CYP Inhibition Studies Using Human Liver Microsomes

CYP Inhibition Studies Using Human Liver Microsomes 

Each drug (at least in five concentration which covers two orders of magnitude) is incubated with human liver microsomes in the presence of the marker substrate. Reactions are initiated with addition of NADPH 

CYP Substrate preferred acceptable Inhibitor preferred acceptable 

1A2 Ethoxyresorufin, Phenacetin Caffeine (low turnover), Theophylline (low turnover), Acetanilide (mostly applied in hepatocytes) Furafylline a-Naphthoflavone (but also inhibits 3A4) 

2B6 S-Mephenytoin (N-desmethyl metabolite) Bupropion Sertraline (but also inhibits 2D6) 

---

II.K.3 CYP Inhibition Studies Using Human Liver Microsomes 554... 

---