Anti Cancer Therapy

Front 1

Methotextrate?
Site of action?

Back 1

Folic acid antagonist
Binds to catalytic site of dihydrofolate reductase
interfers with DNA, RNA, and protein syn.

Front 2

What is retained in cancer cells?

Back 2

Polyglutamates of MTX are retained within tumor cells

Front 3

What is administered to reduce action of methotextrate on normal cells?

Back 3

Leucovorin rescue

Front 4

What is method of resistance to methotextrate?

Back 4

decreased drug transport, decreased polyglutamate formation, Increased DHFR synthesis, decreased affinity of DHFR for MTX

Front 5

MERcaptopurine

Back 5

Metabolized by hypoxanthine guanine phosphoribosyl transferase to the nucleotide form

Front 6

What is the nucleotide form of Mercaptopurine?

Back 6

6-Thioinosinic acid-inhibits enzymes in purine nucleotide pathway

Front 7

Method of resistance?

Back 7

decreased HPGRT activity,

Front 8

Why must you reduce 6-MP with allopurinol?

Back 8

6-MP is converted to inactive form by Xanthine Oxidase, without this you get a build up of drug

Front 9

Cladribine?

Back 9

The intermediate form which is formed by 2-CAMP is resistant to adenosine deaminase, incorporated into DNA leading strands

Front 10

What is the other method of action?

Back 10

Build up of deoxynucleotide that prevents DNA repair

Front 11

What drugs work at the M phase?

Back 11

Inhibitors of microtubule function
Miotic phase, cell division

Front 12

What drugs work at the G0 phase?

Back 12

Glucocorticoids

Front 13

What drugs work at the S phase?

Back 13

Antimetabolites, and folate pathway inhibitors

Front 14

What drug works at both S phase and G2 phase?

Back 14

Topoisomerase inhibitors

Front 15

What drugs work at G2 phase?

Back 15

Antitumor antibiotics

Front 16

5-FU
First active metabolite

Back 16

FdUMP
forms a covalent ternary complex with thymidylate synthase and N5,10 methyltetrahydrofolate
Thymidilate is not synthesized and DNA syn is inhibited

Front 17

FUTP

Back 17

Incorporated into RNA
Interferes with mRNA processing and mRNA transistion

Front 18

FdUTP

Back 18

Incorporated into DNA and inhibits DNA synthesis

Front 19

Capecitabine

Back 19

Flouropyrimidine carbamate prodrug, used for met breast cancer

Front 20

What converts capecitabine into floururacil in the liver?

Back 20

thymidine phosphorylase

Front 21

Cytarabine

Back 21

Metabolized into active metabolite active triphosphate nucleotide, AraCTP

Front 22

What part of cell cycle does Cytarabine work on?

Back 22

The S phase, competitively inhibits DNA polymerase and interferes with chain elongation.

Front 23

What is cytarabine used to treat?

Back 23

AML

Front 24

What are the five plant alkaloids?

Back 24

Vinblastine, vincristine, etoposide, topotecan, Paclitaxel

Front 25

Vinblastine?

Back 25

Derved from th periwinkle plant, depolymerizes microtubule

Front 26

What phase does vinblastine work in?

Back 26

Mitotic arrest in metaphase----used for hodgkins disease, non-hodgkins lymphoma and breast cancer

Front 27

Vincristine?
What is it used to treat?

Back 27

related to vinblastine, AML, Hodgkins disease and non-hodgkins lymphoma, pediatric tumors---ewing's sarcoma and wilm's tumor

Front 28

Etoposide?

Back 28

semisynthetic derivative from mayapple root

Front 29

What stage does etoposide work at?

Back 29

block cell division in late s-G2 phase of cell cycle INhibits topoisomerae II resulting in DNA strand breakage

Front 30

What is it used to treat?

Back 30

Germ cell cancer, lung cancer, hematologic malignancies and gastric cancer

Front 31

Topotecan?

Back 31

Derived from the camptotheca acuminata tree.

Front 32

What does topotecan work on?

Back 32

topoisomerase I-used for cutting and re-ligating single DNA strands

Front 33

What is topotecan used for?

Back 33

Advanced ovarian cancer

Front 34

What is paclitaxel?

Back 34

A taxane, dervied from the Yew tree

Front 35

HOw does it work?

Back 35

Binds microtubules and enhances tubulin polymerization-results in the inhibition of mitosis and cell division-excreted in the feces-----used for solid tumors

Front 36

What antibiotics are used for cancer treatment?

Back 36

Doxorubicin, daunorubicin, dactinomycin, mitomycin and bleomycin

Front 37

What are the four mech of action of doxorubicin and daunorubicin?

Back 37

Inhibit topoisomerase two, DNA binding and inhibition of DNA synthesis, Bind cell membrane and alter fluidity and ion transport, and generation of ROS

Front 38

What is Doxorubicin used for?

Back 38

broad spectrum against hematologic malignancies and solid tumors

Front 39

What is Daunorubicin used for?

Back 39

AML

Front 40

What is mech of action of Dactinomycin?

Back 40

binds DNA synthesis between adjacent guanine cytosine base pairs inhibiting RNA synthesis----Pediatric tumors

Front 41

What is mech of action of Mitomycin

Back 41

Metabolized into an alkylating agent that cross links DNA--hypoxic tumor stem cells of solid tumors are particularly susceptible

Front 42

Bleomycin?

Back 42

Small peptide with a DNA binding region at on end and an iron binding region at the other

Front 43

How does it work?

Back 43

Binds DNA and the iron compoennt becomes oxidized leading to chromosomal abnormalities

Front 44

What is up with it being a CCS drug?

Back 44

Causes accumulation of cells in the G2 phase, must be careful in people with renal insufficiecny

Front 45

HOw does tamoxifen work?

Back 45

Binds the estrogen receptor of estrogen dependent tumors, 10 fold lower affinity than estradiol, endogenous estrogen must be ablated for optimal effect

Front 46

Flutamide?

Back 46

Antiandrogen effects via binding to the androgen receptor Prostate cancer

Front 47

Leuprolide?

Back 47

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

Front 48

Anastrozole?

Back 48

nonsteroidal Aromatase inhibitor, good for breast cancer in women

Front 49

Exemestane?

Back 49

Hormone that irreversibly inhibits aromatase--

Front 50

Imatinib?

Back 50

Inhibits oncoprotein tyrosine kinase-these promote abnormal proliferation and anti-apoptotic pathways

Front 51

Tumor cell markers?

Back 51

Bcr-Abl (CML)
c-kit (GI stromal tumors)

Front 52

Asparginase

Back 52

Bacterial derived enzyme-hydrolyzes L-asparganine to aspartic acid and ammonia