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Table 6 Safety profile of FNDR-20123

From: Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria

  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
  1. Values are expressed as Mean ± SD