Table 1.
Physicochemical properties and in vitro pharmacokinetic profiles of LMT-28
| Parameters | Values |
|---|---|
| LogP | 3.65±0.22 |
| Solubility in water (mg/mL) | 0.39±0.12 |
| Liver microsomal stability | |
| Half-life (t1/2, rat) (min) | 15.3±1.4 |
| Half-life (t1/2, human) (min) | 21.9±2.8 |
| In vitro intrinsic clearance | |
| CLint, in vitro (Rat, μL/min/mg protein) | 91±8.4 |
| CLint, in vitro (Human, μL/min/mg protein) | 64±8.1 |
| In vivo intrinsic clearance | |
| CLint, in vivo (Rat, mL/min/kg) | 164±15 |
| CLint, in vivo (Human, mL/min/kg) | 60±7.7 |
| MDCK cell permeability (Papp, ×10−6 cm/s) | 9.7±1.8 |
| Plasma protein binding (bound drug %) | 92.4±2.1 |
CLint, in vitro, in vitro intrinsic clearance; CLint, in vivo, in vivo intrinsic clearance; MDCK, Madin-Darby canine kidney.