Principles of Drug Discovery

Module code: INC7014-B

Module Aims       

To provide students with an appreciation and understanding of the various stages of the drug discovery process.   To provide students with a current and critical evaluation of methods, techniques and strategies used to select molecules for evaluation of their biological properties.   In particular, a specific aim is to provide students with an understanding of the criteria used for 'druggable' targets.

Outline Syllabus   

The aim of this course is to provide an overview of all aspects of the drug discovery process and an introduction to drug discovery.   Topics include:

Targets
What makes a good drug target, strategies for identification of new targets, target validation

Receptors & Enzymes
A brief introduction/revision to receptor types, enzyme inhibition

Natural products
A source for potential lead agents. Discovery/sourcing of natural products. Drug development from natural product leads

Drug Design & Molecule Structure-Activity
This topic will explore in some detail the molecular structure & physicochemical properties of drug molecules (pKa, ionization, water solubility, stereochemistry), & how they interact with their targets

Computational chemistry
An overview of methods to generate hit compounds using molecular modelling, virtual libraries.  Includes a workshop demonstration.

Peptides, proteins, modern biological therapies:
Unique issues to such molecules, drug delivery, synthesis, therapeutic examples.  Cancer immunotherapy and antibody-conjugates.

Drug screening
Methods for in vitro & in vivo screening of agents

Lead optimisation strategies
Combinatorial approaches, diversity-orientated synthesis

Pharmacokinetics and Drug Metabolism:
Half-life, clearance, elimination, importance of administration route.  Drug metabolism reaction types, Cytochrome P450, Glucuronidation.

Safety Pharmacology
Pre-clinical assessment of potential clinical agents

Pre-clinical evaluation and clinical trials
Stages of clinical trial, examples

Intellectual property, commercialisation and regulation:
Patents, confidentiality; issues related to large scale production, formulation, marketing, regulatory affairs

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