Misc 1: Kinase Inhibitors

Question 1

Name the 5 tyrosine kinase inhibitors

Answer 1

Imatinib, geftinib, erlotinib, nilotinib, and dasatinib

Question 2

Name the 2 serine/threonine kinase inhibitors

Answer 2

Vemurafenib and dabrafenib

Question 3

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

Answer 3

Trametinib

Question 4

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

Answer 4

Geftinib and erlotinib

Question 5

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

Answer 5

Abl kinase

Question 6

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

Answer 6

Imatinib

Question 7

What 2 cancers is imatinib used to treat?

Answer 7

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

Question 8

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

Answer 8

Nilotinib and dasatinib, given orally

Question 9

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

Answer 9

Non-small-cell lung cancer

Question 10

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

Answer 10

Nilotinib

Question 11

What are 3 characteristic side effects of using dasatinib?

Answer 11

Bleeding, fluid retention, and pulmonary artery hypertension

Question 12

What 2 kinases does dasatinib inhibit?

Answer 12

Abl and src

Question 13

Name one characteristic side effect of imatinib treatment.

Answer 13

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

Question 14

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

Answer 14

Unresectable stage III/IV/metastatic melanomas with BRAF mutations

Question 15

What 2 drugs inhibit oncogenic BRAF kinase?

Answer 15

Vemurafenib and dabrafenib

Question 16

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

Answer 16

Malignant melanoma

Question 17

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

Answer 17

Vemurafenib

Question 18

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

Answer 18

Eye inflammation, hyperglycemia, male sterility

Question 19

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

Answer 19

Trametinib