Table 1. ADME properties for Pyronaridine tetraphosphate.
Pyronaridine | |
---|---|
ADME property | Data |
Solubility | 168 μM at pH 7.4 |
CYP inhibition | 1A2, 2C9, 2C19 (>50 μM), 3A4 (42.9 μM), 2D6 (2.23 μM) |
Mouse liver microsomes |
t1/2 = 173 min, CLint = 4 μL/min/mg protein |
Guinea Pig liver microsomes | t1/2 = 44.4 min, 15.6 μL /min/mg protein |
Non-Human primate liver microsomes | t1/2 = 140.1 min, 4.9 μL /min/mg protein |
Human liver microsomes | T1/2 = 169.7 min, 4.1 μL /min/mg protein |
Mouse plasma protein binding | 96.5% |
Human plasma protein binding | 95.1% |
Caco-2 | Papp A-B = 6.46; B-A = 4.8 (x10-6 cm/s) Efflux ratio = 0.74 |
CYP3A4 Induction | 1.5x at 10 μM |