1. Today’s Drug Discovery Process “How Do We Discover Drugs”
Dr. Vincent P. Gullo
Drew University
From the reading, what is the first step in the drug discovery process.
Understand a disease, figure out what’s wrong pick a target to modulate to correct the disease
What is a target?

2. Topics My background Research interests Drug discovery process
Previous seminar topics
Possible seminar topics

3. Background B.S. in Chemistry – City College of NY
Ph.D. in Organic Chemistry – Columbia University
Career in Drug Discovery
Spent 8 years at Merck focusing on discovering new drugs for cardiovascular disease, antibiotics and animal health drugs from natural sources
20 years at Schering-Plough working on discovering drugs from natural and synthetic compound sources for a broad range of therapeutic areas
3 years at a small biotech company searching for drugs from natural sources for a broad range of therapeutic areas.

4. Research Interests Antibacterials
Need to treat resistant microorganisms
MRSA
Carbapenem resistant enterobacteriaceae (CRE)
Lack of major interest by large pharma companies until recently
Can be done at Drew with undergraduates
Microbiological assays (Demain)
Synthetic chemistry and instrumentation available
If we are successful, contacts with small company to follow up further

5. The Drug Discovery Process
Timeline – 12 to15 years
Cost – $1 to 1.6 billion
Target
Selection
Target
Validation
Assay
Development
Hits
& Leads
&
Screening
Lead
Optimization
Clinical Trials
Phase I, Phase II, Phase III
Development
New Drug
Application
Market
& Phase IV

6. Search for a New Antibacterial
Target selection and validation
Inhibit growth of the bacteria - Numerous successes using this approach
Microbial assay - agar diffusion assay

7. Screening and Hit/Lead Identification
Test (screen) 250 compounds from Dr. Houlihan’s library of compounds prepared for anorexia and cocaine addiction
13 compounds discovered with similar structures
Synthesizing analogs to improve potency, spectrum of activity and PK

8. Previous Research Topics
The Antibiotic Crisis (What is the problem and how to address it)
Drug Discovery Compound Sources: Natural or Synthetic Compounds
Tuberculosis (difficulties in treating TB and what are potential solutions)
Hepatitis C virus (Will we ever be able to have a complete viral response)
Collateral Damage: Comparing Targeted Therapies to Non-Specific Chemotherapy in Cancer
Induced Pleuripotent Stem cells and the Potential to Cure Type one Diabetes
Cystic Fibrosis: Are We on the Pathway to a Cure
How is Exploring Nature Helping Us to Fight Cancer?

9. Possible Research Reports
Anything along the drug discovery pathway
Types of assays
Phenotypic vs. Targeted
Natural products
Role in today’s drug discovery process?
Diseases with unmet medical need
Diabetes
Heart disease
Cancer
Antibacterials/antifungals/antivirals