Training Courses
Event
- Title:
- ADME and hERG in Medicinal Chemistry
- Subtitle:
- Succeeding through the Literature
- When:
- 04.10.2011 - 05.10.2011
- Tutors:
- Where:
- Radisson Blu Hotel - Edinburgh
- Brochure:
- View Brochure
Description
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
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
Fee Info
- Course Fee:
- £1050 + VAT @ 20%
- Multi Discount:
- SAVE 5% for 2 attendees and 15% for 3 attendees
Venue
- Venue:
- Radisson Blu Hotel - Website
- Street:
- 80 High Street, The Royal Mile
- Postcode / ZIP:
- EH1 1TH
- City:
- Edinburgh
- Country:
- UK
Description
Located in the heart of Edinburgh's city centre on the historic Royal Mile, the Radisson Blu Hotel is located halfway between Edinburgh Castle and Holy rood Palace. With shopping areas and the business district well within walking distance from the hotel, it is the ideal place to stay. All guests have complimentary access to the fully-equipped Leisure Club with its jet stream pool (10 metres), sauna, solarium and gymnasium.
The hotel is holding standard rooms for us at a discounted rate. Scientific Update is contractually obligated to certain financial goals with the hotel. Your reservation is greatly appreciated, as it helps to meet our agreement. Please make your reservation soon in order to secure the reduced group rate.
Directions:
The hotel is only a five-minute walk from the Waverley Station and just 11.5 kilometres from the Edinburgh International Airport.
Ideal location among hotels near Edinburgh Castle
Built on craggy, extinct volcanoes above a North Sea inlet, Edinburgh is an ancient city best known for its skyline-dominating fortress namesake, Edinburgh Castle, which is only a short walk from this Edinburgh accommodation. The famed castle is home to the city's oldest building, the 12th-century St. Margaret's Chapel. While Edinburgh is steeped in history and features a bevy of impressive museums that are also near this luxury hotel, today the vibrant city has gained new fame for its annual world-class cultural festival.
Edinburgh attractions within walking distance:
- Edinburgh Castle - 10 min.
- Edinburgh Vaults - 5 min.
- Greyfriars Bobby - 10 min.
- Holyrood Palace - 15 min.
- National Museum of Scotland - 5 min.
- Our Dynamic Earth - 10 min.
- Scotch Whisky Heritage Centre - 5 min.
- Scottish Parliament - 10 min.
- Scott Monument - 10 min.
Attractions within driving distance:
- Edinburgh International Conference Centre - 5 min.
- Edinburgh Zoo - 10 min.
- Glenkinchie Distillery - 30 min.
- Roslyn Chapel - 15 min.
- Royal Botanic Garden - 10 min.
- Royal Yacht Britannia - 10 min.
- St. Andrews Links golf - 30 min.