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. 2019 Nov 21;13(11):e0007890. doi: 10.1371/journal.pntd.0007890

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