Lecture 8: Drug Development Flashcards
(34 cards)
what is the most expensive part of drug development?
clinical trials
six stages of drug development
- target selection
- lead discovery
- medicinal chemistry
- in vitro studies
- in vivo studies
- clinical trials & therapeutics
what is target selection
the decision to focus on finding an agent w/ a particular biological action that is anticipated to have therapeutic utility
what is target identification
identifying molecular targets that are involved in disease progression
what is target validation
proving that manipulating the molecular target can provide therapeutic benefit for patients
what are common biochemical classes of drug targets
GPCRs, enzymes, hormones & factors, ion channels, nuclear receptors
concepts involved in target selection
- cellular & genetic targets
- genomics
- proteomics
- bioinformatics
what is lead discovery
identification of small molecule modulators of protein function, and the process of transforming these into high-content lead series
tools for synthesis & isolation in lead discovery
in vitro chemical synthesis
how is combinatorial chemistry useful in lead discovery
optimization of target affinity & selectivity
- ADME properties
- reduce toxicity
how is assay development used in lead discovery
measuring drug activity
how is high throughput screening useful in lead discovery
screening the drug target with chemicals to identify the specific compounds that will move forward
what is medicinal chemistry
a dicipline at the intersection of synthetic organic chemistry & pharmacology
what does medicinal chemistry focus on
small organic molecules (not on biologics & inorganic compounds)
what is medicinal chemistry used in
- drug discovery (hits)
- lead optimization (hit to lead)
- process chemistry & development
tools for medicinal chemistry
- library development
- SAR studies
- in silico screening
- chemical synthesis
what must you do before testing a drug in people
find out the toxicity of a drug
two types of preclinical research
in vitro & in vivo
characteristics of preclinical studies
- not very large (take up to 3 years to complete)
- detailed info on dosing & toxicity levels
- researchers review findings & decide whether the drug should be tested in people after preclinical testing
in vitro studies
(in glass) studies using component of organisms (ie test tube experiment)
purpose of in vitro studies
- drug affinity & selectivity
- cell disease models
- MOA
- lead candidate refinement
in vivo studies
its experimentation using a whole, living organism
what do in vivo studies give info about
metabolic profile, toxicology, drug interaction
tools for in vivo studies
- animal models of disease states
- behavioral studies
- functional imaging
- ex-vivo studies
