Drug discovery by Dr Siva

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Drug Discovery Process : 

Drug Discovery Process Prepared & Presented by Dr.Siva [email protected]

Drug Discovery process up to Preclinical stage : 

Drug Discovery process up to Preclinical stage

Organization of Drug discovery : 

Organization of Drug discovery

Slide 4: 

Role of PK-PD labs in Drug discovery

Development : 

Development

Clinical Trials : 

Clinical Trials Investigational New Drug application IND

Basic steps in drug discovery : 

Basic steps in drug discovery Choose a disease Choose a drug target Identify a “bioassay” bioassay = A test used to determine biological activity. Find a “lead compound” “lead compound” = structure that has some activity against the chosen target, but not yet good enough to be the drug itself. If not known, determine the structure of the “lead compound” Synthesize analogs of the lead Identify Structure-Activity-Relationships (SAR’s)

Basic steps in drug discovery : 

Structure-Activity-Relationship (SAR) = How does the activity change as structure is systematically altered? Identify the “pharmacophore” pharmacophore = the structural features directly responsible for activity Optimize structure to improve interactions with target Determine toxicity and efficacy in animal models. Determine pharmacodynamics and pharmacokinetics of the drug. Pharmacodynamics explores what a drug does to the body, whereas pharmacokinetics explores what the body does to the drug. Basic steps in drug discovery

Choosing a Disease : 

Choosing a Disease Pharmaceutical companies are commercial enterprises Pharmaceutical companies will, therefore, tend to avoid products with a small market (i.e. a disease which only affects a small subset of the population)

Choosing a Disease : 

Choosing a Disease Pharmaceutical companies will also avoid products that would be consumed by individuals of lower economic status (i.e. a disease which only affects third world countries)

Choosing a Disease (cont.) : 

Choosing a Disease (cont.) Most research is carried out on diseases which afflict “first world” countries: (e.g. cancer, cardiovascular diseases, depression, diabetes, flu, migraine, obesity).

Identifying a Drug Target : 

Identifying a Drug Target Drug Target = specific macromolecule, or biological system, which the drug will interact with Sometimes this can happen through incidental observation…

Selectivity is Important! : 

Selectivity is Important! e.g. targeting a bacterial enzyme, which is not present in mammals, or which has significant structural differences from the corresponding enzyme in mammals

Slide 17: 

Having the genetic code for the production of an enzyme or a receptor may enable us to over-express that protein and determine its structure and biological function. If it is deemed important to the disease process, inhibitors (of enzymes), or antagonists or agonists of the receptors can be prepared through a process called rational drug design.

Relation ship of HTS & VS : 

Relation ship of HTS & VS

Thank You : 

Thank You

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