L) |
| Intestinal absorption (human) | 96.901 (% Absorbed) | |
| Skin Permeability | −2.902 (log Kp) | |
| P-glycoprotein substrate | Yes | |
| P-glycoprotein I inhibitor | Yes | |
| P-glycoprotein II inhibitor | Yes | |
| Distribution | VDss (human) | 0.772 (log L/kg) |
| Fraction unbound (human) | 0.057 (Fu) | |
| BBB permeability | −0.164 (log BB) | |
| CNS permeability | −1.72 (log PS) | |
| Metabolism | CYP2D6 substrate | No |
| CYP3A4 substrate | Yes | |
| CYP1A2 inhibitior | No | |
| CYP2C19 inhibitior | Yes | |
| CYP2C9 inhibitior | Yes | |
| CYP2D6 inhibitior | No | |
| CYP3A4 inhibitior | Yes | |
| Excretion | Total Clearance | 0.469 (log ml) |
| Renal OCT2 substrate | Yes | |
| Toxicity | AMES toxicity | No |
| Max. tolerated dose (human) | −0.497 (log mg) | |
| hERG I inhibitor | No | |
| hERG II inhibitor | Yes | |
| Oral Rat Acute Toxicity (LD50) | 2.864 (mol/kg) | |
| Oral Rat Chronic Toxicity | 1.06 (log mg/kg) | |
| Hepatotoxicity | Yes | |
| Skin Sensitisation | No | |
| T. Pyriformis toxicity | 0.727 (log ug/L) | |
| Minnow toxicity | 0.045 (log mM) |