Metabolic Analysis of Benzodiazepines in Human and Mouse Liver Microsomes
Mentor 1
Dr. Arnold
Location
Union Wisconsin Room
Start Date
29-4-2016 1:30 PM
End Date
29-4-2016 3:30 PM
Description
Today, drug discovery programs commonly utilize in vitro pharmacokinetic studies to understand the many biochemical properties of lead drug candidates. For a drug to be metabolized through the body, it must contain highly specific pharmacokinetic properties. The determination of metabolic stability, reactivity, molecular interactions, and identification of drug compounds can be found through the study of cytochrome P450 monooxygenases. These enzymes play a key role in hepatic P450 enzyme metabolism, a mechanistic pathway found to clear approximately 60% of all marketed drugs.¹ The following data is a more in-depth explanation of the development of a LC/MS based microsomal stability study using pooled liver microsomes, and analysis on a Shimadzu 8040 instrument. Specific metabolic properties, such as half-life, internal clearance, and metabolic rate were determined for a variety of benzodiazepines, and were compared to industrial results.
Metabolic Analysis of Benzodiazepines in Human and Mouse Liver Microsomes
Union Wisconsin Room
Today, drug discovery programs commonly utilize in vitro pharmacokinetic studies to understand the many biochemical properties of lead drug candidates. For a drug to be metabolized through the body, it must contain highly specific pharmacokinetic properties. The determination of metabolic stability, reactivity, molecular interactions, and identification of drug compounds can be found through the study of cytochrome P450 monooxygenases. These enzymes play a key role in hepatic P450 enzyme metabolism, a mechanistic pathway found to clear approximately 60% of all marketed drugs.¹ The following data is a more in-depth explanation of the development of a LC/MS based microsomal stability study using pooled liver microsomes, and analysis on a Shimadzu 8040 instrument. Specific metabolic properties, such as half-life, internal clearance, and metabolic rate were determined for a variety of benzodiazepines, and were compared to industrial results.
