Chemo 6 Flashcards
What are the Bcr-Abl Tyrosine Kinase inhibitors?
What do they treat?
- Imatinib and Dasatinib
- CML
how does Imatinib work?
it occupies the APT cofactor binding site on Bcr-Abl, inhibiting transfer of phosphate to tyrosine on substrates
What is Dasatinib used for?
treatment of primary and imatinib resistant CML
What is the mechanism of imatinib resistance
-involves mutation of the ATP binding pocket to exclude imatinib
Imatinib targets what other tyrosine kinases
-c-kit and PDGFR
Dasatinib targets what other tyrosine kinases?
-Src family
Imatinib can be used for what cancer other than CML
GIST
Dasatinib can be used for what other cancer other than CML
ALL with Ph chromosome
85% of GIST tumors contain oncogenic forms of what tyrosine kinases
-KIT or PDGFR
What do you use for imatinib resistant GIST
Sunitinib
What are the adverse drug reactions with imatinib
due to hepatic CYP450 - rifampin and St. John’s wort hasten the clearance of it
HER2 overexpression
Breast cancer
What drugs inhibit only EGFR?
used for what cancer?
- Gefitinib
- Erlotinib
-NSCLC
What drug inhibits both EGFR and HER2?
What cancer?
Lapatinib
-Breast Cancer
what 2 drugs inhibit both PDGFR and VEGFR
- sunitinib
- sorafenib
What cancers do you used sunitinib for?
- GIST
- RCC
What cancers do you use Sorafenib for
- RCC
- HCC
What does Vemurafinib inhibit
-Mutant BRAF V600E
what cancer is Vemurafenib used for
metastatic malignant melenoma
What are the antibodies that target EGFR receptor?
what cancer?
- Cetuximab (colorectal, head and neck)
- Panitumumab (colorectal)
-don’t work if there is KRAS mutations
What is the antibody that targets Her2 receptor?
what cancer?
Trastuzumab
breast with Her2 mutation
What is the antibody that targets VEGF LIGAND?
what cancer?
Bevacizumab
RCC
why are some cancers with Ras mutation not affected by certain tyrosine kinase inhibitors
they by pass that receptor and affect down stream signal
What drug blocks angiogenesis used for advanced solid tumors
Bevacizumab
