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CMOD Week 7 > Targeted Therapies > Flashcards

Flashcards in Targeted Therapies Deck (27)
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1
Q

What is a Philadelphia chromosome?

A

Results in a fusion protein tyrosine kinase that drives CML

2
Q

What percentage of most cancers are due to identifiable cancer susceptibility genes?

A

5-10% are genetic, heredited

3
Q

Which BRCA gene is most commonly mutated in African Americans?

A

BRCA II (Jews- BRCA1)

4
Q

What mutation would lead to GIST?

A

upregulation of c-kit which acts mainly via the RAS/RAF/MEK/ERK pathway

can treat with Gleevec

symptoms: decreased appetite, early satiety, and need to expand his belt.

5
Q

What is c-kit? Pathway?

A

transmembrane receptor that is activated by the ligand ScF (stem cell factor)

acts through RAS/RAF/MEK/ERk and also produces AKT which helps dissociate APC from B-catenin so it can enter the nucleus

6
Q

Fact about metastatic lung cancer.

A

In some patients pill produce better responses than intravenous drugs

5 yr survival rate about 2%

Once in the brain, it can be cured.

Asians and Americans have a different disease

7
Q

EGFR kinase mutation is common in which cancers?

A

lung cancer. Upregulated

Activating mutations present in 5% smokers, 15% non smokers, and 50% never smokers with adenocarcinoma

8
Q

Risk factors for EGFR mutations?

A

female, young, Asian, non-smoker

9
Q

How could you treat EGFR mutation?

A

Erlotinib (Tarceva)

10
Q

EML4-ALK fusion mutation causes what?

A

adenocarcinoma lung cancer

present in about 5% of lung cancers

11
Q

Risk factors for EML4-ALK mutation?

A

increased in never smokers, Asian, females

12
Q

How would you treat a EML4-ALK mutation?

A

Crizotinib- 57% response- better than chemo

13
Q

Describe the EGFR pathway.

A

Ligand (EGF, TGFa) bind to receptor, causing it dimerize and act via a JAK/STAT pathway to promote cell growth and proliferation

mutated (from hereditary or smoking, etc.)= over-expressed=tumor risk

14
Q

What drug can block ligand binding to EGFR?

A

Cetuximab (monoclonal antibody)

15
Q

What drug can prevent autophosphorylation of JAK?

A

Geftinib

16
Q

Facts about brain cancer.

A

Not all are fatal

There are 4 WHO grades of gilomas

gliomas are the most common brain neoplasm

17
Q

What are the most common brain neoplasms?

A

gilomas

WHO Grade I-II considered benign, Grade III-IV considered malignant.

Grade IV= giloblastoma (looks like a single ring-enhancing lesion)

18
Q

How does VEGF-A work?

A

via a VEGFR2 receptor (on vessel walls) and RAS/RAF/MEK/ERK pathway that causes cell proliferation and blood vessel formation

19
Q

How can VEGF be prevented from binding to mutated, over-expressed VEGF receptors?

A

Bevacizumab (Avastin)

20
Q

What does Sunitinib do?

A

used in renal cancer to block auto-phosphorylation of JAK in VEGF pathway

21
Q

What medicine can block an estrogen receptor?

A

Tamoxifen

22
Q

What is Everolimus?

A

mtor inhibitor that can be added to tamoxifen in hormone therapy failure in metastatic breast cancer

23
Q

What is Trastuzumab?

A

can block the HER-2 NEU receptor in breast cancer

24
Q

What is the pathway used in prostate regulation?

A

androgen pathway. ligand is testosterone

25
Q

What drug blocks androgen receptors?

A

Enzalutamide (Zytiga)

26
Q

What does Vemurafenib treat?

A

BRAF V600E/K mutation common in melanomas

27
Q

What is a hedgehog inhibitor?

A

Vismodegib