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Drug Design Chapter 2:
Drug Discovery, Design, and
Development (Part 1)
- 1. Drug Discovery
- Before 19th century:
drugs were mainly
herbs and potions
- Mid 19th century:
scientists attempted
to isolate and purify
active components
- Mid 19th century:
scientists attempted
to isolate and purify
active components
- A. Statistics
- Average time
to market:
12-15 years
- Average cost:
$600-800 billion
- Cost to get
on market
today: $1.2
billion
- Average time
to market:
12-15 years
- B. Choosing a
Disease
- How are target disases
chosen? Logical...
Practical...
- How are target disases
chosen? Logical...
Practical...
- C. Clinical
Trials
- Before clinical trials...
- 1) in vitro and
in vivo testing
on cell cultures
or transgenic
mice
- 2) test on
lab animals
for several
months
- 2) test on
lab animals
for several
months
- 1) in vitro and
in vivo testing
on cell cultures
or transgenic
mice
- Four Phases
of Clinical
Trials
- Phase 1: healthy volunteers
- Phase 2: small group of volunteers
- Phase 3: larger group of patients
- Phase 4: never-ending
- Drug can
be licensed,
marketed,
and
prescribed
- Phase 4: never-ending
- Phase 3: larger group of patients
- Phase 2: small group of volunteers
- Phase 1: healthy volunteers
- Before clinical trials...
- Before 19th century:
drugs were mainly
herbs and potions
- 2. Finding a Lead
Compound
- Prototype
Compound
- Drug
Candidate
- Clinical
Drug
- Clinical
Drug
- Drug
Candidate
- A) No Lead
Compound
(Serendipity)
- 1) Penicillins
- bacteria culture
accidentally
contaminated
with a mold
- bacteria culture
accidentally
contaminated
with a mold
- 2) Mustard
Gas
- led to first
chemotherapy
drug, mustine
- led to first
chemotherapy
drug, mustine
- 3) Cisplatin
- inhibited bacterial
cell division when
electric field was
applied
- inhibited bacterial
cell division when
electric field was
applied
- 1) Penicillins
- B) Lead
Discovery
- bioassay: test system
- in vitro tests: cells, tissues,
enzymes, receptors
- in vivo tests: animals
- bioassay: test system
- C) Random
Screening
- all compounds
tested in
bioassay,
regardless of
structure
- synthetic chemicals
- natural products
- "War on Cancer" allowed new
compounds to be screened for free
- synthetic chemicals
- all compounds
tested in
bioassay,
regardless of
structure
- D)
Nonrandom
Screening
- targeted screening
- budget concerns
- looking for
weak activity or
similar
structures
- targeted screening
- E)
Metabolites
- in vivo drug
degradation
products
- often in
active
compound
- often in
active
compound
- in vivo drug
degradation
products
- F) Clinical
Observations
- observe side
effects of
drugs in
clinical trials
- Example:
Dramamine
- Example:
Dramamine
- observe side
effects of
drugs in
clinical trials
- G) Rational
Approaches
- "computer-aided
design"
- 1) Identify cause of the disease
- 2) Design molecules which correct an
imbalance or stop cell growth
- 2) Design molecules which correct an
imbalance or stop cell growth
- "computer-aided
design"
- Prototype
Compound
- 3. Lead
Modifications
- (continued in part 2 of Chapter 2)
- (continued in part 2 of Chapter 2)
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