Drug Discovery and Development full notes PDF

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Drug Discovery and Development full notesLecture 1- overview of drug discovery and development Medical need of new drugs- drugs could be improved via efficacy or less side effects, more drugs are needed for the aging population and diseases of affluence  A new drug needs to be commercial attractiv...

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Drug Discovery and Development full notes

Lecture 1- overview of drug discovery and development    

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Medical need of new drugs- drugs could be improved via efficacy or less side effects, more drugs are needed for the aging population and diseases of affluence A new drug needs to be commercial attractive- big market size, little competition, need to be able to replace ‘off patent’ drugs and maintain pipeline of new drugs Companies will aim for blockbuster drugs which are cost effective to discover and develop and market one drug Life cycle maintenance- changing a drug in some way to make a new patent and sell more e.g. making the drug once a day instead of three times a day

The molecular target underlying the disease the drug is treating should be identified e.g. gene mutation or altered gene/ protein expression in a disease The target must be validated before getting started this can be done by: using a ‘tool’ compound which interferes with the molecular pathway, knockout animals, looking at cellular pathways of proteins rather than individual proteins, phenotypic screening How new drugs are discovered- serendipity, folk remedies, replacement therapies, rational drug design, high throughput screeninge Structure based drug design- requires knowledge of 3 dimensional structure of target- can e found by X-ray crystallography, NMR spectrography, computer modelling, using the structure of related protein, use information to design compounds that bind with high affinity and selectively to the target Ligand based design- knowledge of other molecules that bind to the biological target, modify chemical structure systematically, can discover potential drugs without knowing structure of target molecule Fragment based design- typically...