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Drug-Like Properties in Drug Discovery
| Type | Course |
|---|---|
| Language | English |
| Date |
August 15, 2009
to August 16, 2009 |
| Venue |
Crowne Plaza Hotel - The Hamilton 1001 14th St NW Washington, DC 20005 US |
| Chemistry Specialties |
|
| Chemistry Techniques |
|
| Contact |
American Chemical Society 1155 Sixteenth Street, NW Washington, DC 20036 US (800) 227-5558 shortcourses@acs.org |
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This course is designed to increase your knowledge of drug-like properties, ADME and how to apply this information in medicinal chemistry for hit selection, lead optimization and development candidate selection and is designed for medicinal chemists and other discovery scientists who design, synthesize, and test new drug candidates, lead research teams, or measure and predict ADMET properties of compounds.
Key Topics
* Essentials of key pharmaceutical properties and practical real-world applications
* Successful structure modification strategies to improve drug-like properties and pharmacokinetics.
* Case studies on how med chemists enhance properties and PK through structure modification.
* The impact of drug properties on drug discovery chemistry, in vitro and in vivo biological testing, pharmacokinetics, and safety.
* Property assays: experimental design, measurement and interpretation.
* Which properties to optimize for improved pharmacokinetics performance.
Who Should Attend?
Medicinal chemists and other discovery scientists who design, synthesize, and test new drug candidates, lead research teams, or measure and predict ADMET properties of compounds. Registrants should possess a basic knowledge of drug discovery.
How You'll Benefit
* Understand and gain confidence with each property and how they affect your success.
* Be able to apply drug-like property data to hit selection, lead optimization, clinical candidate selection, and biological testing.
* Become familiar with how pharmaceutical properties are measured for better data interpretation.
* Gain experience and familiarity with property concepts by participating in individual and group activities, including real-world case studies.
* Learn about examples where leads were successfully optimized to improve drug-like properties.
* Non-mathematical treatment of properties, diagnosis and optimization.
Speakers
Edward H. Kerns is Associate Director of Chemical Technologies in Drug Discovery at Wyeth Research. He leads the pharmaceutical profiling group to provide property data for drug discovery compounds.
Li Di is Principal Research Scientist II in Chemical Technologies in Drug Discovery at Wyeth Research. She is the group leader for property profiling in Princeton and consults for teams on property optimization.
Session titles
The Importance of Pharmaceutical Properties - Candidate failure, the new focus that integrates activity and properties, physiological barriers to drug penetration in vivo, how properties can limit biological activity experiments
Properties That Are Crucial for Drug Discovery - Practical working knowledge of solubility, permeability, metabolism, pharmacokinetics, cytrochrome P450 inhibition, plasma protein binding, metabolites, hERG, Pgp efflux, update transporters, prodrugs; plasma and solution stability, lipophilicity, pKa, rule of 5, lead-like properties, blood-brain barrier, discovery formulation, discovery toxicology, applications of Property Data, liability alerts, hit selection, prioritizing compounds for in vivo studies, diagnosing root property limitations, guide structure modification.
Assays for Each Property - Introduction to property assays, cost/throughput/benefit analysis, selecting the right assay for your needs, interpreting data.
Applying Property Data to Structure Modification - How structural differences affect properties, structure modifications to improve each property, case studies of successful structure modification.
Individual and Group Exercises - Interpretation of data, selecting properties relevant to your specific question, selecting an appropriate assay to meet your needs, modifying structures to improve properties, frequently asked questions and answers.