Drug Discovery and

Development
Hendra Wana Nur’amin, dr., M.Sc
Department of Pharmacology
Faculty of Medicine
Lambung Mangkurat University

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 The development of pharmacology
Approximate
dates Therapeutics
> 3000 BC Magical potions
Herbal remedies

1600 AD Commerce

Apothecaries

1800 AD Chemistry Biomedical

science
Natural products

Pharmaceutical
Pathology industry
Chemical structure Pharmacology
Physiology

Biochemistry Synthetic
Synthetic drugs
1900 AD
chemistry Molecular biology
1970 AD
Biopharmaceutics
2000 AD Pharmacology
 CLINICAL
PSYCOLOGY MEDECINE VETERINARY PHARMACY BIOTECHNOLOGY PATHOLOGY CHEMISTRY
THERAPEUTICS MEDICINE

Psycho- Clinical- Veterinary- Pharmaceutical- Bio- Toxicology Medicinal

pharmacology pharmacology pharmacology science pharmaceutics Chemistry

Pharmacokinetics/ Biochemical
drug metabolis pharmacology

Pharmacology
Molecular
pharmacology Chemotherapy

Systems pharmacology
Neuro- Cardio Gastro intestinal Immuno Respiratory
Pharmacology pharmacology pharmacology pharmacology pharmacology

Pharmacogenetics Pharmacogenomics Pharmacoepidemiology Pharmacoeconomics

GENETICS GENOMICS CLINICAL HEALTH

EPIDEMIOLOGY ECONOMICS
 History in drug discovery

< 1900

Empirical study

1900
Functional study

1975 Ligand-binding study

1980
Molecular biology study
1990
Genomic study
 Drug discovery and development process
Lead compound

Screening of Acute toxicity

pharmacology study

Stability study Sub acute

Advance toxicity studies
pharmacology
Pharmacokinetic Carcinogenicity &
study on animal Mutagenicity studies
Phase I clinical study

Product Chronic
Phase II clinical study toxicity studies
development

Phase III clinical study

Pharmacokinetic
study on human
Registration &
Marketing

Phase IV clinical study

 Appling pharmacogenomics in drug discovery and
development

Discovery Exploratory Development Full Development

Phase I Phase II Phase III Phase IV

0 5 10 15
Years

11-15 Years

Idea Marketed Drug

Disease Target Selecting Pharmacogenetics
genetics variability responsders

Choosing the Better Improving early Predicting

best targets understanding decision making efficacy and
of our Targets safety
 Identify disease

Find a drug effective

against disease protein
Isolate protein (2-5 years)
involved in Scale-up
disease (2-5 years)

Preclinical testing
(1-3 years) Human clinical trials
(2-10 years)

Formulation

FDA approval
(2-3 years)
 Site and mecanism of action of drugs

• Enzymes → inhibitor (reversible and non reversible)

• Receptors → antagonis and agonis
• Ion channel → channel blocker
• Transporter → inhibitor of transport
• DNA → antisen, chelator DNA
From Genomics to Drug Discovery
Drugs
Genomics
DNA Proteomics PROTEINS DRUGS
(cf. EPO, Interferons, …)
Protein GENETICS
PHYSIOPATHOLOGY ANTIBODY DRUGS
(in vitro, in vivo, ..)

SMALL MOLECULES
DRUGS
FUNCTIONAL DRUG RATIONAL DRUG
VALIDATION DISCOVERY DESIGN
STRUCTURE-BASED
DRUG DESIGN
• AS DRUGS (incl. in silico…)
• AS TARGETS
HIGH THROUGHPUT
SCREENING

- RELEVANT ASSAYS…
- VERY LARGE LIBRARIES
OF COMPOUNDS
(SYNTHETIC OR NATURAL)
“INVENTORY”
 References
• Katzung BG, Trevor AJ. Basic & Clinical Pharmacology by Bertram G.
Katzung 13th Edition. The McGraw-Hill Companies Inc, 2015
• Golan DE, Tashjian AH, Armstrong EJ, Armstrong AW. Principles of
Pharmacology The Pathophysiologic Basis of Drug Therapy. 2012.
• Goodman & Gilman’s Manual of Pharmacology and Therapeutics
12th ed, 2011
• DiPiro JT, et al. Pharmacotherapy: A Pathophysiologic Approach 7th
Ed. San Fransisco: McGraw Hill, 2008
• Wells BG, DiPiro JT. Schwinghammer TL, DiPiro CV.
Pharmacotherapy Handbook 9th Ed. San Fransisco: McGraw Hill,
2015
• Finkel R, Cubeddu LX, Clark MA. Lippincott's Illustrated Reviews:
Pharmacology, 4th Edition. Lippincott Williams & Wilkins, 2009
• Lullmann H, Mohr K, Hein L, Bieger D. Color Atlas of Pharmacology
3rd Ed. New York: Thieme Stuttgart, 2005

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Contact: hendranuramin@gmail.com

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