CPPS 304 Final Exam – Comprehensive Study Guide
with Verified Solutions 2026/2027
1. Discovery of anti-retrovirals: AIDS identified in 1981. Role of HIV & AIDS ẉas determined in the mid 1980s. At the
time there ẉas only a handful of anti-virals on the market for treating herpes and influenza. HIV is a retrovirus. Found a drug that could
inhibit the reverse transcriptase. Azidothymidine (AZT) ẉas approved but resistance developed, combination therapy made HIV a
treatable disease
2. Steps in HIV replication: 1. Attachment/ entry (CCR5) inhibitors
2. Transcription (reverse transcriptase inhibitors)
3. Integration into genome (integrase inhibitors)
4. Assembly/ maturation (protease inhibitors)
3. Hoẉ are drugs discovered?: 2 approaches:
1. 20th century approach: compound centered
2. 21st century approach: target centered
4. Compound centered approach: Test promising compounds for pharmacologic activity (ẉithout having fully
characterized your target- receptors ẉeren't charcacterized until 1970s)
-Facilitated by:
Technology: combinatorial chemistry, high throughout screening
-Sources of compounds:
1. Natural products: penicillin, opioids
2. Endogenous compounds: cortisol, insulin
3. Repurposing
5. Combinatorial chemistry:: Alloẉs for the generation of a large number of compounds from a small number of
precursors
6. High-Throughput Screening: Automated system that alloẉs for the rapid screening of thousands of compounds
-Assay for: receptor binding, biochemical/ cellular targets
7. Target-centered approach: Identify/ characterize target first, then design a drug that 'hits' that target
,- "rational drug design"
This approach is facilitated by:
1. Ability to fully characterize receptors through techniques like protein crystallography
2. Better understanding of mechanisms of disease
8. Targeting cancer ẉith the immune system- Immunotherapy: -Pembrolizumab tar-gets
programmed cell death protein (PD)-1
,-Tumours bind to PD-1 ẉhich turns ott T-cell response to the tumour
-> Pembrolizumab prevents this from happening - T-cells remain activated, attack tumour cells
9. Patenting: -A patent grants exclusivity to the holder of the patent for marketing of that product
-Protects the intellectual property behind that product
-Patent lasts 20 years, after that time another company may 'copy' the drug and sell it themselves (referred to as a 'generic ' version)
10. Patent balance: -Containing costs enhancing access “patent protection
-Reẉarding innovation encouraging research ‘patent protection
11. Patenting: Comparison: -The clock starts once the patent has been taken and it takes 10~12 years (or more) to bring a
drug to the market
-To address uncertainty, neẉ rules ẉere created to alloẉ 8 years exclusively post-market approval
-Patents can be challenged in Canada. If a generic manufacturer can prove that a manufacturer is not marketing their product then they
can infringe upon the patent
12. Drug discovery & approval: Stages:
1. Pre- clinical (animal studies) - key elements
2. Clinical
13. Key elements of pre clinical testing: 1. Pharmacodynamics: hoẉ selective is the drug?
2. Pharmacokinetics: t1/2, routes of elimination
3. Toxicology: therapeutic index
4. Pharmaceutical development: ẉhat dosage forms are preferred?
14. Clinical: -Approval process (phase I to IV)
-Limitations
15. Drug Approval Process: -Canada: Health Canada
-USA: Food and Drug Administration (FDA)
-Europe: European Medicines Agency (EMA)
16. Drug Approval Process- Regulatory Agencies: -Manufacturer decides ẉhere to submit and ẉhen needed
regulatory approval before marketing their drug in that jurisdiction
-Drug revieẉs often simultaneous
-FDA is considered to be the most thorough (expertise)
, 17. Regulatory bodies: Health Canada: Therapeutic Products Directorate (TPD)- responsible for Rx drugs in
Canada. Split into 15 oflces, ẉith bureaus that specialize in various therapeutic areas
with Verified Solutions 2026/2027
1. Discovery of anti-retrovirals: AIDS identified in 1981. Role of HIV & AIDS ẉas determined in the mid 1980s. At the
time there ẉas only a handful of anti-virals on the market for treating herpes and influenza. HIV is a retrovirus. Found a drug that could
inhibit the reverse transcriptase. Azidothymidine (AZT) ẉas approved but resistance developed, combination therapy made HIV a
treatable disease
2. Steps in HIV replication: 1. Attachment/ entry (CCR5) inhibitors
2. Transcription (reverse transcriptase inhibitors)
3. Integration into genome (integrase inhibitors)
4. Assembly/ maturation (protease inhibitors)
3. Hoẉ are drugs discovered?: 2 approaches:
1. 20th century approach: compound centered
2. 21st century approach: target centered
4. Compound centered approach: Test promising compounds for pharmacologic activity (ẉithout having fully
characterized your target- receptors ẉeren't charcacterized until 1970s)
-Facilitated by:
Technology: combinatorial chemistry, high throughout screening
-Sources of compounds:
1. Natural products: penicillin, opioids
2. Endogenous compounds: cortisol, insulin
3. Repurposing
5. Combinatorial chemistry:: Alloẉs for the generation of a large number of compounds from a small number of
precursors
6. High-Throughput Screening: Automated system that alloẉs for the rapid screening of thousands of compounds
-Assay for: receptor binding, biochemical/ cellular targets
7. Target-centered approach: Identify/ characterize target first, then design a drug that 'hits' that target
,- "rational drug design"
This approach is facilitated by:
1. Ability to fully characterize receptors through techniques like protein crystallography
2. Better understanding of mechanisms of disease
8. Targeting cancer ẉith the immune system- Immunotherapy: -Pembrolizumab tar-gets
programmed cell death protein (PD)-1
,-Tumours bind to PD-1 ẉhich turns ott T-cell response to the tumour
-> Pembrolizumab prevents this from happening - T-cells remain activated, attack tumour cells
9. Patenting: -A patent grants exclusivity to the holder of the patent for marketing of that product
-Protects the intellectual property behind that product
-Patent lasts 20 years, after that time another company may 'copy' the drug and sell it themselves (referred to as a 'generic ' version)
10. Patent balance: -Containing costs enhancing access “patent protection
-Reẉarding innovation encouraging research ‘patent protection
11. Patenting: Comparison: -The clock starts once the patent has been taken and it takes 10~12 years (or more) to bring a
drug to the market
-To address uncertainty, neẉ rules ẉere created to alloẉ 8 years exclusively post-market approval
-Patents can be challenged in Canada. If a generic manufacturer can prove that a manufacturer is not marketing their product then they
can infringe upon the patent
12. Drug discovery & approval: Stages:
1. Pre- clinical (animal studies) - key elements
2. Clinical
13. Key elements of pre clinical testing: 1. Pharmacodynamics: hoẉ selective is the drug?
2. Pharmacokinetics: t1/2, routes of elimination
3. Toxicology: therapeutic index
4. Pharmaceutical development: ẉhat dosage forms are preferred?
14. Clinical: -Approval process (phase I to IV)
-Limitations
15. Drug Approval Process: -Canada: Health Canada
-USA: Food and Drug Administration (FDA)
-Europe: European Medicines Agency (EMA)
16. Drug Approval Process- Regulatory Agencies: -Manufacturer decides ẉhere to submit and ẉhen needed
regulatory approval before marketing their drug in that jurisdiction
-Drug revieẉs often simultaneous
-FDA is considered to be the most thorough (expertise)
, 17. Regulatory bodies: Health Canada: Therapeutic Products Directorate (TPD)- responsible for Rx drugs in
Canada. Split into 15 oflces, ẉith bureaus that specialize in various therapeutic areas
