17. Anti-Cancer Agents

Question 1

Cyclophosphamide

Answer 1

alkylating agent. causes DNA damage in various ways (can cross link DNA strands, bind groups…)

Question 2

Odansetron

Answer 2

Serotonin receptor blocker, anti-emetic that makes use of alkylating agents much more bearable.

Question 3

methotrexate

Answer 3

antimetabolite, inhibits DHFR, blocks DNA synthesis, only works in S phase

Question 4

general, side effects?

Answer 4

nausea, vomiting, alopecia

Question 5

Leucovorin: with methotrexate?

Answer 5

rescue body cells, still kill cancer cells

Question 6

5-fluorouracil (5-FU)

Answer 6

binds thymidylate synthase, prevents purine synthesis

Question 7

Leucovorin with 5-FU?

Answer 7

stabilizes binding to thymidylate synthase, enhances effect

Question 8

vincristine

Answer 8

binds to protein tubulin, prevents mT assembly, M phase specific. NOT toxic to BM, can be combined with drugs that are

Question 9

vinblastine

Answer 9

binds to protein tubulin, prevents mT assembly, M phase specific. toxic to bone marrow.

Question 10

toxicity: vincristine v vinblastine?

Answer 10

vinc: NOT toxic to BM,
vinb: TOXIC to BM

Question 11

taxol

Answer 11

binds to mTs, prevents normal mitosis

Question 12

Velcade

Answer 12

proteasome blockade! binds proteosome, abnl proteins build up, apoptosis

Question 13

Lenolidimide

Answer 13

immunomodulatory in a way we don’t understand. SE = neuropathy
very effective in multiple myeloma

Question 14

G-CSF, GM-CSF, EPO

Answer 14

hematopoietic growth factors. prevent blood counts from dropping w chemo

Question 15

IL2

Answer 15

biologic response modifier. give to pts to incr immune response to cancer

Question 16

rituximab

Answer 16

monoclonal antibody, targets CD20, B cell NHL. then macrophage destroys cell.

Question 17

5-Azacytidine

Answer 17

DNA methylation can –> cancer. this prevents methylation. tumor suppressor genes that may have been silenced will be turned back on.

Question 18

biggest class of chemo drugs?

Answer 18

DNA damaging agents

Question 19

in general, how do these drugs all work?

Answer 19

by inducing apoptosis in various ways

Question 20

alkylating agents: phase? response curve?

Answer 20

phase non-specific. linear dose response.

Question 21

alkylating agents associated with high incidence of what?

Answer 21

secondary cancers (esp leukemia, lymphoma, MDS)

Question 22

cyclophosphamide: has to be activated? by what?

Answer 22

yes by the hepatic p450 system

Question 23

side effect of cyclophosphamide?

Answer 23

hemorrhagic cystitis. caused by acrolein.

Question 24

how to prevent cyclophosphamide-induced hemorrhagic cystitis?

Answer 24

MESNA, binds acrolein

Question 25

secondary malignancies are mos common with what drugs, treatments?

Answer 25

alkylating agents, XRT

Question 26

what is an antiemetic that can be combined with 5-HT inhibitors like odansetron?

Answer 26

aprepitant. blocks Substance P binding

Question 27

antimetabolite drugs have to act on drugs in what phase?

Answer 27

S phase

Question 28

what are ways tumor cells can become resistant to methotrexate?

Answer 28

decreased transport, gene amplification, mutation of DHFR

Question 29

methotrexate is also used for what?

Answer 29

immunosuppression in other diseases like RA, lupus, to prevent GVHD

Question 30

Cytarbine (ara-C)

Answer 30

nucleoside analog. inhibit DNA polymerase.

Question 31

Ara-C: phase specific?

Answer 31

S phase specific

Question 32

Ara-C most commonly used to treat what?

Answer 32

AML

Question 33

Ara-C: part of what chemo regimen?

Answer 33

given continuously for 7 days as part of the 7+3 regimen, with daunarubicin.

Question 34

Ara-C: what side effects?

Answer 34

acute cerebellar toxicity.

Question 35

topo inhibitors: what do they do?

Answer 35

cause single or double strand breaks.

Question 36

anthracycline antibiotics: what are the classic drugs of this group?

Answer 36

doxorubicin and daunarubicin

Question 37

anthracyclines: what do they do?

Answer 37

get right into the DNA strand, inhibit repl and mRNA synth. Topo II inhibitor as well.

Question 38

anthracycline antibiotics: side effects?

Answer 38

damage to the heart, vesicants. problems with IV sites

Question 39

Etoposide: mechanism

Answer 39

Topo II inhibitor

Question 40

Camptotheca: mechanism?

Answer 40

Topo I inh

Question 41

what can happen if we drive EPO too high with exogenous growth factors?

Answer 41

HTN, stroke

Question 42

ESA stands for what?

Answer 42

erythropoietin stim agent

Question 43

benefit of G-CSF?

Answer 43

counts will recover earlier, increases the max dose a patient can tolerate

Question 44

Gemtuzumab: target, disease?

Answer 44

CD33 (immature myeloid), AML

Question 45

Rituximab: target, disease?

Answer 45

CD20 (B lymphs), lymphoma

Question 46

tiuxetan: target, disease?

Answer 46

CD20 (B lymphs), NHL

Question 47

cetuximab: target, disease?

Answer 47

EGFR, colorectal, head, neck

Question 48

bevacizumab: target, disease?

Answer 48

VEGF, several