Drug and drug design with It's development

2. 
 Drug is a chemical substance that have some kind of
physiological or biochemical effect on our body.
 Drug design’ or ‘tailor-made compound’ aims at
developing a drug with high degree of
chemotherapeutic index and specific action.
Drug & Drug design

3.  Various processes by which the drugs usually produce
their pharmacological effects.
How the drugs specifically react with the protoplasm to
elicit a Particular Pharmacological response.
 How the drugs usually get modified or metabolized or
Neliminated by the organism.
 Probablee relationship between biological activities with
chemical structure.
Drug design seeks to explain:

4. 
Drug design process

5. 
 Analogue- drugs having same activity but from
different origin.
 Uses
• Modification in carbon skeletal
• Substitute synthesis
Analogue

6. 
 Pro-drug- Inactive compounds which are converted to
active compounds in
 the body.
 Uses:
• Improving membrane permeability
• Prolonging activity
• Masking toxicity and side effects
• Varying water solubility
• Drug targeting
• Improving chemical stability
Pro-drug

7. 
 Shortly it is drug modification
 Steps:
• Pre-clinical studies
• Clinical studies
phase 1
phase 2
phase 3
phase 4
Drug development

8. Pre-clinical studies
Identify disease
Isolate protein
Find drug
Preclinical testing
GENOMICS, PROTEOMICS & BIOPHARM.
HIGH THROUGHPUT SCREENING
MOLECULAR MODELING
VIRTUAL SCREENING
COMBINATORIAL CHEMISTRY
IN VITRO & IN SILICO ADME MODELS
Potentially producing many more targets
and “personalized” targets
Screening up to 100,000 compounds a
day for activity against a target protein
Using a computer to
predict activity
Rapidly producing vast numbers
of compounds
Computer graphics & models help improve activity
Tissue and computer models begin to replace animal testing

9. Clinical trials
Identify disease
Isolate protein
involved in
disease (2-5 years)
Find a drug effective
against disease protein
(2-5 years)
Preclinical testing
(1-3 years)
Formulation
Human clinical trials
(2-10 years)
Scale-up
FDA approval
(2-3 years)

10. 
 Nature has made all the provisions for curing a
disease or disorder.
 The findings of the human genome project has
added more understanding to the target
identification.
 New safer drugs.
 Less side effects.
 More bio-availability.
 Faster onset of action.
conclusion

11.  Dr. V.M. Kulkarni, Dr. K.G.Bothara,Drug Design Nirali Prakashan,2010.pp.1.1-1.5.
 Abuin, A.; Holt, K.H.; Platt, K.A.; Sands, A.T.; Zambrowicz, B.P. (2002). Full-speed
mammalian genetics: in vivo target validation in the drug discovery process. Trends
Biotechnol., Vol. 20, no. 1, pp. 36-42.
 Augen, J. (2002). The evolving role of information technology in the drug discovery
process. Drug Discovery Today, Vol. 7, No, 5, pp. 315-323.
 Caldwell, G.W.; Ritchie, D.M.; Masucci, J.A.; Hageman, W.; Yan, Z. (2001). The New
Pre-Preclinical Paradigm: Compound Optimization in Early and Late Phase Drug
Discovery. Current Topics in Medicinal Chemistry, Vol. 1, No. 5, pp. 353-366.
 Foye’s Principles of Medicinal Chemistry, Williams DA and Lemke T.L. (Eds),
Lippincot Willams & Wilkins, 5th edn., 2002.
 Internet:
 Drug Designing, Discovery and Development Techniques, Elvis A. Martis1 and
Rakesh R. Somani2 PDF.
 Jornal of scientific and industrial research vol60, sep.2001,pp. 699-716.
References