PHAR 5091.002

Course Name: Drug Discovery: Nuts and Bolts

Course Director: Dr. Wouter Koek

Course Content:

The process of discovery of medicinal compounds has evolved from the earliest attempts to discover herbal remedies to the present quest to develop safe, efficacious medicines. The last hundred years have witnessed the introduction of drugs that have revolutionized medicine. Early and recent drug discovery will be exemplified by the following papers:

1) Paul Ehrlich: magister mundi. Drews J. Nat Rev Drug Discov 3:797-801, 2004

2) Case history: the discovery of fluoxetine hydrochloride (Prozac). Wong DT, Perry KW, DT Wong. Nat Rev Drug Discov 4:764-774, 2005

3) Discovering risperidone: the LSD model of psychopathology. Colpaert FC. Nat Rev Drug Discov 2:315-320, 2003

and by selected chapters from: Drug Discovery: A History.  Sneader W.  John Wiley & Sons, 2005

Chapter 27: Drugs originating from the screening of dyes

Chapter 28: Drugs originating from the screening of organic chemicals

Chapter 29: Drugs discovered through serendipitous observations involving humans

Chapter 30: Drugs discovered through serendipity in the laboratory.

History shows that it has been relatively easy to discover a new drug, but exceedingly difficult to discover one that is safe enough to be administer as a medicine.  The current status of drug discovery and development will be illustrated by selected chapters from Drug Discovery: from Bedside to Wall Street. Bartfai T, Lees GV. Elsevier, 2006

Chapter 1: The art of putting a molecule in man

Chapter 7: Target-based drug discovery: part 1

Chapter 8: Changes need to be made

Chapter 9: Target-based drug discovery: part 2

Chapter 10: “Drugable” targets

Chapter 11: So many drugs, so few entities

Chapter 12: How to find a candidate drug

Chapter 13: Practicalities: the hoops and hurdles of big pharma

Chapter 15: How to improve the odds of finding a safe drug that works`

Grading: The student will read, present, and discuss the articles and chapters. In addition, the student will write a one-page drug discovery project proposal. The final grade will be on a lettered scale and will be based equally on the oral presentations and the written paper.

Pre-requisites: Consent of Instructor

Credit Hours: 1 credit

When offered: Anytime