B3-042 Anti Cancer Drugs Flashcards

1
Q

CCNS alkylating agents

A

cyclophosphamide
mechlorethamine
cis-platin

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2
Q

Mechanism: transfering an alkyl group over to DNA. Blocks access to DNA by cross linking.

A

CCNS alkylating agents

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3
Q

can lead to secondary malignancy due to DNA damage induced

A

CCNS alkylating agents

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4
Q

adds alkyl group to guanine
prodrug, metabolized by CYP450

A

cyclophosphamide

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5
Q

clinical use for multiple myeloma, lymphoma, leukemia, ovarian/breast cancer, small cell lung cancer, neuroblastoma, sarcoma

A

cyclophosphamide

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6
Q

delayed adverse effect is sterile hemorrhagic cystitis (hematuria/excessive voiding)

A

cyclophosphamide

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7
Q

produces acrolein-toxic metabolite

A

cyclophosphamide

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8
Q

mechanism of resistance for CCNS alkylating agents

A

impermeable to drug
pump drug out
alternate targets for drug (GSH)
increased DNA repair
no apoptosis

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9
Q

first ever alkylating agent, Hodgkins lymphoma

A

mechlorethamine

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10
Q

cross links DNA with platinum

A

cis-platin

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11
Q

cisplatin with less toxicity but more myelosuppression

A

carboplatin

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12
Q

cisplatin with less renal but more neurotoxicity

A

oxaliplatin

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13
Q

aromatase inhibitors that decreases estrogen synthesis [2]

A

anastrozole, letrozole

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14
Q

hormonal agents

A

anastrozole
letrozole
flutamide
hydrocortisone
prednisone
tamoxifen

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15
Q

androgen receptor antagonist

A

flutamide

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16
Q

adrenocorticosteroids [2]
suppress proliferation of immune cells

A

hydrocortisone
prednisone

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17
Q

selective estrogen receptor anatagonist

A

tomoxifen

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18
Q

used for breast cancer in post menopausal women
ER+ primary and metastatic cancers [2]

A

anastrozole
letrozole

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19
Q

used for metastatic prostate cancer

A

flutamide

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20
Q

hormonal agents [2] used for leukema/lymphoma

A

hydrocortisone
prednisone

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21
Q

hormonal agent used for breast cancer

A

tamoxifen

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22
Q

adverse effects: anastrozole

A

nausea, headache, hot flashes

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23
Q

adverse effects: flutamide

A

hepatic effects

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24
Q

adverse effects: hydrocortisone/prednisone

A

elevated fasting glucose
fluid retention
immunosuppression
diabetes

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25
Q

hormonal agents: CYP2D6 activation

A

tamoxifen

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26
Q

CCS Topoisomerase inhibitors

A

etoposide
irinotecan

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27
Q

inhibits DNA topoisomerase II

A

etoposide

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28
Q

inhibits DNA Topoisomerase I, pro-drug

A

irinotecan

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29
Q

topoisomerase inhibitor for colon cancer

A

irinotecan

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30
Q

topoisomerase inhibitor for testicular, small cell lung, leukemia, lymphoma

A

etoposide

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31
Q

irinotecan is metabolized by UGT1A1. A deficiency can cause

A

increased toxicity, leading to
Crigler-Najjar, Gilbert’s, hyperbilirubinemia

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32
Q

checkpoint inhibitors

A

ipilimumab
nivolumab
atezolimumab

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33
Q

mAb against CTLA-4

A

ipilimumab

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34
Q

mAb against PD-1

A

nivolumab

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35
Q

mAb against PD-L1

A

atezolimumab

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36
Q

checkpoint inhibitor used for unresectable or metastatic melanoma

A

ipilimumab

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37
Q

checkpoint inhibitor used for melanoma, colon, HENT, hepatocellular, hodgkins, non-small cell lung, urothelial

A

nivolumab

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38
Q

adverse effects: ipilimumab

A

immune inflammatory response

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39
Q

Antimetabolites CCS

A

cytarabine
5-flurouracil
gemcitabine
6-thioguanine
6-mecaptopurine
methotrexate

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40
Q

inhibits thymidylase synthase

A

5-FU

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41
Q

cytosine analog, chain terminator

A

cytarabine

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42
Q

cytosine analog, inhibits polymerase and chain terminator

A

gemcitabine

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43
Q

more toxic than purines, cause BM and GI toxicity

A

cytarabine
5-FU
gemcitabine

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44
Q

purine analong
blocks DNA and RNA synthesis
inhibits AMP and GMP synthesis

A

6-mercaptopurine

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45
Q

purine analog
incorporated into RNA and DNA, alters function

A

6-thioguanine

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46
Q

inactivated and cleared by TPMT thiopurine methyltransferase

A

6-thioguanine
6-mercaptopurine

**test genotype for TPMT

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47
Q

folic acid analog
inhibits DHFR by adding a hydrogen to reduce it

A

methotrexate

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48
Q

adverse effect: methotrexate

A

myelosuppression

49
Q

CCS microtubule poisons

A

docetaxel
paclitaxel
vinblastine
vincristine

50
Q

stabilize microtubules in M phase, prevents progression to anaphase [2]

A

docetaxel
paclitaxel

51
Q

bind beta tubulin, inhibit formation of mitotic spindle causing metaphase arrest [2]

A

vinblastine
vincristine

52
Q

used for ovarian, breast, and pancreatic solid tumors [2]

