L2 - Sources of drugs Flashcards
Drug discovery in industry:
- Idea
- Hypothesis (pitch your idea)
- Make chemical
- Assay system
- Active chemicals
- Animal models
- Drug candidate
Natural products where drugs are made from: Animals
Fungi penicillium makes penicillin.
Hirudin medicinalis makes hirudin which is an anticoagulant and prevents blood clotting when leech suck out your blood.
Frog makes epibatidine which can be used to treat Alzheimer’s disease.
Natural products where drugs are made from: Plants
Monkshood and Wolfsbane make aconitine.
Willow bark makes salicylic acid (produces aspirin).
Opium poppy makes morphine.
Manmade products where drugs are made from:
Series of known synthetic pathways to make batches of unidentified chemical products - combinatorial chemistry. Test them to see if you find activity in a chemical and make more of specific one.
Assay design requirements:
High assay - identify activity
Medium assay - Confirm activity and quantify (High quality).
Low assay - Prove hypothesis and prove concept.
Have to see safety issues, ethical issues, cost, intellectual property (could be taking someone else’s idea).
Importance of structure-activity relationships:
Small changes in chemical structure alter both pharmacokinetic and pharmacodynamic properties of drug.
Switch functional groups and put back into assay system and test again.
Purpose of clinical drug trials:
phase 0 - look at unexpected effects
phase 1 - looks at side effects and how long body can tolerate large doses of drugs
phase 2 - larger sample size and looks at effectiveness of drugs on specific disease.
phase 3 - largest sample size and looks at side effects and safety and effectiveness by comparing to other drugs with similar treatments.
If drug pass this level they have to be approved by MHRA, EMEA and FDA.
phase 4 - drug is given to patients and given to different populations and doctor monitors and see if there are any symptoms.
