VERIFIED 2025 LATEST EDITION.
previously salicylic acid was used but was vey hard on stomach
Discovery process of aspirin: - also used to burn off warts. Felix Hoffman added an acetyl
group to SA to make acetylsalicylic acid (ASA)
HIV/AIDS is a retrovirus and the key enzyme in its replication
why was an anti-retroviral drug
needed? was a reverse transcriptase
- attachment/entry (CCR5 inhibitor)
- transcription (reverse transcriptase inhibitors)
Steps of HIV replication
- integration
into genome (integrase inhibitors)
- assembly/maturation (protease inhibitors)
Azidothymidine (AZT) was previously used as an anti-cancer
drug that had been shelved due to poor results. then they
anti-retroviral drugs
discovered its use in treating HIV, but
resistance quickly developed and other therapies joined AZT. By
1996 combination therapy made HIV a very treatable disease.
What are the 2 fundamental - compound-centered (20th century)
approaches to how drugs are - target-centered (21st century)
discovered?
test promising compounds for pharmacologic activity without
Compound centered approach
having fully characterized your target
how is the compound centered technology (combinatorial chemistry and high throughout screening)
approach facilitated?
- naturalproducts (penicillin and opioids)
sources of compounds for
- endogenous compounds (cortisol and insulin)
compound- center approach?
- re-purposing
allows fir the generation of a large number of compounds from
combinatorial chemistry
a small number of precursors
automated system that allows for the rapid screening of
high throughput screening
thousands of compounds . Assay for: receptor binding and
biochemical/cellular targets
identify/characterize target first, then design a drug that 'hits'
Target centered approach
that target (rational drug design)
, - ability to fully characterize receptors through
Target centered approach is techniques like protein crystallography
facilitated by - better understanding of mechanisms of disease
pembrolizumab targets programmed cell death protein (PD-1)
Targeting cancer with the immune - tumors normally bind to PD-1 which turns off T-cell response to the
system (Immunotherapy) tumor
- pembrolizumab prevents this from happening and t-cells
remain activated and attack tumor cells
What is a patent? it grants exclusivity to the holder for the marketing of that product
in Canada, they last for 20 years from the date of issue. After that time,
how long does a patent last?
another
company may 'copy' the drug and sell it themselves (referred to as a generic
version)
containing costs and enhancing access (lowering patent protection)
patenting balance
vs rewarding innovation and encouraging research (increasing
patent protection)
if a generic manufacturer can prove that a manufacturer is not
when can a patent be challenged?
marketing their product then they can infringe upon it
1) pre-clinical (animal studies)
Stages for Drug Approval
2) clinical (approval process phase I to IV, limitations)