Drug Design and Synthesis

Tutorial 1
CH215
1. How long does it take (on average) to develop a new drug? Approximately how

much does it cost? How long does a patent on a new drug last?

2. Before being permitted to market a drug in the USA, a pharmaceutical company

must submit a successful New Drug Application (NDA). What information about the

drug is the NDA expected to contain?

3. Drugs may be active at mammalian and non-mammalian targets. (a) What two

types of cellular proteins account for the majority of human drug targets? (b) Give an

example of non-mammalian target.

4. In what way has the chemical nature of top selling drugs (in gross sales) changed

over the last 10 years?

 5. Using a named example such as HIV, to illustrate your answer, outline the conventional

strategies that have been used to identify new drug targets.

6. List THREE technologies that are used to investigate the molecular basis of human

disease. For ONE of these technologies, explain how it is used in drug discovery and

a limitation for its use.

7. Define the terms “assay” and “screen” in relation to the process of identifying

“hits” during drug discovery and give one example of each (4 marks).
 8. (a) In relation to a drug screening cascade, define a lead compound.

(b) Provide FOUR properties desirable in a lead compound.

9. Provide THREE key differences between Phase 1 and Phase 2 drug

metabolism actions:

10. Provide THREE differences between “drug-like” small molecules and biologic drug

compounds.
 11. (a) Name FOUR properties a compound must have in order to go into lead

optimization

11 (b). Provide ONE reason which is NOT related to the properties you describe in (a)

why chemical modification of a lead compound may be required.

12. Define “primary”, “secondary” and “tertiary” assay within a typical lead

optimization biological screening cascade.

6. Give TWO limitations associated with using ligand binding assays.

 13. a. Define the term, bioavailability.

13 b. How is bioavailability measured?

13 c. Provide TWO factors that could affect the bioavailability of an orally administered drug.

14. Give TWO examples of what an ethical review panel must determine and approve prior
to submission of a project license application.