How Can We Help?
Skip to content
Researcher looking at a book

Inhibitory effect of typical CYP inhibitors under long term incubation in human liver microsomes

  • Published on October 5, 2018
  • Enzyme Inhibition
  • Test Systems & Methods
  • Scientific Posters

Presented at the 33rd JSSX Annual Meeting / 2018 MDO Meeting in Japan


Sho Nishinoaki, Ryo Fujino, Kenta Hashizume, Tsutomu Negama

Drug Development Solutions Center, Drug Development Solutions Division, SEKISUI Medical Co., Ltd. 2117 Muramatsu, Tokai, Ibaraki 319-1182, Japan


Cytochrome P450 (CYP) isoforms are responsible for the metabolism of the majority of drugs in Human. In case of the metabolic enzyme identification of CYP isoforms for the low intrinsic clearance (CLint) candidate compounds, it is necessary to perform metabolic reaction with long term incubation. In addition, when performing the metabolic enzyme identification with long term incubation, the specificity and sustainability of a typical inhibitor are important.

In this research, we evaluated the inhibitory effect of typical inhibitor for each CYP isoform in human liver microsomes (HLM) under long term incubation (incubation time of CYP typical inhibitors was 60 minutes, final concentration of HLM was 1 mg protein/mL) to clarify an optimal concentration of the CYP typical inhibitors under long term incubation. In this presentation, we have confirmed specificity and sustainability of each typical inhibitor for CYP isoform under long term incubation in HLM.

Download Poster