Short Course 1
Colloquium on LC-MS Method Development:
Fundamentals, New Technologies, and Advanced Methods

This practical course on HPLC method development for LC-MS is a tutorial on LC-MS/MS in the bioanalytical and clinical laboratory. As a conduit for learning, a major portion of the course will feature a step-wise method development approach and tutorial on how to develop LC-MS/MS methods based on compound structure. The course will emphasize the importance of HPLC when interfaced with mass spectrometry including the HPLC and SPE separation of undetected matrix components (a major cause for ion suppression!), isomers and labile metabolites. Much of the course is geared towards development of HPLC methods for LC-MS in a regulated quantitative bioanalysis laboratory for both pharmaceutical and clinical applications. Seven experts will present their recent experiences with fundamentals, new technologies and advanced methods. This colloquium will feature a dynamic format where the latest technology in HPLC column chemistries, tools for microsampling, MFLC, UPLC of large molecules and tools for gaining extra selectivity with HPLC-MS/MS are openly discussed. A significant time will be devoted to answering questions from the audience about their specific issues, needs and requirements.

Featured Presenters:

History and Applications of LC-MS Method Development
Shane Needham, Alturas Analytics

The Latest Column Materials, Formats, and Chemistries for LC-MS Applications in Clinical and Pharmaceutical Laboratories
Matt Przybyciel, ES Industries

MLFC Applications and Advantages in Pharmaceutical and Clinical Applications
Subodh Nimkar, Eksigent

Tools for Achieving Microsampling Accuracy in DMS Applications
Joe Siple, Drummond Scientific

Adding a 4th Dimension to LC-MS/MS: Differential Mobility
Yves Leblanc, AB SCIEX

Justification and Use of LC-MS and Bioanalytical Technologies by Management
Jim Shen, Bristol-Myers Squibb

Short Course Chair:
Shane Needham, Alturas Analytics

Short Course 2
Targeted Metabolomics: The Art & Science of Measuring Drug Efficacy

Efforts in translational and diagnostic medicine frequently require quantitative measurement of small endogenous molecules to access the need for and/or efficacy of treatment. These measurements often start to be employed in early disease biology research for proof of concept purposes and some ultimately evolve into tools to provide data for routine physician decision making. More recently, great interest has risen in the use chromatographic separations with a variety of detectors (particularly mass spectrometry) to make these measurements and expand the range of molecules that can be measured. These measurements are increasingly being employed across the need space from basic biology to patients and the business of making these measurements is rapidly growing.

In this course, chromatographic separation and measurement with most of the common detectors will be described as applied the full range of need space (research to patient). While a variety of separation and detection approaches will be discussed, there will be a particular focus on liquid chromatography and mass spectrometry (LC/MS). The emphasis will be on the lab work including achieving the needed separation and sensitivity in the measurement as well as streamlining speed and efficiency of methods and overall lab operations. An open and interactive environment will be encouraged so all participants learn more about what works well and how to be effective.

Instructors:
Mark Hayward, Revlon
Ken Lewis, OpAns

Short Course 3
Analysis of Peptides and Proteins: Sample Preparation to Identification and Quantitation

This year's CPSA program highlights a key trend within the pharmaceutical industry: The rapidly growing demand for the quantitative analysis of proteins and peptides by LC-MS/MS. From the opening plenary lecture on Tuesday morning, the Wednesday biologics session, through to the Thursday biomarkers session, this short course will help conference participants deeply appreciate specific challenges associated with highly successful outcomes in LC-MS based protein analysis. In line with these sessions at the conference program, this preprogram short course will provide an indepth view of the practical aspects involved in protein/peptide analysis by LC-MS/MS.

The use of nanospray enabled MS has developed from a qualitative tool for (global) proteomics to a quantitative method suitable for peptide/protein biomarker validation. Key to success has been the combination of highly specific sample preparation methods, high sensitivity nanospray ionization, and high performance tandem mass spectrometry. Critical parameters involved in robust sample preparation, nanobore LC and nanospray, sensitive & selective MS detection along with their analytical benefits will be emphasized. The transition of the traditionally qualitative nLC-MS/MS technology to those suitable for absolute quantification will be discussed. Real world examples from the literature will be presented. The target audience includes analysts that have been engaged in qualitative proteomics wishing to transition to quantitative methods or analysts that have specialized in small molecule quantification wishing to transition to peptide/protein quantification.

Instructors:
Nalini Sadagopan, Agilent Technologies
Gary Valaskovic, New Objective
Nathan Yates, University of Pittsburgh

Short Course 4
Assessment of Oral Bioavailability in Preclinical Species and Human: Impact of Physicochemical, Biopharmaceutical and Physiological Factor

Poor oral bioavailability is one of the leading causes of compound failure in preclinical and clinical development. Compounds with poor oral bioavailability and short half life tend to have large dose and higher inter and intra-individual variability, which would limit their therapeutic usefulness and increase the cost of their developments. Poor oral bioavailability in preclinical species does not necessarily translate into poor human oral bioavailability and vice versa. This practical/hands on course is specifically designed for personnel in the pharmaceutical and biotechnology industries and contract research organizations (CROs), who need to understand:

• General principles of pharmacokinetics
• The parameters that determine oral bioavailability in human
• Approaches to optimize physicochemical and biopharmaceutical parameters that
• influence drug solubility, permeability, and metabolism, where applicable
• Anatomical and physiological factors that lead to species differences in oral
• bioavailability
• The state-of-the-art in vitro and in vivo ADME assays, and how pharmacokinetics, and drug metabolism and transporter research studies are conducted to select the candidates to advance in preclinical and clinical development
• The utility of validated physiologically based pharmacokinetics (PBPK) modeling during discovery and development of drug candidates
• The use of Biopharmaceutics Drug Disposition Classification System (BDDCS) in predicting drug disposition, drug-drug interaction, and impact of food on the pharmacokinetic profile of new chemical entities (NCEs)
• The workshop will also include a hands-on session that aims at improving your ability to apply these strategies to medicinal chemistry for hit selection, lead optimization, and development candidate selection

Instructor:
Ayman El-Kattan, Pfizer