4th EFMC Short Course on Medicinal Chemistry - Fall 2011
07/12/2011
10:00
Welcome
11:00
Introduction to the Safety & Attrition Workshop
Including a review of attrition rates, causes of failure and cost to the industry. To include examples of clinical attrition due to tox findings, worked examples and tutorials.
Esther SCHMID (EFS-SERVICES, Sandwich, United Kingdom)
12:30
Lunch
13:30
General Overview of Current Safety and Toxicity Testing
A review of established pre-clinical and post FIH toxicity testing. To include invitro & invivo testing such as Gen Tox and functional observation; illustrated by examples and breakouts
Dominic WILLIAMS (UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom)
15:30
Coffee Break
16:00
Small Molecule Based Attrition (1)
The Safety Related Attrition Challenge, including Structural Alerts:
A Medicinal Chemists Perspective of what can be controlled, including Structural Alerts; illustrated by examples and breakouts
Steve SWALLOW (ASTRAZENECA, CHERSCHIRE, United Kingdom) Karl GIBSON (PFIZER GLOBAL RESERCH AND DEVELOPMENT, Kent, United Kingdom)
18:00
Close
19:30
Dinner
08/12/2011
08:30
Small Molecule Based Attrition (2)
Molecular Properties
Physicochemical properties and toxicology outcome, including Med Chem risk; including worked examples and breakouts
Steve SWALLOW (ASTRAZENECA, CHERSCHIRE, United Kingdom) Karl GIBSON (PFIZER GLOBAL RESERCH AND DEVELOPMENT, Kent, United Kingdom)
10:30
Coffee Break
11:00
Choosing The Right Target
Including druggability, linking the target to the disease and the importance of understanding Ceff
Steve SWALLOW (ASTRAZENECA, CHERSCHIRE, United Kingdom) Karl GIBSON (PFIZER GLOBAL RESERCH AND DEVELOPMENT, Kent, United Kingdom)
12:30
Lunch
13:30
Off-target Based Attrition (1)
Ion Channel Safety:
Ion channel basics; their general roles in physiology; ion channel families and sub-types; their pharmacology in the context of drug safety; ion channel assays and screens; illustrated by case studies and worked examples
Chris POLLARD (ASTRAZENECA, Macclesfield, United Kingdom)
15:30
Coffee Break
16:00
Off-target Based Attrition (2)
Role of transporter interactions in toxicology and attrition:
Transporter interactions that have been linked to toxicity, e.g. kidney, liver (BSEP). Mechanisms and consequences. In vitro tools and predictive strategies; illustrated by case studies and worked examples
Gerry KENNA (ASTRAZENECA, Macclesfield, United Kingdom)
18:00
Close
19:30
Dinner
09/12/2011
08:30
ADMET or DMPK based Attrition
Focusing on Cyp inhibition, idiosyncratic toxicity, including reactive metabolites, time dependent inhibition; PK variability and can earlier and rapid PK assessment & insilico prediction methods reduce attrition
Kevin BEAUMONT (PFIZER, Cambridge, United States)
10:30
Coffee Break
11:00
Newer Methods of Predicting Toxicity (1)
Characterising Mechanisms of toxicity
Including pathway mining and investigative pathology type approaches to elucidating mechanisms
Mark M. GOSINK (PFIZER, Groton, United States)
12:30
Lunch
13:30
The Safety & Attrition Game (includes Coffee break)
