Carboxylesterases in Drug Metabolism: Challenges and Opportunities
Room: 155E
Speaker: Brian Ogilvie, PhD, VP of Scientific Consulting
Abstract: Carboxylesterases (CES) represent an important pathway of drug metabolism. However, the striking differences in terms of number of carboxylesterases and tissue distribution make interspecies extrapolation a challenge. Several factors affect biotransformation and efficacy of drugs that are metabolized by CES. CES-mediated clinical drug-drug interactions (DDI) should also be evaluated. The regulatory guidance recommends examining CES-mediated metabolism for drugs that do not undergo significant metabolism by CYP enzymes.
The presentation is a high-level overview of in vitro DDI and ADME studies required for drug development with a focus on study design and data interpretation, as well as red flags to look for in in vitro DDI study reports, including methods and conclusions drawn from the underlying data.