Misc 1: Kinase Inhibitors Flashcards Preview

Unit 1: Pharm > Misc 1: Kinase Inhibitors > Flashcards

Flashcards in Misc 1: Kinase Inhibitors Deck (19)
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1
Q

Name the 5 tyrosine kinase inhibitors

A

Imatinib, geftinib, erlotinib, nilotinib, and dasatinib

2
Q

Name the 2 serine/threonine kinase inhibitors

A

Vemurafenib and dabrafenib

3
Q

Which kinase inhibitor acts on MEK (mitogen-activated protein kinase kinase)?

A

Trametinib

4
Q

Which 2 tyrosine kinase inhibitors act on EGFR (epidermal growth factor receptor)?

A

Geftinib and erlotinib

5
Q

Imatinib, nilotinib, and dasatinib can all inhibit which tyrosine kinase?

A

Abl kinase

6
Q

What drug can inhibit Abl kinase, as well as the PDGFR and c-kit proteins?

A

Imatinib

7
Q

What 2 cancers is imatinib used to treat?

A

CML (first line therapy for) and GIST (gastrointestinal tumor)

8
Q

What 2 tyrosine kinase inhibitors are used to treat imatinib-resistant CML, and how are they given?

A

Nilotinib and dasatinib, given orally

9
Q

What cancer is linked to EGFR, which can be inhibited by geftinib and erlotinib?

A

Non-small-cell lung cancer

10
Q

Which drug, used to inhibit Abl kinase, can cause QT prolongation, hepatotoxicity, and electrolyte abnormalities as side effects?

A

Nilotinib

11
Q

What are 3 characteristic side effects of using dasatinib?

A

Bleeding, fluid retention, and pulmonary artery hypertension

12
Q

What 2 kinases does dasatinib inhibit?

A

Abl and src

13
Q

Name one characteristic side effect of imatinib treatment.

A

Fluid retention (muscle cramps and arthralgia are also listed in the excel table, but UpToDate doesn’t list them as very common)

14
Q

Vemurafenib, dabrafenib, and trametinib are all used to treat what specific kind of cancer?

A

Unresectable stage III/IV/metastatic melanomas with BRAF mutations

15
Q

What 2 drugs inhibit oncogenic BRAF kinase?

A

Vemurafenib and dabrafenib

16
Q

Vemurafenib has been shown to be superior to dacarbazine in Phase III trials treating what kind of cancer?

A

Malignant melanoma

17
Q

What kinase inhibitor drug can cause side effects such as QT prolongation, arthralgia, photosensitivity, alopecia, and increased risk of developing skin cancers?

A

Vemurafenib

18
Q

Besides skin toxicity and carcinogenesis, what are 3 unusual side effects of using the serine/threonine kinase inhibitor dabrafenib?

A

Eye inflammation, hyperglycemia, male sterility

19
Q

What drug, used to treat melanoma, can cause diverse side effects including skin toxicity, cardiomyopathy, interstitial lung disease, retinal disorders, and female sterility?

A

Trametinib