Misc 1: Kinase Inhibitors Flashcards
Name the 5 tyrosine kinase inhibitors
Imatinib, geftinib, erlotinib, nilotinib, and dasatinib
Name the 2 serine/threonine kinase inhibitors
Vemurafenib and dabrafenib
Which kinase inhibitor acts on MEK (mitogen-activated protein kinase kinase)?
Trametinib
Which 2 tyrosine kinase inhibitors act on EGFR (epidermal growth factor receptor)?
Geftinib and erlotinib
Imatinib, nilotinib, and dasatinib can all inhibit which tyrosine kinase?
Abl kinase
What drug can inhibit Abl kinase, as well as the PDGFR and c-kit proteins?
Imatinib
What 2 cancers is imatinib used to treat?
CML (first line therapy for) and GIST (gastrointestinal tumor)
What 2 tyrosine kinase inhibitors are used to treat imatinib-resistant CML, and how are they given?
Nilotinib and dasatinib, given orally
What cancer is linked to EGFR, which can be inhibited by geftinib and erlotinib?
Non-small-cell lung cancer
Which drug, used to inhibit Abl kinase, can cause QT prolongation, hepatotoxicity, and electrolyte abnormalities as side effects?
Nilotinib
What are 3 characteristic side effects of using dasatinib?
Bleeding, fluid retention, and pulmonary artery hypertension
What 2 kinases does dasatinib inhibit?
Abl and src
Name one characteristic side effect of imatinib treatment.
Fluid retention (muscle cramps and arthralgia are also listed in the excel table, but UpToDate doesn’t list them as very common)
Vemurafenib, dabrafenib, and trametinib are all used to treat what specific kind of cancer?
Unresectable stage III/IV/metastatic melanomas with BRAF mutations
What 2 drugs inhibit oncogenic BRAF kinase?
Vemurafenib and dabrafenib
Vemurafenib has been shown to be superior to dacarbazine in Phase III trials treating what kind of cancer?
Malignant melanoma
What kinase inhibitor drug can cause side effects such as QT prolongation, arthralgia, photosensitivity, alopecia, and increased risk of developing skin cancers?
Vemurafenib
Besides skin toxicity and carcinogenesis, what are 3 unusual side effects of using the serine/threonine kinase inhibitor dabrafenib?
Eye inflammation, hyperglycemia, male sterility
What drug, used to treat melanoma, can cause diverse side effects including skin toxicity, cardiomyopathy, interstitial lung disease, retinal disorders, and female sterility?
Trametinib
