Table 6 Safety profile of FNDR-20123

Plasma protein binding (% bound)

 Mouse/Rat/Dog/Monkey/Human

< 30.00/41.89/< 20.00/< 20.00/57.30

Microsomal stability (% remaining at 120 min)

 MLM/RLM/HLM (Test Conc. 10 µM)

76.15/74.56/85.31

Plasma stability

 Mouse/Rat/Dog/Human (% remaining at 240 min)

89.16/88.90/97.72/98.94

CYP inhibition (IC₅₀ µM)

 CYP 1A2

> 60

 CYP 2C9

> 60

 CYP 2C19

> 60

 CYP 2D6

28.00

 CYP 3A4

27.00

CYP induction (% induction relative to respective positive controls)

 CYP 1A2

2.8 ± 0.8

 CYP 2B6

0.0

 CYP 3A4

0.9 ± 1.5

Cytotoxicity

 HepG2 (% @ 100 µM)

12.6%

 THP-1 (IC₅₀ µM)

113.6 µM

hERG binding

 IC₅₀ in µM

> 100 µM