- UCAS course code
- F152
- UCAS institution code
- M20
Course unit details:
Advanced Drug Discovery
Unit code | CHEM30441 |
---|---|
Credit rating | 10 |
Unit level | Level 3 |
Teaching period(s) | Semester 1 |
Available as a free choice unit? | No |
Overview
This course unit detail provides the framework for delivery in 22/23 and may be subject to change due to any additional Covid-19 impact.
Lectures from staff from the Department of Division of Pharmacy & Optometry, The Paterson Institute for Cancer Research and Signature Discovery Ltd and the Department of Chemistry will discuss new strategies for drug discovery, the clinical and preclinical evaluation of drug candidates and the chemical tools most commonly used to build drug candidates.
The following topics will be discussed in this unit:
1. Review the failings of traditional medicinal chemistry and the new concepts behind contemporary drug discovery
2. To study the top reactions used by medicinal chemists.
3. Look behind the scene of the Phase I, II and II trials of drug candidates, new directions in preclinical development and understand issues related to drug-drug interactions
Pre/co-requisites
Unit title | Unit code | Requirement type | Description |
---|---|---|---|
Fundamentals of Biochemistry | BIOL10551 | Pre-Requisite | Compulsory |
Properties of Medicines | PHAR10102 | Pre-Requisite | Compulsory |
Fundamentals of Drug Discovery | CHEM20422 | Pre-Requisite | Compulsory |
The Big Killers | PHAR20301 | Pre-Requisite | Compulsory |
Aims
The unit aims to:
provide insights into how new medicinal lead compounds are identified, provide an understanding of the synthetic strategies that are deployed in their synthesis and discuss how these molecules are evaluated in order to arrive at new medicinal agents.
Learning outcomes
On successful completion of the course students should be able to:
1. Be able to understand and explain how medicinal chemistry has in the past approached drug discovery and articulate the limitations of these approaches.
2. Describe and rationalize new approaches including HT, Fragment-Based Drug Discovery and virtual screening, and discuss and critically analyse HTS data outcomes.
3. Explain, calculate and apply drug physical characteristics such as ligand efficiency (LE) and lipid ligand efficiency (LipE). Define Lipinski’s rule and be able to apply to drug candidates.
4. Identify and explain examples of drug synthesis using reaction types that have been presented in lecture material or made available as on-line material, including providing mechanistic explanations for the outcome of synthetic schemes.
5. Suggest reaction processes, reagents and mechanisms, for specific drug synthetic steps provided.
6. Discuss specific drug development case histories articulating candidate selection criteria.
7. Describe and discuss importance of bioavailability, provide an account of processes for drug formulation, including aspects relevant to manufacture (tableting, particle size etc), as well as drug delivery.
8. Provide explanations of the key features of clinical trials, being able to explain important characteristics of trials.
9. Discuss the importance of drug-drug interactions and be able to explain case history examples.
Syllabus
Part 1: (Dr Allan Jordan and Dr. Ali Raoof): Historical perspective and failings of traditional medicinal chemistry, hit finding technologies (including fragment-based drug design, HT screening and virtual screening), target ID and target validation, Lipinski’s rules as guidelines/learnings from past failures, routes of Administration & Drug Delivery Systems, metabolism and its importance in drug design, SAR, personalized medicine and biomarkers, and oncology case studies showing contrasting use of technologies and timeline reduction
Part 2:
Top Reactions (Dr. John Gardiner): Common Structural Types found in Medicinal Agents; Exemplification of most-used chemical transformations. The organic reactions that underpin contemporary medicinal chemistry will be discussed in detail. For example, the course will cover amide bond formation, metal-catalyzed cross-couplings, heterocycle synthesis and modification and approaches to the asymmetric synthesis of drug candidates where applicable.
Part 3:
Clinical and Preclinical development (Prof. Alex Galetin, Dr Doug Steinke, Dr. Katharina Edkins): This section will cover new directions in clinical development of medicines, covering aspects of drug absorption, drug-drug interactions and new drug delivery. The final journey in the drug development pathway is making sure that the medication works in humans. This section will describe clinical trials where the new medication is tested in humans to determine dose, adverse drug reactions and efficacy of the drug on a disease and provide a virtual experience of a clinical trial. Post marketing surveillance of the medication once available to the market will also be examined.
Transferable skills and personal qualities
- Problem-solving skills
- Communications skills
- Numeracy and mathematical skills
- Analytical skills
- ICT skills
- Time management and organisational skills
- Interpersonal Skills
- Ethical behaviour
- Entrepreneurial Skills
Assessment methods
Method | Weight |
---|---|
Written exam | 100% |
Feedback methods
Students will be given problem sheets and example exam questions; outline solutions will be uploaded to BlackBoard. Staff will be available to answer queries during the course, especially during the workshop sessions.
Recommended reading
“An Introduction to Medicinal Chemistry, 5th Edn.” by G. L. Patrick. Oxford University Press, 2013. ISBN 978-0-19-969739-7. Main library, 3rd floor, blue area: 615.19 PA;
“An Introduction to Drug Synthesis”, by G. L. Patrick. Oxford University Press, 2015. ISBN 978-0-19-870843-8. Main Library, 3rd floor, blue area: 615.19 PAT
Study hours
Scheduled activity hours | |
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Assessment written exam | 2 |
Lectures | 24 |
Independent study hours | |
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Independent study | 74 |
Teaching staff
Staff member | Role |
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John Gardiner | Unit coordinator |