PHRM30003 Study Guide - Final Guide: Hair Loss, Microtubule, Kinase Insert Domain Receptor

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Drug name
Drug class
Molecular target(s)
Mechanism
/Function
/
AE/
Notes
Anti
-
HER
(5)
Tratuzumab
HER dimerization
inhibitor/Ab
Dimerised HER
HER2: no ligand
Cetuximab
Anti
-
EGFR
blocking Ab
HER
1
/EGFR
-
Anti
-
ligand blocking Ab
HER ligand
Erlotinib
Gefitinib
Lapatinib
Tyrosine kinase inhibitors
Tyrosine kinase
-
Ligand
-
toxin conjugates
HER
Cytotoxic Anti
-
cancer (4)
Cisplatin
Alkylating agents
Guanine in dsDNA
Bind covalently with nucleophilic cell
components (guanine)
Bifunctional: bis-alkylate two sites
simultaneously
Cross-linking of DNA intrastrand to
denature DNA
Treat testicular and ovarian cancer
Trans isomer is inactive
cannot form cross-linking
AE: dose-limitation
- Nephrotoxicity, neurotoxicity
- Nausea and vomiting
can be controlled with ondansetron
5HT3 antagonist
Methotrexate
Sulphonamide
Anti
-
metabolites
Non-biological DMARDs
Dihydrofolate
reductase (DHFR)
>>folate
Inhibit DNA synthesis
pathways
dTMP (thymidylate)
decrease synthesis of dihydrofolate,
tetrahydrofolate
lack of tetrahydrofolate disrupts the
conversion from dUMP to dTMP
Low
lipid solubility
do not cross BBB
AE:
- immunosuppression
- bone marrow depression
- GIT epithelium damage
- Resistance – use high dose + folate
5
-
fluorouracil
Anti
-
metabolites
dUMP
Inhibit DNA synthesis pathways
dTMP (thymidylate)
convert into false nucleotide
FdUMP
Directly inhibits thymidylate
synthetase
Administered with folate
(same as
MTX)
- Decrease toxicity
AE:
- GIT damage
- Bone marrow toxicity
Doxorubicin
An
thracyclines
(=cytotoxic anti-biotics)
DNA/topoisomerase
II complex
Topoisomerase II:
Unwind & rewind = nick & rejoin
o To relieve supercoiling
When doxorubicin intercalates DNA,
Topoisomerase II is able to nick dsDNA
AE:
- Bone marrow suppression
- Oxygen free radical – ROS
cardiotoxicity
can be reduced by co-administer
dexrazoxane, Fe chelator
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