Drug Design and Discovery

Course code PHAR2202Units 10Level 2000Faculty of Health and MedicineSchool of Biomedical Sciences and Pharmacy

This course provides knowledge of the basics of microbiology, the pharmacology and principles of antimicrobial use and the use of synthetic chemistry to alter the properties of drugs. The course follows the evolution of drugs through time covering the principles of drug discovery in the areas of pharmacognosy and natural products; synthetic medicinal chemistry and the development of medicinal substances; the development of modern and innovative therapeutic substances including biopharmaceuticals; and future trends in drug discovery. The course will focus on chemistry and in particular how the chemical structure of a drug relates to its biological activity. Structure-activity relationships of drug families will include the discovery, development and design of antibiotics. The drug development pipeline from lead discovery to clinical trials will be introduced. Introductory concepts around regulatory affairs, patenting, registration and marketing will be covered in the context of new drug discovery.

An introduction to pharmacogenomics and bioinformatics is included in relation to the development of new drug development. Key concepts in globalisation and cultural aspects of pharmacy are integrated into this course in the areas of traditional medicine and Complementary and Alternative Medicines.

The course builds on existing knowledge in pharmaceutics to look at chemical kinetics and the stability of pharmaceuticals.

In order to participate in this course, students must complete a compulsory Health and Safety requirement.

Available in 2015

Callaghan CampusSemester 2
ObjectivesStudents will:
1. Be able to discuss the pharmacological management of infectious diseases including the mechanism of action of specific agents and their structure activity relationships.
2. Understand key principles of pharmacognosy and natural products and their role in shaping the pharmaceutical industry, including Traditional, Complementary and Alternative Medicines.
3. Understand the role of synthetic chemistry in the development of pharmaceutical agents; and the modification of chemical structures to develop new drug molecules.
4. Have an advanced understanding of the chemical structure of a pharmaceutical agent and determine the chemical group/s responsible for a given biological effect.
5. Be able to describe the modern and innovative discovery of biopharmaceuticals as it relates to today's healthcare and future trends in modern drug discovery globally.
6. Develop an understanding of drug targets as a recognition site for pharmaceutical agents; how the chemical structure of a substance influences interaction with a drug target; and the identification of new drug targets for future drug discovery.
7. Understand key concepts of the drug discovery process including regulatory affairs, patenting, registration and marketing in a global context.
8. Demonstrate a basic understanding of pharmacogenomics and bioinformatics as it relates to drug design and discovery.
9. Understand how stability of pharmaceuticals is affected by their chemical properties.
Content1. Pharmacognosy and the evolution of drugs from natural products:
- Pharmacognosy and where it fits into the evolution of drugs and the pharmaceutical industry.
- Examples of these pharmaceutical agents including digoxin and digitalis lanata; aspirin and willow; and taxanes and the yew tree and their evolution to modern medicine.
2. Complementary and Alternative Medicines:
- Global and cultural aspects of medicine including Chinese Traditional Medicine and the use of Traditional Medicines in Aboriginal and Torres Strait communities.
3. Synthetic chemistry and modification of chemical structure:
- Chemical properties of pharmaceutical agents and their modification to yield different chemical structures and thereby different pharmaceutical agents with the potential for different biological and/or immunological effect/s e.g. beta-lactam antibiotics.
- Biological properties of pharmaceutical agents and their modification to yield different biological molecules and thereby agents with varying pharmacokinetic and pharmacodynamic properties e.g. insulin analogues.
- Chemical stability and mechanisms of pharmaceutical degradation.
- The underlying chemical principles of pro-drugs and their application.
4. Structure Activity Relationships:
- Identify the chemical component of a structure that contributes to, or determines the biological activity of, a pharmaceutical agent.
- Look at how variance in chemical structure allows for differences in interaction with drug target; spectrum of activity; potency; duration of action and other biological effects.
5. General principles of the use of anti-infective agents in the management of infectious diseases, including counselling points and mechanisms of action.
6. Modern and innovative new drug technologies, which have led to the discovery of biopharmaceuticals including monoclonal antibodies and small peptides.
7. Understanding of various drug targets including protein molecules such as receptor, enzyme, transporter and ion channel. Introduce the concept of immunological drug targets and how this relates to biopharmaceuticals.
8. Scientific methods and future trends applied in drug discovery such as High Throughput Screening and how this related to the identification of drug targets.
9. Introduction to regulatory affairs in drug discovery outlining the process of getting a drug approved and the functions of various Australian and global regulatory authorities. Includes patenting, registration and marketing.
10. Introduction to bioinformatics and its role in drug discovery.
11. Introduction to pharmacogenomics and its role in drug discovery.
Replacing Course(s)NA
Industrial Experience0
Assumed KnowledgeCHEM1010 Introductory Chemistry I, CHEM1020 Introductory Chemistry II , PHAR1201 Introduction to Pharmacy and Formulation Sciences 2
Modes of DeliveryInternal Mode
Teaching MethodsLecture
Assessment Items
Examination: ClassCourse Learning Objectives 1, 2, 3, 4, 5, 6, 7, 9
Essays / Written AssignmentsCourse Learning Objectives 1, 2, 3, 4, 5, 6, 7, 9
Examination: FormalCourse Learning Objectives 1, 2, 3, 4, 5, 6, 7, 8, 9

Compulsory Course Component: This examination component will test a student's competency in one or more of the course learning objectives since these form part of the core competencies required of a pharmacist. Students must achieve a passing grade in the formal written examination component to be able to obtain a passing or higher grade in this course. On achieving a passing grade, a final mark will be given in the course and it will be recorded that the student has satisfied the compulsory course component. Students who fail to satisfy this compulsory course component will be offered a supplementary examination. Students who are required to complete a supplementary examination and satisfactorily pass the assessment and pass the course overall will be awarded a maximum mark of 50 for the course. Those who do not pass the supplementary examination will be awarded a zero mark and a FF grade, irrespective of their final numeric mark.
Other: (please specify)Practical reports
Course Learning Objectives 1, 2, 3, 4, 6, 9
Presentations - IndividualCourse Learning Objectives 5,6
Contact HoursLecture: for 3 hour(s) per Week for 12 weeks
Tutorial: for 1 hour(s) per Week for 12 weeks
Practical: for 3 hour(s) per Week for 8 weeks
Compulsory Components
Requisite by EnrolmentThis course is only available to students enrolled in the Bachelor of Pharmacy (Honours) program.
Compulsory Program ComponentSuccessful completion of CHEM1010 Introductory Chemistry I and CHEM1020 Introductory Chemistry II.
Compulsory Course ComponentStudents must complete a compulsory Health and Safety requirement.
Compulsory Course ComponentThe assessment components test a student's competency in one or more of the course learning objectives since these form part of the core competencies required of a pharmacist so students must:
1. achieve a passing grade in the formal written examination component.
Timetables2015 Course Timetables for PHAR2202