drug development Flashcards
what things are investigated to identify drug targets?
- underlying disease mechanisms
- cell type/receptor involvement
- changes to signalling pathways
- changes to gene expression
what characteristics of P2X7R have identified it as a potential drug target?
- distribution of receptor subtype on neurones and inflammatory cells
- activated by high concentrations of ATP following cell trauma
how was the link between P2X7R and and arthritis shown?
using P2X7R knockout mice
what identifies P2X7R as a potential target for analgesia?
knockout mice lack inflammatory and neuropathic hypersensitivity to stimuli
what characteristics are desirable for a target assay?
method that is capable of testing a large number of compounds in a way that is simple, robust and can be automated
how can cell based assays be used to study P2XRs as a drug target?
- express recombinant receptors
- use fluorescence microscopy with calcium sensitive dye to understand how drug affects receptor activity
why are animal models used for early drug testing?
to establish safety and pharmacokinetic information
what considerations are there for a drug trial?
- ethics and consent
- drug vs placebo
- randomisation
- blindness vs double blindness
- compliance
what happens in phase 1 of a drug trial?
- safety testing
- using a small group of healthy individuals
- determine safe dose, identify side effects
what happens in phase 2a and 2b of a drug trial?
use a small number of patients with disease to test if the drug is effective, then perform longer term testing
what happens in phase 3 of a drug trial?
give the drug to large groups of people to confirm effectiveness and compare to existing treatments
