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. 2018 Jan 25;62(2):e01711-17. doi: 10.1128/AAC.01711-17

TABLE 1.

In vitro ADME properties for tilorone

ADME property Value(s)
Solubility 465 μM at pH 7.4
Cytochrome P450 inhibition CYPs 1A2, 2C9, 2C19, 3A4, 2D6 (IC50 >50 μM)
Mouse liver microsome properties t1/2, 47.8 min; CLint, 14.5 μl/min/mg protein
Mouse plasma protein binding 61.4%
Mouse plasma stability (at 5 h) 95.2%
Human plasma protein binding 52%
Human plasma stability (at 5 h) 94.8%
Caco-2 permeability Papp A-B, 20.4 × 10−6 cm/s; Papp B-A, 8.87 × 10−6 cm/s; efflux ratio, 0.435