Table 7. In Vitro ADME Profile of LAS191954.
| human PPB (% bound)a | PAMPA Papp (× 10–6 cm/s)b | plasma stability (24 h)c | CYP450 inhibitiond | CYP450 inductione |
|---|---|---|---|---|
| 95.4 | 2.8 | 100% | >25 μM | No issues |
a
Mean PPB values determined by equilibrium dialysis at a plasma concentration of 1 μM at 37 °C.
b
Permeability values at RT in PBS (containing 2% DMSO),; compound concentration in donor compartment: 20 μM.
c
LAS191954 stability at 37 °C at 2 μg/mL in plasma (anticoagulant: sodium heparin).
d
CYP450 in HLM with and without preincubation for CYP1A2, 3A4, 2D6, 2C9, and 2C19 isoforms.
e
Induction of CYP1A and 3A4 isoforms was assessed in cultured human cryopreserved hepatocytes at concentrations up to 50 μM.