BPS 2110. Sample questions.
Which area of the following areas pharmaceutical industry holds the most promise for new
drugs in the next ten years? Support your choice.
- New antibiotics are needed because bacteria are becoming resistant, and not many
companies invest into making new antibiotics because they generate low profit
- Drugs that are used for pain are always needed, so this is a good area to get involved in.
- None of the drugs made today for dementia actually treat it, so this is a good field to
- New cancer drugs are needed as new cancers are being discovered.
- Personalized drugs are the future because people respond differently to different
- Stem cell research is huge
- New vaccines will always be needed because viruses change each year.
A tremendous need and opportunity exists for developing new drugs to slow down rate of
decline of patients suffering from dementia eg, Alzheimers disease.
Discuss the issues which made progress in this area slow at this time. What breakthrough(s) is
(are) needed to change the situation?
The drugs developed for Alzheimer’s disease do not cross the blood-brain barrier. Also,
alzheimer’s disease couldn’t be predicted in a patient until symptoms started to occur, so it is
hard to develop a drug that will cure alzheimer’s disease because it is hard to tell what the
source of the disease is. It was later discovered that genetics can tell a lot about a
predisposition to developing alzheimer’s disease – alzheimer’s genome project. From studying
the genetics, you can prevent the disease better.
Give the names and headquarters country of three of the top ten pharmaceutical companies in
1. Pfizer (USA)
2. Johnson&Johnson (USA)
3. Hoffman-Laroche (Switzerland) 4. Novartis (Switzerland)
Describe briefly the mode of action of Aspirin and explain why its action as an anti-inflammatory
agent is accompanied in many patients by gastrointestinal bleeding.
Aspirin is a drug that inhibits the formation of prostaglandins, which involves the enzyme COX.
This enzyme has two variants – COX1 and COX 2, where COX1 mediates the formation of
prostaglandins involved in important bodily functions such as the renewal of the stomach and
esophagus lining, and COX2 is associated with inflammation. When aspirin is taken by the
patient, both the enzymes are inhibited so that on one hand all inflammation is reduced, but the
stomach and esophagus lining formation is also inhibited causing gastrointestinal bleeding.
COX2 inhibitors were initially expected to act as anti-inflammatory agents without the typical
side effects associated with Aspirin [ASA] and the other NSAIDs such as Ibuprofen sold as Advil
or Motrin. Explain the basis of this expectation.
It was expected that if only the enzyme COX2 was inhibited and not COX1, that you could take
the drug to reduce inflammation without suffering from gastrointestinal bleeding because COX1
would still be active to renew the lining. However, when the drug only inhibited COX2 activity, it
increased the patient’s risk of developing colon cancer and was taken off the market.
Knowing the structure of lead structure published by the Dupont company, DuP697, and
suggest two additional compounds that you would expect to have significant COX-2 vs COX-1
selectivity. Your compounds cannot have a sulfur containing ring since such compounds would
obviously infringe on the Dupont patent.
The compounds have to be similar to DuP697 in size to be able to fit in the COX-2 receptor to
inhibit it but too big to fit in the COX-1 inhibitor. The structure can be altered by using a
nitrogenous 5-membered central ring, and by changing the substituents on the aromatic rings
from SO2CH3 to SO2NH2 or CF3
Generic companies produce drugs whose patents have expired. In order to obtain permission
from Health Canada to sell a particular drug what key property of the generic drug show
compared to the originally approved drug.
The drug must be bioequivalent. They must have the same active ingredients and must have
Question 8. a) What key questions are addressed in a Phase 1 Clinical Trial? In a phase II Clinical trial?
In a Phase III Clinical trial?