Antimetabolites Flashcards
What is the MOA of antimetabolites, what part of the cell cycle do they arrest, and what type of cell is most susceptible to these?
Mimic or reduce normal cell comments necessary for DNA, RNA and protein synthesis
S phase
Rapidly dividing
3 mechanisms of resistance to antimetabolites?
Don’t let these guys metabolize to active forms
Stop transporting
Lower FPGS
1 unique adverse effect of antimetabolites?
Hand foot syndrome, painful swelling of hands and feet.
2 cancers we use methotrexate for?
Breast and NHL
2 cancers to treat with pemetrexed?
Mesothelioma
NSCLC
What cancer do we treat with pralatrexate?
T cell lymphoma
What drug is the most widely used chemo drug against colorectal cancer? What else does this drug work well against as far as cancers?
5 fu
Variety of solid tumors
What is capecitabine metabolized into, what are two cancers it is used for, and what is the regimen it is part of with what drug to treat what cancer?
5FU
Metastatic breast and colorectal
XELOX where it is combined with oxaliplatin as first line treatment for colorectal metastatic cancer
What cancer do we use TAS 102 for?
Colorectal
What cancers do we use cytarabine for and what cancers does it have no activity for?
Blood cancers like AML and NHL
No activity against solid tumors
What can we use gemcitabine for?
Solid and hematologists cancers
The thiopurines are metabolized by what enzyme and loss of this enzyme leads to what?
TPMT
If we don’t have this those drugs are hanging around causing their adverse effects stronger and longer. Myelosuppression and GI
What do we use 6 mercaptopurine for, what cancer?
Childhood AL
What cancer do we treat with 6 thioguanine?
Adult acute leukemia
Big time adverse effect of fludrarabine and what do we need to do about it?
Potent immunosuppressant. Increased risk of opportunistic infection. Pneumocystis jiroveci pneumonia. Need to give TMP/SMX
