DRUG

DEVELOPMENT
PROCESS
Divine Grace M. Parcon, RPh
NEW CHEMICAL ENTITY
 Sources

A. PLANT MATERIALS
 RESERVOIR for potential new drugs
 Botanical folklores remedies into modern wonder drug
 Reserpine from Rauwilfia serpentina
 Vinca rosea – Folklore: use for diabetes
 Vinblastine & vincristine = antitumor
 Molecular manipulation – creation of slightly different
chemical structures
 Produce semi-synthetic drugs (inactive to active)
 Dioscorea species- Steroids (inactive) from which
cortisone and estrogen are semi-synthetically
produced
B. Animal source
 Tissues and biological processes
 Hormonal substances = thyroid extract, insulin
 Biologicals
a. Poliomyelitis vaccine – renal monkey tissue
b. Mumps and influenza vaccine – chick embryo
c. Rubella – germanmeasles – duck embryo
d. small pox vaccine – skin of bovine calf
GOAL DRUG
 Qualities and features are not completely
attainable but they are still sought in drug and
dosage form desire.

METHODS OF DRUG DISCOVERY
1. SCREENING
A. Random or untargeted – test large number of
synthetic organic compounds or substances of
natural origin for biological activity
B. Non-random or Targeted – use to determine a specific
activity
BIOASSAY
 Use to differentiate the effect and potensy
of the test agent from those controls of
known action or effect
 Can be done :
 In-vivo –using more expensive and disease
specific animal models
 In – vitro – using cell cultures to test agents
2. Molecular Modification – chemical alteration of
the known and previously characterized organic
compound for the purpose of enhancing
usefulness as a drug
 Enhancing specificity for a particular body target site
 Increase potency
 Improving rate and extent of absorption
 Modifying the advantage of its time course in the body
 Reduce its toxicity
 Changing its physical and chemical properties
 Mechanism based drug design
 Molecular modification to design a drug that
interferes specially with the known or
suspected biochemical pathway or mechanism
of a disease process
 Example:
 Enalaprilat (vasotec)– inhibits angiotensin converting
enzyme---- prevents vasoconstriction ------decreases
vasopressor -----------decreases BP
 Ranitidine ( Zantac) ------inhibits histamin at the H2
receptor -------inhibits gastric acid secretion.