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Hem/Onc > 31 & 32 - Common Cancer Drugs > Flashcards

31 & 32 - Common Cancer Drugs Flashcards

1
Q

alkylating agents - general what are they

A

strong electrophiles that form pos charged intermediates w/ target molecules and cause DNA damage

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2
Q

alkylating agents - mechanism

A

inhibit DNA synth / cell division by covalent attachment at 2 points
crosslinks DNA > cytotoxicity

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3
Q

example class and drug of alkylating agents

A

nitrogen mustards > cyclophosphamide

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4
Q

cyclophosphamide - category

A

alkylating agent > nitrogen mustard

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5
Q

cyclophosphamide uses

A

lymphoma regimens, breast cancer, ovarian cancer, some kinds of lung cancer

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6
Q

cyclophosphamide - AEs

A

myelosuppression (dose limiting)

alopecia, immunosuppression, cystitis

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7
Q

anitmetabolites - what are they

A

structurally related to natural compounds, compete for normal metabolites

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8
Q

folate antagonist mechanism

A

block biosynth of fully reduced tetrahydrofolic acid

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9
Q

example of folate antagonist

A

methotrexate

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10
Q

methotrexate mech

A

competitively inhibits folic acid binding to dihydrofolate reductase > death due to thymidylate and purine blockage; s-phase specific agent

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11
Q

uses of methotrexate

A

curative regimen for ALL, trophoblastic choriocarcinoma, Burkitt’s

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12
Q

methotrexate AEs

A

myelosuppression - dose limiting

renal insufficiency - c/i in pts w/ renal impairment

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13
Q

rescue drug for myelosuppression due to methotrexate

A

leucovorin

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14
Q

purine analogue mechanism

A

prevent biosynth of purine precursors
get incorporated into RNA/DNA > fraudulent nucleic acids made

require activation - “lethal synthesis”

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15
Q

ex of purine analogue

A

thioguanine (a thiolated purine analogue)

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16
Q

use of thioguanine

A

AML, ALL, CML

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17
Q

AEs of thioguanine

A

myelosuppression

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18
Q

ex of pyrimidine analogue

A

5-fluorouracil (halogenated pyrimidine)

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19
Q

uses of 5FU

A

CA of breast, stomach, COLON, rectum, pancreas, liver, ovary

short story: lots of solid tumors

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20
Q

major AE of 5FU

A

myelosuppression

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21
Q

hydroxyurea - mech

A

inhibits ribonucleoside diphosphate reductase

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22
Q

hydroxyurea - use

A

myeloprolif syndromes

CML

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23
Q

AEs of hydroxyurea

A

myelosuppression

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24
Q

anticancer abx - general mechanism

A

inhibit nucleic acid synth by blocking DNA replication or transcription either by direct binding to nucleic acid or polymerizing enzyme

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25
Q

ex of anthracycline (anticancer abx)

A

doxorubicin

26
Q

doxorubicin mech

A

intercalating agent - insert btwn DNA base pairs, S-phase specific

27
Q

use of doxorubicin

A

CA of breast, ovary, endometrium, bladder, thyroid, lung

bottom line: solid tumors

28
Q

AEs of doxorubicin

A

cardiotoxicity (unique)

myelosuppressive (major)

29
Q

bleomycin mech

A

strand scission - cut phosphate backbone

30
Q

use of bleomycin

A

potentially curative in combo for testicular CA;

Hodgkin’s and non-Hodgkin’s lymphoma

31
Q

AEs of bleomycin

A 
lung tox (fibrosis)
skin toxic
32
Q

mech of platinum coordination complexes

A

electrophile that forms strong coordination complexes w/ DNA (guanine)

33
Q

use of cisplatin

A

curative for testicular cancer

34
Q

AEs of cisplatin

A

renal tox

35
Q

2 subcategories of plant derived cancer drugs

A

vinca alkaloids

taxanes

36
Q

vincristine mech

A

binds to tubulin and blocks polymerization > M phase specific agent

37
Q

use of vincristine

A

curative for ALL, hodgkins and NHL

38
Q

AEs of vincristine

A

neuro toxicity (dose limiting)

39
Q

ex of taxane

A

paclitaxel

40
Q

mech of paclitaxel

A

binds to beta tubulin and antagonizes MT diasassembly

41
Q

use of paclitaxel

A

cisplatin refractory metatstatic ovarian and breast CA

42
Q

AEs of paclitaxel

A

myelosuppressive, myalgias, stocking/glove sensory neuropathy

43
Q

topotecan mech and class

A

camptothecin analog

binds to topoisomerase I, ssDNA breaks

44
Q

use of topotecan

A

ovarian and small cell lung CA

45
Q

AEs of topotecan

A

neutropenia

46
Q

etoposide mech

A

complex w/ topoisomerase II, dsDNA breaks

47
Q

use of etoposide

A

testicular cancer

48
Q

AEs of etoposide

A

causes leukemia w/ chromosomal translocation

49
Q

uses of prednisone for cancer

A

used to induce remission in ALL
used to treat both Hodgkin and NHL

destroys lymphocytes

50
Q

what did estrogens used to be used for in cancer?

A

prostate cancer

51
Q

tamoxifen

A 
estrogen agonist (SERM) - binds but not transcriptionally active
first line therapy for ER+ breast cancer
52
Q

use of GnRH agonists and antagonists

A

prostate cancer - leuprolide is equivalent to orchiectomy in terms of response

53
Q

examples of GnRH agonists

A

leuprolide
histerelin
nafarelin
goserelin

54
Q

examples of GnRH antagonists

A

abarelix *(no testosterone flare)

triptorelin

55
Q

aromatase inhibitors mech

A

stop extra-adrenal synth of estrogen in other tissues

56
Q

ex of aromatase inhib

A

anastrozole

57
Q

use of anastrozole

A

adv ER and PR pos breast cancers

58
Q

aminoglutethimide

A

first aromatase inhib, largely replaced by newer ones that dont block hydrocortisone synth

59
Q

exemestane

A

irreversible inhib of aromatase

60
Q

imatinib (Gleevic)

A

tyrosine kinase inhib targeted to PDGF-R
good for inhibiting Philadelphia chromosome product in CML and c-kit (in GI stromal tumors)

lots of side effects - basically platelet like bleeding, fever/flu sx

61
Q

bevacizumab (avastin)

A

ab against VEGF that inhibits angiogenesis

used in colorectal cancer, non-small cell lung cancer, some breast cancers

62
Q

bortezomib

A

reversible inhibitor of proteasome (stop breakdown of cell cycle regulators)
used in multiple myeloma and relapsed mantle cell lymphoma

Hem/Onc (29 decks)

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