The Methods for Bioanalysis and Drug Metabolism course is an interactive course focussing on the core principles of bioanalytical methods and the application to both drug bioanalysis and metabolite identification. The course includes both fundamental concepts and more in-depth bioanalytical application to support drug discovery and development, with a strong focus on small molecules but also with an introduction to these principles for large molecules.

The course starts by examining how the structure of a drug molecule influences its physicochemical properties and how these properties can be used to develop good extraction, separation and detection strategies. This provides a platform to learn in more detail the fundamental aspects of mass spectrometry, with a focus on modern techniques, together with HPLC theory and practice, with associated sample treatment and extraction procedures. Basic principles of chromatographic process with some practical tips and help with common problems, are also presented; including how to get the best from your HPLC system - focusing on resolution, efficiency and performance. Real world application is then explored in quantitative mass spectrometry, with the challenges of ion suppression a core topic. Optimisation of HPLC methods for LC/MS/MS, the effect of mobile phase on ionisation, and automated MS method development are also examined. This is integrated into strategies for method development, including initial considerations and experiments, chromatographic options, optimisation, validation and application of the final method. Quantitative bioanalysis is complemented with a series of lectures on qualitative methods, to support metabolite identification with detailed discussions on the use of MS/MS for structural elucidation (concepts, instrumentation and experimentation), accurate mass measurements, on-line radiochemical detection and integration with NMR spectroscopy. This section of the course also describes sample selection criteria and experiment types (in vivo, in vitro, in situ) for successful metabolite identification.

Several lectures are now devoted to the analysis of larger biopharmaceutical molecules, as a prelude to the DMDG “Large Molecule” training course. Introduction to this topic includes peptides, oligonucleotides and large intact proteins, comparing both LC/MS and ligand binding approaches.

Course content includes:

• Physicochemical Properties of Drugs

• Fundamental Aspects of Mass Spectrometry (MS) – focus on atmospheric pressure ionisation (API) techniques

• Sample Preparation & Retention Mechanisms – protein precipitation, liquid/liquid extraction and solid phase extraction

• HPLC & UHPLC Theory and Practice – reverse-phase, normal phase, ion-pair, ion-exchange, chiral HPLC and HILIC chromatography

• Quantitative Mass Spectrometry www.dmdg.org For more information contact info@dmdg.org October 2021

• An introduction to Biopharmaceutical Analysis

• Qualitative Mass Spectrometry (Metabolite Identification)

• Strategies for Bioanalytical Method Development

• Strategies for Metabolite Isolation

Intended audience:
This course is intended for DMPK scientists wanting to further develop their bioanalytical practice to support drug discovery and development. It is recommended that delegates have some industrial experience. Although the course is designed to develop bioanalytical understanding for DMPK applications, and is applicable to scientists entering this discipline, it is also suitable to other scientists within the wider DMPK field, medicinal chemistry, biology, pharmacology, toxicology, who may want to gain insight into how bioanalysis supports their project work.