Anti Cancer Therapy

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Methotextrate? 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
MERcaptopurine: 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
Cladribine?: 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?: Glucocorticoids
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
5-FU First active metabolite: FdUMP
forms a covalent ternary complex with thymidylate synthase and N5,10 methyltetrahydrofolate
Thymidilate is not synthesized and DNA syn is inhibited
FUTP: Incorporated into RNA
Interferes with mRNA processing and mRNA transistion
FdUTP: Incorporated into DNA and inhibits DNA synthesis
Capecitabine: Flouropyrimidine carbamate prodrug, used for met breast cancer
What converts capecitabine into floururacil in the liver?: thymidine phosphorylase
Cytarabine: 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?: AML
What are the five plant alkaloids?: Vinblastine, vincristine, etoposide, topotecan, Paclitaxel
Vinblastine?: 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
Vincristine? 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
Etoposide?: 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
Topotecan?: 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?: AML
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
Bleomycin?: Small peptide with a DNA binding region at on end and an iron binding region at the other
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
Flutamide?: Antiandrogen effects via binding to the androgen receptor Prostate cancer
Leuprolide?: 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
Anastrozole?: nonsteroidal Aromatase inhibitor, good for breast cancer in women
Exemestane?: Hormone that irreversibly inhibits aromatase--
Imatinib?: Inhibits oncoprotein tyrosine kinase-these promote abnormal proliferation and anti-apoptotic pathways
Tumor cell markers?: Bcr-Abl (CML)
c-kit (GI stromal tumors)
Asparginase: Bacterial derived enzyme-hydrolyzes L-asparganine to aspartic acid and ammonia

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Number of cards 51