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• Undergraduate study:
• Courses
• Order a prospectus
• How to apply
• Information for applicants
• Why choose Kingston University
• Disability and mental health support
• Accommodation
• Undergraduate fees
• Fees, funding and payments
• Access, participation and inclusion

Drug Design and Medicine Development

• Module code: PY5010
• Year: 2018/9
• Level: 5
• Credits: 30
• Pre-requisites: None
• Co-requisites: None

Summary

The module builds upon themes and chemical topics that are introduced in the level 4 modules PY4030; Making Medicines and PY4040; The Science of Drugs developing them further in conjunction with pharmacologists, pharmaceutical scientists and pharmacists. The chemistry of carbonyl compounds is developed from the level 4 module to include carbanion chemistry and the associated reactions with applications in biosynthetic pathways such as the catabolism of glucose. Similarly aromatic chemistry is extended to look at the second substitution reaction-orientation effects using the formation of an anaesthetic as a case study. Asymmetric synthesis will be extended to include the synthesis of chiral medicines using ibuprofen as a case study. The mechanistic chemistry, bioinorganic chemistry and bioanalytical chemistry taught in this module will underpin applications in later Level 6 and 7 modules.

The medicinal chemistry topics will include antifungals, enzyme inhibition and novel peptides (solid support synthesis). Drug/receptor interaction will be introduced in terms of bonding interactions and signal transduction. Pharmacognosy will introduce you to natural products used for the treatment of cancer eg. taxol, calicheamicin and vincristine/vinblastine and cardiothoracics such as plant glycosides and bronchodilators. These topics will be taught in the context of themes/case studies and be augmented by inputs covering formulation and pharmaceutics, regulatory affairs associated with drug development in terms of clinical trials, licensing and registration. Various anchor points throughout the module will feed into other level 5 modules as well as higher level modules.

The lectures and associated workshops will attempt to develop your problem solving and team working skills in preparation for your future careers. This will be carried out in workshops and during the laboratory-based work where you will undertake various activities including group "mini-projects" that will be assessed using a range of methodologies such as oral presentations, report writing and group poster presentations.

Aims

• To give students an understanding of the origins, chemistry and in vivo behaviour of drugs and drug drug-like molecules
• To explore examples of organic and bioinorganic chemistry of relevance to drug discovery and the associated analytical techniques for verifying structures and purity and the measurement of drugs in body fluids.
• Discuss the development of ACE inhibitors and others as antihypertensives, antifungals, chiral drugs, anticancer drugs and drugs associated with the cardiothoracic system.
• To examine the pre-formulation/formulation of representative drugs including pharmacokinetics/dynamics, biopharmaceutics and sterile formulations

Learning outcomes

On successful completion of the module, students will be able to:

• Identify various types of types of bioorganic and bioinorganic molecules and explain their chemistry and their medicinal actions
• Discuss advanced methods in chemistry including asymmetric synthesis of chiral molecules and solid phase peptide synthesis
• Describe the chemistry of enzymes and enzyme inhibition, and identify why inhibitors can be drug candidates.
• Describe analytical and bioanalytical principles and instrumentation.  Explain their application in determining the identity, concentration and purity of drugs
• Explain the process of drug development from the laboratory to the dispensary-regulatory affairs and pharmacovigilance.
• Explain methods for the pre-formulation of a drug, dosage forms and the design of clinical trials

Curriculum content

• Pharmocognosy using relevant examples for the treatment of cancer, heart disease, bronchodilators, infection or other relevant topics. These may be taken from taxol, enediynes, vincristine/vinblastine, cardiac glycosides, development of salbutamol, ACE inhibitors, antimalarials, anti-inflammatory Semi-synthesis e.g. 10-deacetylbaccatin III, polymer supported peptide synthesis-     orthogonal protecting groups
• Examples of asymmetric drug synthesis, chiral catalysts and reagents.
• Bioinorganic chemistry themes such as the in vivo role of inorganic ions and metal ions in drug discovery and development
• Chemistry of carbanions, EAS (2nd substitution) and heterocyclic chemistry
• The drug effect-drug binding and secondary effects, enzymes, enzyme-substrate, enzyme inhibitors.
• Bioanalytical principles to determine the concentration of drugs in fluids, to ascertain the purity of a compound and to describe the technology involved.
• The process of drug development from the laboratory to the dispensary-regulatory affairs and pharmacovigilance.
• Methods for the pre-formulation of a drug, dosage forms and the design of clinical trials
• To develop problem solving and team working skills.
• Laboratory practical experiments and a mini-project to supplement the taught material

Teaching and learning strategy

Two concurrent series of lectures (22 each) will be used to deliver the core material which will be supported by workshops. These workshops are intended to supplement and illustrate the lecture material and to provide the student with an opportunity to clarify any aspects of the topics being taught. The workshops will also provide opportunities for student to get feedback from staff on their progress. The practical sessions will provide an opportunity for team (group) working.

Breakdown of Teaching and Learning Hours

Assessment strategy

This module will include a number of different strategies. Laboratory based practical experiments and workshops will be assessed formatively by either individual practical report, preparation of short proformas and in practical quizzes.  

Students will be asked to write a brief one-page introduction to the mini-project focussing upon the structure and dissemination of their results. This will be a formative assignment and provide each group with important feedback before they embark upon the summative assignment. The group mini-project will be summatively assessed by a group submitted short report.

An in module assessment, comprising of an in class test, will be used to assess student progress and performance as well as give an opportunity to provide feedback, as well as identify students requiring additional support. A 3-hour end of module exam will be used to ensure students can demonstrate the GPhC 'knows' and 'knows how' outcome standards associated with this module.

Level 5 MPharm students are required to pass a synoptic OSCE style assessment and a synoptic calculations test before they can progress to Level 6. These are to assure that even at this Level the student is demonstrating the appropriate skills, knowledge, understanding and attributes to become a future pharmacist. Components of the learning, including calculations skills and regulatory issues, in this module feeds forward into these synoptic assessments.

Mapping of Learning Outcomes to Assessment Strategy (Indicative)

Elements of Assessment

Achieving a pass

It is a requirement that the elements of assessment are passed separately in order to achieve an overall pass for the module.

Bibliography core texts

Organic Chemistry

Fessenden, R. J.; Fessenden J. S. (1998), Organic Chemistry, 6^th Edition, Brooks/Cole

In conjunction with -Clayden, J.; Greeves, N.; Warren, S.; Wothers, P. (2012) Organic Chemistry, 2^nd Edition, OUP

Medicinal Chemistry

Patrick, G. (2009) An Introduction to Medicinal Chemistry, 4^th Edition OUP

Natural Products, Biosynthesis and Pharmacognosy

Derwick, P.M. (2009) Medicinal Natural Products: A Biosynthetic Approach. 3^rd Edition, John Wiley and Sons Ltd, ISBN: 9780470741689

March, J. (2007) Advanced Organic Chemistry, 6^th Edition Wiley.

Bibliography recommended reading

Sykes, P. (1996) A Guidebook to Mechanism in Organic Chemistry, 6^th Edition, Prentice-Hall, ISBN 0582446953

Silverman, R. (2004) The Organic Chemistry of Drug Design and Drug Action, 2^nd Edition, Academic Press.

Mann, J. (2004) Chemical Aspects of Biosynthesis, Reprinted OUP, ISBN: 019 855677