Drug discovery (1) Flashcards

1
Q
A
  • POM =>
  • P MEDS =>
  • OTC N
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2
Q

Cimetidine

A
  • Cimetidine is a histamine H2 antagonist original used to treat peptic ulcers
  • Cimetidine was discovered at Smith, Kline, French by James Black, Robert Ganellin and others
  • Cimetidine was first licensed in the UK in 1976 and approved by the FDA in 1979
  • It was marketed by GSK under trade name Tagamet
  • Generic cimetidine is now available
  • Now available in OTC medicines treating heartburn symptoms
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3
Q

Top 20 best selling drugs

A
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4
Q

Top 10 pharmaceutical companies

A
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5
Q

Naming drugs

A
  • A marketed drug may have up to 4 names: Chemical name, company code, brand and generic name
  • Prefixes differentiate one drug from another but have no other meaning- normally come from there MOA
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6
Q

DRUG DISCOVERY

A
  1. Targets, Screening and compound= 2-3years
  2. Leads => project = 2-5 years
  3. Clinical trials (regulatory approval)= 6-7 years
  • Hit- appropriately targets the protein
  • Lead is a compound you can change which will change the reactivity
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7
Q

Clinical trials and there phases

A
  1. Human replacing pre-clinical animal data; called microdosing at subther (trial size = 10-15)
  2. Safety evaluation; Safe dosage; range; side effects (Trial size= 20-80)
  3. Effectiveness and dose response (Trial size= 100-300)
  4. Effectiveness; side-effects, compare to other treatments (Trial size= 1000-5000)
  5. Post-marketing; effect in general population; rare side effects; optimise protocols; pharmacogenomics (Size= patient population)
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8
Q

Drug stages with cost

A
  • Cost of developing a new drug range from $4 billion to $12 billion
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9
Q

Attrition

A
  • Attrition of drug discovery programmes at each stage from idea to Phase III CT is a fundamental property of Pharma R&D
  • Thousands of biological targets get smaller and smaller to eventually one marketed drug
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10
Q

Fiscal trajectory of a drug

A
  • Saviours
    • Biological vaccines
    • Personalised medicine
    • Drug repurposing
  • Patents expired for drugs worth $250 billion between 2011-15
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11
Q
A
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