DRUG DEVELOPMENT

DRUG DEVELOPMENT

Overall View

1.      Identify Molecular Target

-        Involved in cancer growth/development

-        Promise ‘Lead’

2.      Find/Screen/Design a product to interact with target (inhibitor/activator)

3.      Optimisation and Formulation

4.      Pre-clinical studies

-        ‘proof of principle’

-        Animal models for proof of concept and safety data 

5.      Clinical Studies  Phase 1 à 4

e.g. Imatinib (Gleevec)

-        Identify Target: Chromosome Transolcation t(9,22), BCR-ABL fusion protein

-        Lead Compound was found to have Kinase Inhibition, from screening of high throughput screening

-        Optimisation to enhance bioavailability and target specificity

-        Pre-clinical testing demonstrated proof of principle

-        Phase I  to III trials

Screening for Useful Compounds

•       High Throughput –millions of compounds (libraries) exposed to cell cultures and levels of apoptosis measured
•      Cominatorial Chemistry- synthetic molecules created
•            Natural products
•      ‘In-silico’ approach – virtual computer screening, selecting compounds binding based on knowledge of target structure