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Updated: Aug 2, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Lead optimization strategies as part of a drug metabolism environment
1Schering-Plough Research Institute, Department of Drug Metabolism and Pharmacokinetics, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. walter.korfmacher@spcorp.com
Abstract:
The rapid increase in the rate at which new chemical entities can be synthesized by medicinal chemists and tested in vitro for potency using high-throughput screening has provided opportunities for lead selection and optimization of thousands of compounds in major pharmaceutical companies. This opportunity coincides with the realization that drug metabolism input at the lead optimization stage is crucial for the development of compounds, with increased likelihood of success when tested in preclinical safety studies and in phase I trials. This has led to new discovery and optimization paradigms, in which drug metabolism is playing an important role.
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