Introduction to course: why in vitro pharmacology is important!
Mike TREVETHICK (FORMERLY WITH PFIZER, Broadstairs, United Kingdom)
In this introductory session we will discuss the principle of how drugs interact with receptors, ion channels and enzymes and then discuss major reasons why drugs fail in clinical trials and why this highlights the importance of ’thorough ‘ pharmacology.
21:00
Close
11/04/2011
Day 1: Data from the world of equilibrium: Antagonist Pharmacology
08:30
Introduction to day 1 - What Data is collected in Equilibrium Assays and what does it miss?
Mike TREVETHICK (FORMERLY WITH PFIZER, Broadstairs, United Kingdom)
Assessing Drug binding to Receptors
09:00
What is a Ki and Kd - What do they mean, what is the Value of such Data in Drug Discovery Programmes
David WINPENNY (PFIZER GLOBAL RESEARCH AND DEVELOPMENT, Sandwich, Kent, United Kingdom)
09:45
Breakout Session: Ligand Binding in Agonist v. Antagonist Programmes
David WINPENNY (PFIZER GLOBAL RESEARCH AND DEVELOPMENT, Sandwich, Kent, United Kingdom)
11:00
Coffee Break
Antagonist/Inhibitor Pharmacology
11:15
Types and Antagonism, Assay used, Interpretation of Data
Jenny KOENIG (UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
12:00
Breakout: Types of Inhibition/Antagonism; Ligand Binding v. Function; Allosterism
Jenny KOENIG (UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
13:00
Lunch
Translating Antagonist Action from in vitro to in vivo Environment
14:00
How can you predict if your Antagonist/inhibitor is likely to have Efficacy in vivo
Simeon RAMSEY (PFIZER, Sandwich, Kent, United Kingdom)
14:45
Breakout: can you explain why one Antagonist/inhibitor has worked but one hasn’t
Simeon RAMSEY (PFIZER, Sandwich, Kent, United Kingdom)
15:45
Coffee Break
16:00
Drug Case History Angiotensin 1 receptor antagonists for hypertension
Mike TREVETHICK (FORMERLY WITH PFIZER, Broadstairs, United Kingdom)
17:00
Round up of Day 1
12/04/2011
Day 2: Data from the World of Equilibrium: Agonist Pharmacology
08:30
Introduction to Day 2
Agonist Pharmacology at GPCRs and Ion Channels
08:45
Defining Agonist Action: Assays used to assess Potency and Efficacy at GPCRs and Ion Channels
Elliot LILLEY (INDEPENDENT PHARMACOLOGICAL CONSULTANT, United Kingdom)
09:30
Breakout Session: Assessing Potency and Selectivity of Agonists in vitro
Elliot LILLEY (INDEPENDENT PHARMACOLOGICAL CONSULTANT, United Kingdom)
10:45
Coffee Break
Translating agonist Action from in vitro to the in vivo Environment
11:00
The importance of defining Agonist Action in terms of Affinity driven and Efficacy
Sarah NICKOLLS (PFIZER, Sandwich, Kent, United Kingdom)
11:45
Breakout Session: why doesn’t your Agonist work in Natural Receptor Systems?
Sarah NICKOLLS (PFIZER, Sandwich, Kent, United Kingdom)
13:00
Lunch
14:00
Breakout session: What do these PK-PD Profiles indicate about Drug Receptor Interactions?
Elliot LILLEY (INDEPENDENT PHARMACOLOGICAL CONSULTANT, United Kingdom) Sarah NICKOLLS (PFIZER, Sandwich, Kent, United Kingdom)
15:30
Coffee Break
16:00
Drug Case History – The Transformation of Adrenaline into inhaled beta 2 Agonists to treat Asthma
Mike TREVETHICK (FORMERLY WITH PFIZER, Broadstairs, United Kingdom)
17:00
Round Up of Day 2
13/04/2011
Day 3: Warning – Receptor Kinetics can seriously improve you Project!
08:45
Introduction
Mike TREVETHICK (FORMERLY WITH PFIZER, Broadstairs, United Kingdom)
09:00
Principles of Receptor Kinetics and Assays
Yogesh SABNIS (PFIZER, Braine-l'Alleud, Belgium)
09:45
Coffee Break
Breakout session: Improving your Project with Receptor Kinetics
11:00
What do these Kinetic Profiles indicate?
Yogesh SABNIS (PFIZER, Braine-l'Alleud, Belgium) David WINPENNY (PFIZER GLOBAL RESEARCH AND DEVELOPMENT, Sandwich, Kent, United Kingdom)
11:45
Feedback from Breakout Session
Yogesh SABNIS (PFIZER, Braine-l'Alleud, Belgium) David WINPENNY (PFIZER GLOBAL RESEARCH AND DEVELOPMENT, Sandwich, Kent, United Kingdom)
