Advanced Drug Discovery


Unit code: CHEM30441
Credit Rating: 10
Unit level: Level 3
Teaching period(s): Semester 1
Offered by School of Chemistry
Available as a free choice unit?: N

Requisites

Prerequisite

Aims

 1. Review the failings of traditional medicinal chemistry and the new concepts behind contemporary drug discovery (Part    1).

2. To study the top reactions used by medicinal chemists (Part 2).

3. Look behind the scene of the Phase I, II and II trials of drug candidates, new directions in preclincal development and understand issues related to drug-drug interactions (Part 3).

 

Overview

Lectures from staff from the Division of Pharmacy and Optometryand School of Chemistry, and The Paterson Institute for Cancer Research 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.

Part 1 “Contemporary Drug Discovery”

Dr Allan Jordan, Dr Niall Hamilton and Dr Stuart Jones (The Paterson Institute for Cancer Research ) (8 lectures)

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 “Clinical and Preclinical Development”

Dr Zahraa Al-Ahmady, Dr Alex Galetin, Dr Doug Steinke (Division of Pharmacy and Optometry) (8 lectures)

This section will cover new directions in clinical development of medicines, covering aspects of drug absorption, drug-drug interactions and new drug delivery, including nanomedicines. The final journey in the drug development pathway is making sure that the medication works in humans. This interactive 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 surviellance of the medicaton once available to the market will also be examined.

 

Learning outcomes

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 from lectures, including providing mechanistic explanations for the outcome of drug synthetic reactions.

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.

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

  • Written exam - 100%

Feedback methods

Students will be given problem sheets and example exam questions and staff will be available to answer queries during the course

Study hours

  • Assessment written exam - 2 hours
  • Lectures - 24 hours
  • Independent study hours - 74 hours

Teaching staff

Peter Quayle - Unit coordinator

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