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L2- Sources of drugs and their nature
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- 1Key moments in the history of the pharmaceutical industry- The modern pharmaceutical industry emerged at an intersection between 3 critical areas: biomedical sciences, chemistry and therapeutics.
- 1909- Ehrlich showed syphilis could be treated using arsenic compounds
- 60s, 70s, 80s, era of 'rational drug design'; beta blockers, ACE inhibitors
1961- Thalidomide withdrawn
2002- Human genome mapped - 2Key stages in the drug discovery process1. Basic research eg in Unis- leads to better understanding of physiology and disease mechanisms
2. Identification of potential drug targets- looking for molecular targets- usually proteins- that play a critical role in the disease
3. Hypothesis generation- 'a drug that acts on its target to change activity will be more effective in treating disease - 3Other considerations in the drug discovery process- Safety considerations: harm to patients/environment
- Ethical issues: is development of the drug conducive to a civilised society
- Intellectual property- is the drug covered by a patent?
- Cost- does it make buisiness sense to develop a drug to treat a particular condition? - 4Main sources of drugs with examplesMany drugs are, or are derivatives of natural products, while others are synthesised in the pharmaceutical industry
Examples:
Morphine- opium poppy- analgesia
Penicillin- penicillin funghi- antibiotic
Dixoxin- digoxin mould- treating heart failiure
Botulinium digitoxin- bacterium clostridum botulinum- botox - 5Combinatorial chemistryChemicals reacted together from a library. Products mixed and reacted together to create new chemicals
- 6High throughput screening- Using assay techniques to screen compounds in the library in order to identify which compounds have the required biological activity.
- Early assays must have the ability to screen lots of compunds quickly, hence the term 'high throughput' screening
- Highly automated, often done by robots - 7Structure-activity relationships, and why they are important in the drug discovery processStructure-activity relationships; aka SARs can be used to optimise the properties of promising drug candidates.
- Similar-structured drugs often have similar activities eg morphine, coedine - 8Drug discovery and development: Clinical trials: Pre clinical stages- Preclinical stages: last about 5-10 years, usually result in 1/2 drug candidates being taken forward into human trials. Patent granted early during this stage & lasts for 20 years
- 9Clinical trials: phase 1: exploratory studies in man- Drug will have already be tested in rodents and mammals, this is the first test in humans.
- Involves a small amount of voulenteers, receivingincreasing doses in specialised facilities
- This phase is to asses for:
Safety- identifying potentially dangerous side effects
Tolerability- unpleasant symptoms/side effects - 10Clinical trials: phase II: Proof of concept and safety- To determine clinical effect of the drug i n patients, as well as confirming safety and tolerability
- Phase IIa- exploratory, 50-200 patients, approx 1 yr, dose and regimen based on phase 1 results. Placebo-controlled, randomised , double-blind.
- Phase IIb- confirmatory- 200-500 patients, approx 2 yrs. Tests safety and efficacy compared to placebo/current treatment in randomised, double-blind trials. - 11Clinical trials: Phase 3: Confirmatory- Full scale evaluation of how effective and safe the treatment is compared to current treatment/placebo
- Usually 2,000 to 10,000 patients, often in multi centres, including different air groups
- Lasts several years
- Provides data to support registration - 12Clinical trials: Phase 4: Ongoing clinical trials- Conducted once drug is licensed and on the market eg pharmacovigilance, post-market surveillance.
- Monitors consequences of increasing exposure
- Yields info on efficacy in sub-groups of the population - 13Drug regulatory bodiesUK: Medicines and healthcare regulatory agency
EU: European medicines agency
USA: Food and drug administration FDA
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- Pharmacology lecture 2 sources of drugs and their nature
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- Rose P
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