Fees
- The course fee is £995
- Refreshments & lunch each day
- Dinner on Wednesday 29 October 2008
- The comprehensive course manual
General Information
The course begins with registration from 8.30am on Wednesday 29 October and finishes at approximately 5pm on Thursday
30 October.
ADME and hERG in Medicinal Chemistry
29 - 30 October 2008, Basel, Switzerland
A 2 day course given by Dr Corinne Kay, Med-Simple
Introduction
In addition to maintaining their sound synthetic organic chemistry knowledge, Medicinal Chemists have to address complex ADME (Absorption, Distribution, Metabolism and Elimination) and pharmacology issues on a day to day basis.
Although relevant principles of pharmacology can be picked up from traditional medicinal chemistry books, much of the wisdom required to progress projects takes years to acquire and many ‘tricks of the trade.’ These are often concealed within a profusion of medicinal chemistry papers. Distilling practical help from the literature itself requires experience as well as time.
‘ADME - hERG – Succeeding through the Literature’ is a new, interactive approach to learning medicinal chemistry.
The course is divided into self-contained blocks that require no prior knowledge of the topic. It spans the foundations of ADME as well as all relevant terms in pharmacokinetics. The hERG topic is treated in two parts: a comprehensive introduction to the topic and a comprehensive up to date review of the literature. Each block first gives sound background to the topic and then focuses on distilling ‘solutions’ from past and current literature, enabling participants to become effective and productive readers of the literature, thus promoting innovation. New concepts are applied in realistic group sessions which are designed to mimic real life situations.
The uncluttered and highly practical teaching style has been tried and tested in a number of pharmaceutical companies as well as in academia and has received much positive feedback.
Course Outline
- DAY ONE
- DAY TWO
Introduction to ADME
ADME Made Simple
A colourful voyage through the digestive system outlining the elements of ADMET, absorption, permeability, pgp, CYP’s, phase 1&2, enteropatic cycling, toxicity, renal excretion, glomerular filtration, oral absorption, first pass.
Round Table Discussion
Route of administration. Detection of pharmacologically active metabolites in drug discovery. Ames test.
Pharmacokinetics - Definitions and Assays
A useful, easy to follow yet comprehensive guide to elimination (half-life, extraction ratio, clearance, AUC) Distribution (volume of distribution, half-life) absorption (bioavailablilty, iv, po), and overview of corresponding assays methodologies.
Making the correct Diagnosis - ADME and the Medicinal Chemist
A step by step guide to correctly diagnosing the perennial issues in lead optimization for drug design.
Workshop: ADMET Issues - Solutions that Work
Making the diagnosis and abstracting working solutions to recurrent ADME issues from a range of key medicinal chemistry papers. This team exercise provides a range of quality ideas that have been successfully applied in topical research projects taken from a broad spectrum of pharmaceutical companies.
Roundup Session and Outstanding Questions
hERG – La Bête Noire
hERG – An Introduction
hERG and IKr, ECG, TDP, QTC. The hERG channel structure, in silico models, site directed mutagenicty studies. Assay methodologies. Regulatory issues, current issues.
The hERG 4 Commandments – Designing out hERG Activity
An up to date overview of the literature and summary of key approaches employed by the major players in the field. Lecture illustrated with numerous worked examples on designing out hERG activity.
Round up Session
WORKSHOP - Strategies for Diluting out hERG
A productive group session aimed at working through real life projects designing out hERG activity. The ‘hERG 4 Commandments’ will be evaluated in parallel and discussed.
Round up Session: Conclusions and Recommendations
The organisers reserve the right to change the published programme of events and course content as circumstances dictate.