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52 Cards in this Set

  • Front
  • Back
Site of action?
Folic acid antagonist
Binds to catalytic site of dihydrofolate reductase
interfers with DNA, RNA, and protein syn.
What is retained in cancer cells?
Polyglutamates of MTX are retained within tumor cells
What is administered to reduce action of methotextrate on normal cells?
Leucovorin rescue
What is method of resistance to methotextrate?
decreased drug transport, decreased polyglutamate formation, Increased DHFR synthesis, decreased affinity of DHFR for MTX
Metabolized by hypoxanthine guanine phosphoribosyl transferase to the nucleotide form
What is the nucleotide form of Mercaptopurine?
6-Thioinosinic acid-inhibits enzymes in purine nucleotide pathway
Method of resistance?
decreased HPGRT activity,
Why must you reduce 6-MP with allopurinol?
6-MP is converted to inactive form by Xanthine Oxidase, without this you get a build up of drug
The intermediate form which is formed by 2-CAMP is resistant to adenosine deaminase, incorporated into DNA leading strands
What is the other method of action?
Build up of deoxynucleotide that prevents DNA repair
What drugs work at the M phase?
Inhibitors of microtubule function
Miotic phase, cell division
What drugs work at the G0 phase?
What drugs work at the S phase?
Antimetabolites, and folate pathway inhibitors
What drug works at both S phase and G2 phase?
Topoisomerase inhibitors
What drugs work at G2 phase?
Antitumor antibiotics
First active metabolite
forms a covalent ternary complex with thymidylate synthase and N5,10 methyltetrahydrofolate
Thymidilate is not synthesized and DNA syn is inhibited
Incorporated into RNA
Interferes with mRNA processing and mRNA transistion
Incorporated into DNA and inhibits DNA synthesis
Flouropyrimidine carbamate prodrug, used for met breast cancer
What converts capecitabine into floururacil in the liver?
thymidine phosphorylase
Metabolized into active metabolite active triphosphate nucleotide, AraCTP
What part of cell cycle does Cytarabine work on?
The S phase, competitively inhibits DNA polymerase and interferes with chain elongation.
What is cytarabine used to treat?
What are the five plant alkaloids?
Vinblastine, vincristine, etoposide, topotecan, Paclitaxel
Derved from th periwinkle plant, depolymerizes microtubule
What phase does vinblastine work in?
Mitotic arrest in metaphase----used for hodgkins disease, non-hodgkins lymphoma and breast cancer
What is it used to treat?
related to vinblastine, AML, Hodgkins disease and non-hodgkins lymphoma, pediatric tumors---ewing's sarcoma and wilm's tumor
semisynthetic derivative from mayapple root
What stage does etoposide work at?
block cell division in late s-G2 phase of cell cycle INhibits topoisomerae II resulting in DNA strand breakage
What is it used to treat?
Germ cell cancer, lung cancer, hematologic malignancies and gastric cancer
Derived from the camptotheca acuminata tree.
What does topotecan work on?
topoisomerase I-used for cutting and re-ligating single DNA strands
What is topotecan used for?
Advanced ovarian cancer
What is paclitaxel?
A taxane, dervied from the Yew tree
HOw does it work?
Binds microtubules and enhances tubulin polymerization-results in the inhibition of mitosis and cell division-excreted in the feces-----used for solid tumors
What antibiotics are used for cancer treatment?
Doxorubicin, daunorubicin, dactinomycin, mitomycin and bleomycin
What are the four mech of action of doxorubicin and daunorubicin?
Inhibit topoisomerase two, DNA binding and inhibition of DNA synthesis, Bind cell membrane and alter fluidity and ion transport, and generation of ROS
What is Doxorubicin used for?
broad spectrum against hematologic malignancies and solid tumors
What is Daunorubicin used for?
What is mech of action of Dactinomycin?
binds DNA synthesis between adjacent guanine cytosine base pairs inhibiting RNA synthesis----Pediatric tumors
What is mech of action of Mitomycin
Metabolized into an alkylating agent that cross links DNA--hypoxic tumor stem cells of solid tumors are particularly susceptible
Small peptide with a DNA binding region at on end and an iron binding region at the other
How does it work?
Binds DNA and the iron compoennt becomes oxidized leading to chromosomal abnormalities
What is up with it being a CCS drug?
Causes accumulation of cells in the G2 phase, must be careful in people with renal insufficiecny
HOw does tamoxifen work?
Binds the estrogen receptor of estrogen dependent tumors, 10 fold lower affinity than estradiol, endogenous estrogen must be ablated for optimal effect
Antiandrogen effects via binding to the androgen receptor Prostate cancer
GNRH analog, causes a transient release of FSH and LH followed by desensitization of the receptor, decreases FSH and LH release, good for prostate cancer
nonsteroidal Aromatase inhibitor, good for breast cancer in women
Hormone that irreversibly inhibits aromatase--
Inhibits oncoprotein tyrosine kinase-these promote abnormal proliferation and anti-apoptotic pathways
Tumor cell markers?
Bcr-Abl (CML)
c-kit (GI stromal tumors)
Bacterial derived enzyme-hydrolyzes L-asparganine to aspartic acid and ammonia