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Question 1

what is drug discovery

Answer 1

a compound is found which is biologically active in the desired therapeutic area

Question 2

what is drug development

Answer 2

a compound discovered to be biologically active then has that activity and its toxically optimized for the clinic

Question 3

6 steps to drug discovery

Answer 3

1. observation of a beneficial effect
2. identification of component with positive attributes
3. identification of target
4. improved compound
5. formulation
6. development continues

Question 4

what is a me too compound

Answer 4

a drug containing an active pharmaceutical ingredient which is chemically related and very structurally similar to an existing API

Question 5

what design rationale does me too compounds use and how do they differ

Answer 5

• improvement of existing drugs
• series of derivatives were made based on the rationally designed drug

Question 6

5 things you look for when making me too compounds

Answer 6

1. avoid patent issue
2. improve efficacy
3. improve safety profile
4. allow for improved formulation which is easier to administer
5. improved physical properties which affects pharmacokinetic parameters

Question 7

7 pros of me too compounds

Answer 7

• high probability of ending up with an active molecule
• if enough copies are made then there is a good chance of finding a compound with an improvement on the efficient of the original
• show a different profile of adverse effects (e.g. improve safety profile)
• previous info about the original drug is available
• can work in patients who don’t react to original drug
• can be less expensive than the original or drive down prices
• occasionally, very different properties discovered

Question 8

4 cons of me too compounds

Answer 8

• not very innovative
• can be seen as simply a way of propping up the pharmaceutical industry with minimal effort
• patient are often difficult to get around and the original inventor will already have covered most variation
• unlikely to lead to any dramatic or radical improvement over existing treatments

Question 9

3 ways to increase half-life

Answer 9

• add groups which prevent elimination of molecule
• and/or increase binding strength of the compound
• addition of a halogen to block metabolite formation extends half-life