Cytochrome P450 Inhibition Assay
Creative Animodel is a pioneer in the frontier of DMPK. With a team of experienced experts and professional technical platforms, we provide high-quality cytochromes P450 inhibition assay for our clients. Creative Animodel guarantees our clients the most efficient and reliable services to best meet their needs and facilitate developments of pharmaceutical products.
What Is Cytochrome P450 Inhibition Assay?
Cytochromes P450 (CYPs) are hemoproteins which constitute a superfamily containing heme as a cofactor. The human cytochrome P450 system is implicated in many drug interactions. Drugs can inhibit CYP450 enzymes, leading to clinically significant drug-drug interactions that can cause unanticipated adverse reactions or therapeutic failures. There are 3 different mechanisms of CYPs inhibition, including reversible inhibition, quasi-irreversible inhibition, as well as ireversible inhibition. Because human liver samples and recombinant human CYPs are now readily available, in vitro systems have been used as screening tools to predict the potential for in vivo drug interaction.
Why Choose Cytochrome P450 Inhibition Assay?
The CYPs play a key role in oxidative metabolism of drugs. In reality, drug interaction by mutual inhibition between drugs is almost inevitable, because many drugs are mainly eliminated through CYP-mediated metabolism. When conducting a drug discovery study, it is extremely essential to elucidate if a new chemical entity(NCE) acts as an inhibitor to CYPs that are mainly responsible for the metabolism of drugs in the body. Moreover, the data of in vitro cytochrome P450 inhibition is helpful for developing strategies about drug-drug interactions. Therefore, the draft FDA guidance for drug interaction studies and the EMA guideline recommend evaluating the CYP450 inhibition of a new investigational drug.
Figure 1. Comparison of Creative Animodel's IC50 values for the control inhibitors with literature values
Cytochrome P450 Inhibition Assay at Creative Animodel
• Using N-in-one or individual CYP assay. We provide services for individual enzymes as well as a cocktail approach to determine inhibition towards multiple enzymes in the same incubation.
• Using liver microsomes or recombinant CYP enzymes. Liver microsomes are recommended for these assays. From the systematic approach, human hepatocytes can be used to conduct the CYP inhibition in the cellular environment.
• Various substrate reaction and known specific positive control inhibitors are used for each of the isoform assays to obtain accurate and reliable data.
• State-of-the-art technical platforms. We utilize LC-MS/MS detection according to the recommendation.
Creative Animodel has years of experience in the area of in vitro ADME services. Moreover, we provide comprehensive solutions for the whole process of drug discovery and development. Based on expert teams and professional platforms, we are confident to provide our clients with high-quality and high-efficient services about cytochromes P450 inhibition assay.