Short Courses

Monday, October 27
Bucks county Sheraton Hotel
Langhorne, PA

• Method Development for LC/MS: Traditional Approaches and Emerging Trends
  
  

  This practical course on HPLC method development for LC/MS covers the specifics of how sample preparation and HPLC methods are developed for interfacing to ESI and APCI. The course discusses the importance of HPLC when interfaced with mass spectrometry including the HPLC separation of undetected matrix components, isomers and labile metabolites. The development of HPLC methods for LC/MS for use in qualitative and quantitative analysis throughout drug discovery and drug development are presented. The most advantageous column chemistry for each LC/MS application are thoroughly discussed including, reverse phase, normal phase, ion-exchange, HILIC, monolithic and polar embedded phases. The latest technologies such as UPLC, micro-SPE and on-line SPE will also be discussed. Orthogonal approaches to extraction and chromatography to achieve optimized LC/MS methods will be presented. Step-wise method development tutorials of developing methods for specific compound classes based on the structure are included in the final summary.
  
  Instructors: Roger Hayes, Schering-Plough Research Institute; Shane Needham, Alturas Analytics
  

• High Throughput Drug Discovery Support: LC/MS Strategies for Method Development, Profiling and Workflow Solutions
  
  

  Integrated HPLC and MS approaches for high throughput analysis have become standard practice in a pre-clinical drug discovery setting. Successful support strategies often provide a blend of high throughput methodologies with appropriate resources (tools and personnel). This course will target the “bread and butter” functions of discovery medicinal chemistry support. Real-world experiences with method development and analytical support will be discussed. Examples that feature ultra high throughput (library-based formats and individual sample processing), fast LC (theory & practice), generic gradient RP method strategies , scaling for HT purification, building in robustness into LC/MS set ups, details and perspectives on open-access success, fast physico-chemical profiling of compounds, and IT based workflow solutions.
  
  Instructors: Mark Hayward, Lundbeck Research USA; Ken Lewis, OpAns
  

• Is Poor Bioavailability in Early drug Discovery a Problem and If So, How Can We Solve It?
  
  

  Poor oral bioavailability is one of the leading causes of compound failure in preclinical and clinical development. Compounds with poor oral bioavailability have low plasma exposure and tend to demonstrate high inter-individual variability, which can limit their therapeutic application. Poor oral bioavailability in preclinical species does not necessarily translate into poor human oral bioavailability. This practical/hands-on course is designed to increase participants knowledge of:

  • The parameters that determine drug oral bioavailability
  • The factors that lead to species differences in oral bioavailability and how to deal with them
  • Approaches for optimizing the physicochemical parameters that influence drug solubility/permeability and metabolism
  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.
  
  Targeted Audience: Medicinal Chemists, Discovery Biologists, ADME Scientists
  
  Instructor: Ayman El-Kattan, Pfizer
  

• Sample Preparation for Non-Traditional and Traditional Biological Matrices: Mass Spectrometry Quantitation from Organic Molecules to Peptides/Proteins
  
  

  This course is targeted toward method development scientists in a development or discovery bioanalytical laboratory who wish to expend into new sample preparation techniques. The course will be informal and discussions among the faculty and attendees will be encouraged. The course is focused on the sample preparation process for LC-MS/MS quantitation of analytes in both traditional and nontraditional biological matrix. A brief description of the LC-MS/MS method development and validation will be used as introduction and the course will generally follow the workflow of a bioanalytical laboratory.
  
  The technical portion of this course will start with pre-extraction sample preparation that is usually the source of non-reproducibility of assay results. Common sample preparation techniques such as solid phase extraction (including online solid phase extraction), liquid-liquid extraction (including solid-liquid extraction), and protein preparation will be discussed next. An extensive discussion will be given on how to select the sample preparation technique based on factors such as the requirements on sensitivity, throughput, available equipment, the physical, chemical and the LC-MS/MS properties of the analytes and internal standard.
  
  One focal point of the course is regarding to the handling samples in non-traditional matrix such as tissue samples and recommendation for the method validation process. Analyte and matrix issues such as sample stickiness, solubility and stability will also be emphasized. Examples sample preparation techniques of nontraditional analytes including proteins, peptides, oligonucleotides, prodrugs, oligosaccharides will be covered, as appropriate. In addition, new sample preparation technologies will be introduced as part of the discussions.
  
  Instructors: Min Chang, Abbott Laboratories; Qin Ji, Covance