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25 Cards in this Set

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Who would benefit from Iressa treatment?
1) Lung and breast cancer patients who overexpress EGFr-erbB1/HER1??????? 2) adenocarcinoma and bronchoalveolar carcinoma 3) responders got rash… 4) non-smokers.
Does Iressa improve the response to other chemotherapy?
What is the mechanism of action of Iressa?
binds to the tyrosine kinase domain and blocks ATP binding on the TKR
What are the notable toxicities of Iressa?
Diarrhea, rash and acne
What is the receptor target for Iressa?
EGFr erbB1/HER1
In general, what are 2 things we consider in pharmacogenetics?
1. Is there a viable target (is that target something being misexpressed or overexpressed in a patient)… 2. Variability in drug metabolism of enzymes (Does the patient over or under-metabolize the drug, e.g., toxicity or active metabolite)
What two pharmacogenomics do we consider in EGFr inhibiting cancer drugs?
Expression of EGF receptor, and a metabolism consistent with drug metabolite
What mechanism would explain the response of some patients to Iressa?
Responder have a mutation in the ATP binding site of the EGFr tyrosine kinase domain… 2) these mutated EGF receptors respond are inhibited more compared to wild-type receptors… 3) mutant EGF receptors are constitutively active
In which cases does Iressa work best?
Gene amplification?
Does Iressa prolong life?
While Iressa does not prolong life for lung cancer patients, what drug does prolong life?
Erlotinib (which is similar to Iressa)
Which cancer type is Alimta suggested for treatment?
Lung: Mesothelioma and non-small cell lung cancer
What is used in combination with Alimta for treatment of Mesothelioma?
What is used in combination with Alimta for treatment of non-small cell lung cancer?
None… Alimta is used as a single agent
Why, if Alimta and Docetaxol have similar response rate, is Alimta preferred? (three reasons)
1. less leukopenia and neutropenia… 2. Less febrile netruopenia… 3. Less infection with grade 3/4 neutropenia
How is RAS important in explaining why Iressa may not work?
If RAS is constitutively active it doesn’t matter what you do to the receptor protein tyrosine kinase, because RAS is downstream.
Who would benefit from Herceptin treatment?
Breast cancer patients that overexpressed erbB2 Receptor
What kind of receptor is the erbB2 Receptor?
Heterodimerizing-activating TKR
What receptor does Iressa target?

What is the two step mechanism of Iressa?

What is also believed to be inhibited by Iressa?
1) erbB2/Her2

2) mAb binds the erbB2 receptor kinase domain --> followed by CdK inhibition

3) Herceptin may also suppress angiogenesis
Who would benefit from Tamoxifen treatment?
breast cancer patients that overexpressed estrogen receptors
What is the mechanism of action of Tamoxifen?
Competitive inhibitor of estrogen @ estrogen receptors
What are the proposed mechanisms of action for EGFr tyrosine kinase inhibitors? (hint: 5 decrease, and 2 increase)
reduces: proliferation, invasion, metastasis, agiogenesis, and adhesion… Increases: apoptosis and sensitivity to chemotherapy.
What would explain why non-smokers responded to Iressa?
Their cancer may have arisen primarily due to EGFr tyrosine kinase overexpression
What type of mutation is seen in the EGFR of Iressa (Gefitinib) responders?
Mutation in the tyrosine kinase (ATP) binding site
What type of cancers respond to Iressa? (Hint: histopathology)
Adenocarcinoma of lung, and Bronchioalveolar carcinoma