A

docetaxel
paclitaxel

53
Q

adverse effects of docetaxel/paclitaxel

A

meyolesuppression
neuropathy

54
Q

adverse effects: vinblastine

A

nausea, vomiting, alopecia, myelosuppression

55
Q

adverse effects: vincritstine

A

peripheral neuropathy

56
Q

tyrosine kinase inhibitors [2]

A

gefitinib
imatinib

57
Q

TK inhibitor of EGFR

A

gefitinib

58
Q

TK inhibitor of BCR-ABL

A

imatinib

59
Q

TK used for non-small cell lung cancers

A

gefitinib

**less effective for asian, non-smoker

60
Q

TK used for CML, Ph+ALLm GI stromal tumors

A

imatinib

61
Q

antitumor antibiotics CCNS [3]

A

bleomycin
daunorubicin
doxorubicin

62
Q

binds to DNA and induces ROS production causing strand breaks

A

bleomycin

63
Q

block topoisomerase II, generates ROS [2]

A

daunorubicin
doxorubicin

64
Q

adverse effect: bleomycin

A

pulmonary fibrosis

65
Q

adverse effect: daunorubicin, doxorubicin

A

cardiotoxicity

66
Q

decreases vascularization, increases capillary permeability, inhibits angiogenesis

A

bevacizumab

67
Q

inhibits 26S proteosome, disrupts signaling cascades leading to apoptosis

A

bortezomib

68
Q

mTOR inhibitor
inhibits cell cycle progression, angiogenesis, promotes apoptosis

A

sirolimus

69
Q

adverse effects: bevacizumab

A

arterial thromboembolism

70
Q

adverse effects: bortezomib

A

thrombocytopenia, peripheral neuropathy

71
Q

half life 60 hrs, CYP3A substrate

A

sirolimus

72
Q

biologics [2]

A

interferon a
trastuzamab

73
Q

cytokine inhibitor of cell growth
alters gene expression, antiviral immunomodulator

A

INF-a

74
Q

Her-2/ErbB-2 onogene antogonist

A

trastuzamab

75
Q

biologic used for hematologic malignancies, metastatic melanoma, renal cell carcinoma

A

INF-a

76
Q

biologic used for HER-2 breast cancer

A

trastuzamab

77
Q

adverse effects: trastuzamab

A

infusion reactions
hypersensitivity
cardiomyopathy

78
Q

ancillary drugs

A

EPO
GM-CSF
Mesna
Ondansetron

79
Q

inactivates acrolein in kidneys

A

mesna

80
Q

serotonin antagonist

A

ondansetron

81
Q

used to stimulate erythroid precursor maturation in anemia

A

EPO

82
Q

used to treat myelosuppression
stimulates granulocytes/macrophage precursor development

A

GM-CSF

83
Q

used for iatrogenic nausea and vomiting

A

ondansetron

84
Q

used for prevention of hemorrhagic cystitis

A

mesna

85
Q

dosing regimen is determined by

A

the time for recovery from adverse effects

86
Q

chemotherapeutic administration is limited by

A

toxicity to other rapidly growing cell populations

bone marrow, GI, epitehlium

86
Q

chemotherapeutic administration is limited by

A

toxicity to other rapidly growing cell populations

bone marrow, GI, epitehlium

87
Q

most cancer drugs target

A

processess essential for cell proliferation

88
Q

stimulates the production of WBCs

A

GM-CSF

WBCs are most sensitive to effects of decreased cell production

89
Q

activated by salvage pathway for nucleotide synthesis

A

purine analogs

90
Q

activated by hprt

A

purine analogs

91
Q

bone marrow suppression only observed at very high doses

A

purine analogs

92
Q

inhibits human dihydrofolate reductase

A

methotrexate

93
Q

prevents denovo synthesis of purines and the conversion of uracil to thymidine

A

methotrexate

94
Q

rescue methotrexate with

A

folinic acid (levocorine)

95
Q

cytarabine
gemcitabine
methotrexate

are all

A

cell cycle specific

96
Q

cis platin is administered

A

IV

97
Q

mechlorethamine is administered

A

IV

98
Q

very short half life
marked bone marrow suppression

A

mechlorethamine

99
Q

particularly associated with secondary malignancy

A

alkylating agents and anti-tumor antibiotics

100
Q

drug related cancers are caused by

A

DNA damage caused by the drugs in the normal cells producing oncogenic mutations

101
Q

secondary malignancies develop ….. years after treatment

A

5-20

102
Q

resistant cells are a

A

continuation of the same malignancy

103
Q

blocks normal hormonal stimulation of the prostate

A

flutamide

104
Q

alkylating agent associated with nephrotoxicity

A

cisplatin

105
Q

microtubule poison associated with myelosuppresion

A

vinblastine

106
Q

anti-tumor antibiotic that is cell cycle specific

A

bleomycin

107
Q

SN-38 is the active metabolite for

A

irinotecan

108
Q

SN-38 is inactivated by

A

glucuronidation of UGT1A1

109
Q

FDA recommends genotyping for patients for UGT1A1 related to decreasing toxicity of

A

irinotecan

110
Q

does not cross BBB

A

trastuzumab

111
Q

targets VEGF-A receptro

A

bevacizumab

112
Q

monotherapy for glioblastoma

A

bevacizumab

113
Q

targets CTLA-4

A

ipilimumab

114
Q

modulates T cell activation

A

CTLA-4

115
Q

enhances T cell activations

A

ipilimumab

116
Q

targets unique kinase found only in CML

A

imatinib

very selective in toxicity

117
Q

signature adverse effect of bleomycin

A

irreversible pulmonary fibrosis