MDD David Thurston How Drugs Are Discovered - Past Present 01 10 24

what is personalized medicines and pharmcogenomics?

giving a patient a drug based on their genome, biomarkers and metabonomics rather than following a one size fits all approach

why is there a high costs for drug discovery? 3 reasons

expense of research and investment, short period of exclusivity, high risk of failure and litigation

how long does an average patent last for?

20 years

why are block buster drugs more popular for drug discovery than pharmacogenomic based drugs

they are able to target a mass market and recoup the investment and gain a profit

what are some problem with explosive marketing?

side effect and toxicities can arise as a larger group of patients are taking the drug, which may not have been seen in smaller clinical trials

how do companies try and reduce the risk in drug discovery?

staying in research areas in which they have expertise in

what are some examples of targets in drug discovery?

macromolecules like proteins(enzymes), glycoproteins(receptors) or DNA/rNA

what is screening?

this is a process where thousand of molecules are tested to see whether they show activity against a target, and can become HIT molecules.

what are some problems with trying to find LEADS from plants and trees?

isolating active ingredient can tricky and stereotypical is often complex

what is drug repositioning? with an example

purposeful research to see whether an existing drug has a different therapeutic use e.g. pregablin for neuropathic pain

what are some advantages of using drug repositioning for drug discovery?

drug has already passed toxicity and other test and safety is known for risk of failure is reduced

what is molecular pruning?

rationale form of drug discovery where parts of a HIT molecule are chopped off to identify the pharmacophore and editing the drug to make in more potent.

how can increasing rigidity of a molecule enhance potency?

decreases degrees of freedom for rotation of the molecule and enhances the interaction with the target.

what are some examples of conjugates?

drug- drug conjugates, drug-antibody conjugates, enzyme-antibody(ADEPT)