Chapter 2 (E1) Flashcards
Cost and timeline of drug development/discovery, naming drugs.
A compound that affects physiological functioning once absorbed into the body.
What is a drug?
The cooperative effort of various disciplines to bring a drug from concept to market.
What is drug discovery?
List 3 key individuals involved in the drug discovery process.
1) Molecular biologists
2) Medicinal chemists
3) Lawyers
A general rule of thumb in the drug discovery process is that the profit of { } successful drug(s) must be able to support approximately { } drug(s) in development.
Blank #1) 1
Blank #2) 8.5
What are the main 3 considerations when choosing a profitable disease area?
Choose diseases that are:
1) Highly profitable b/c they affect a lot of people
2) Without current or effective treatment
3) Requiring long-term treatment
What are 2 other strategies to consider when choosing a profitable drug project?
1) “Me too” drugs
2) Finding a new mode of action
What is the purpose of developing “me too” drugs?
To push a similar drug onto the market just b/c there’s enough need and enough patients
What does finding a new mode of action for a drug entail?
Finding a new receptor/enzyme/target
Site of action for a drug that controls a biological response.
What is a target?
What are 3 general examples of drug targets?
Receptors, enzymes, & nucleic acids
Term used describe a promising target.
What is druggable?
How do you determine the structure of a drug target?
X-Ray crystal structure data if available
What is the difference between the “one drug, one target” and “multi-target” approaches to identifying a target?
“One drug, one target” is the traditional approach that can prevent or greatly reduce side effects since the drug only hits one target.
“Multi-target” is the newer approach that hits several targets weakly, and the combined weak responses across multiple pathways could yield a larger biological effect
What is the major pro/up-side to the “multi-target” approach to target selection?
You can hit multiple pathways with a single drug, effectively reducing the amount of medicine required, especially for complex diseases where the pathogenesis depends on a series of simultaneous biochemical events
Method to measure the activity of a compound.
What is an assay?
What are the 3 main types of assays (ordered from least expensive to most expensive)?
1) Biochemical
2) Cellular
3) Animal
The study of { } in biochemical assays is essential to determining how a drug binds to a specific receptor or checking the rate of an enzyme-catalyzed reaction.
Pharmacodynamics
Method of quickly testing a library of hundreds to thousands of compounds for activity against a target via a robot.
What is high-throughput screening (HTS)?
How does high-throughput screening (HTS) of enzymes typically occur in biochemical assays (HINT: Pharmacokinetics)?
Biologists typically follow the reaction profile of the enzyme with and without the drug present via UV-Vis and a plate reader
How does high-throughput screening (HTS) of receptors typically occur in biochemical assays (HINT: there are 2 main methods discussed in lecture)?
1) Tagging drug w/ radioactive isotope
2) Fluorescence assay or UV-Vis
How are compounds chosen for biochemical assays?
A class of molecules is usually known for a target depending on available literature
How many tests are run during a biochemical assay?
As many as needed for all unique compounds, at varying concentrations, duplicated or triplicated
Where or how do we get the compounds needed for biochemical assays (HINT: 3 solutions all involving money)?
1) Synthesize them
2) Merge/buy a company already studying compound of interest
3) Renting out a company
What is the general purpose of cellular assays during assay development?
To see how a compound behaves throughout a whole cell
