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Pharmacokinetics and Pharmacodynamics: Principles and Applications in Pre-Clinical Drug Development |
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| Course Code: PKPD |
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| This course will help you understand the fundamental issues in pharmacokinetics, safety pharmacology and pharmacodynamics and how those issues are used in drug discovery. The course emphasizes the value of the independent variables in biological experiments (drug concentration, i.e. pharmacokinetics) but also discusses the interface of pharmacokinetics with pharmacodynamics (measurement of magnitude of the biological effect). Methods (in vitro and in vivo ADME Pharmacokinetic and in vitro pharmacodynamic and safety) to assess both of these will be discussed as well as strategies to optimize the drug discovery process from screening and drug design to final lead optimization. Emphasis is placed on the use of ADME data to optimize ‘druglike’ character of prospective drugs. |
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Dates - TBA |
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Check-in opens at 7:30 a.m. on the first day of the course.
Course runs from 8:30 a.m. to 5:00 p.m. each day. |
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Event Location: |
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TBA |
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Early Registration: |
$1,295 |
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Advanced Registration: |
$1,395 |
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Standard Registration: |
$1,495 |
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The course fee includes a course binder and a continental breakfast each day.
Five for Four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. Note: This discount is only available if you register by fax or mail and mention this discount. May not be combined with any other offer. |
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- Principles of first-order (linear) kinetics and comparison with non-linear processes.
- Linkage of physicochemical properties of molecules and ADME properties.
- Use of in vitro data (absorption Caco-2, PAMPA / metabolism microsomes, S9, hepatocytes) to predict PK in humans.
- Discussion of in silico solutions to ADME and safety pharmacology problems.
- Meaning and application of compartmental (vs. non-compartmental) models and their analysis.
- How ADME characteristics affect dosing and how drugs are used (i.e. once a day oral)
- Definition, measurement and inter-relationships among apparent volume of distribution, plasma protein binding, clearance and half-life.
- Critical issues in drug candidate selection.
- Factors affecting oral drug absorption and bioavailability.
- Relationships between PK and PD / system-independent measurement of drug activity.
- pK-PD interface: drug requirements for activity in open (in vivo) systems
- First-time dosing in humans / allometric scaling / interpretation of in vivo PK data.
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| Terry Kenakin in is Principal Research Investigator Molecular Discovery in the Department of Assay Development at GlaxoSmithKline Research and Development and teaches Pharmacokinetics and Pharmacodynamics: Principles and Applications in Pre-Clinical Drug Development and webcasts A Pharmacology Primer for Chemists and Pharmacokinetics and Pharmacodynamics for Chemists. |
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