Metabolic Stability

Metabolic stability influences both oral bioavailability and plasma half life of a compound, which in turn, affect its efficacy. XenoTech evaluates the metabolic stability of drug candidates in a variety of test systems (S9, microsomes and hepatocytes). Human liver microsomes and hepatocytes have been well established as the test system of choice to study cytochrome P450-dependent and conjugation of drugs, respectively.

Our contract service assesses the stability of the compound relating to biotransformation by measuring the disappearance of parent compound in the selected test system.

• LC/MS method development for analysis of test article 
• Incubations in suitable test system (S9, microsomes, hepatocytes, rCYP enzymes) with appropriate cofactors and measured at multiple time-points in triplicate, with additional replicates for critical samples
• Comparisons of time and cofactor blanks
• Incubations of marker substrates as positive controls to check for metabolic competency of the test system (positive controls quantified by formation of metabolites)
• Full data summary