Reaction Phenotyping

The members of the Cytochrome P450 (CYP) superfamily are considered the most important drug metabolizing enzymes. A detailed understanding of the contribution of individual CYPs towards the clearance of a drug candidate is important for two reasons:

• To predict and understand potential drug-drug interactions.
• Some CYP isoforms, e.g. CYP2D6, CYP2C9, CYP2C19, are known to be polymorphic, leading to significant inter-individual variability in the rate of metabolism, which can alter drug exposure significantly and, as a consequence, have serious effects on drug efficacy and safety.

Bactosomes are a patented, highly efficient and cost effective source of recombinant CYPs and other drug metabolizing enzymes. Bactosomes contain recombinant CYP isoenzymes combined with CYP reductase leading to higher specific activity as compared to liver microsomes. As many as 18 human CYPs plus a variety of CYPs from pre-clinical species along with other drug-metabolizing enzymes are currently commercially available.

If you require other CYP isoforms/substrates or other drug metabolizing enzymes such as:

• sulfotransferases
• glutathione S-transferases
• aldehyde oxidase
• aldehyde dehydrogenase
• carboxylesterase
• UDP-glucuronosyltransferases

we can provide detailed reaction phenotyping for your drug candidate(s) using either Bactosomes or liver microsomes in combination with specific chemical inhibitors.

For further details or a quote, contact us.