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SS- CMOD Block 2 > Anticancer Drugs > Flashcards

Anticancer Drugs Flashcards

1
Q

methotrexate

A

S phase
DHFR inhibitor: no THF to provide carbon for DNA and DNA
inhibit thymidylate synthase (decrease DNA syn.)
inhibits GRAFT, AICARFT: accumulation of adenosine (anti-inflamm.)
polyglutamation: traps in cell
hepatotoxicity, GI toxicity (mucositis and esophagitis), pulmonary fibrosis
renal excretion

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2
Q

flurouracil

A

S phase
req. activation
pyrimidine analog that complexes with folic acid that irreversible inhibits thymidylate synthase (decrease DNA syn.)
genetic differences in dihydropyrmidine dehydrogenase: major pathway of detoxification in tumor cells (converts 5-FU to dihydrofluorouracil): significant differences in toxicity
myelosuppresion, hand-foot syndrome, GI toxicity

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3
Q

capecitabine

A

S phase
oral prodrug for fluoruracil
CNS toxicity, more hand-foot syndrome

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4
Q

cytarabine

A

S phase
other names: arabinoside and Ara-C
req. activation to Ara-CTP
ITH, SC, IV
pyrimidine analog: selective inhibition of DNA pol
myleosuppresion, stomatitis, hand-foot syndrome

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5
Q

gemcitiabine

A

S phase
req. activation
deoxycytidine analog: decrease DNA syn.
myelosupression, pulmonary toxicity

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6
Q

6-mercaptopurine

A 
S phase
Purine analog
req. activation by HGPRT
patient: TPMT genotype (deficient: normal dose will kill patient)
allopurinol increases toxicity
myelosuppresion and hepatic dysfunction
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7
Q

thioguanine

A 
oral
S phase
Purine analog
req. activation by HGPRT
patient: TPMT genotype (deficient: normal dose will kill patient)
myelosuppresion and hepatic dysfunction
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8
Q

fludarabine

A

S phase

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9
Q

cyclophosphamide

A

oral or IV
cross-linking of dsDNA: N7 guanine
req. activation: microsomal enzymes-> aldophosphamide-> nonenzymatic cleavage-> phosphoramide mustard and acrolein
acrolein: hemorrhagic cystitis
lung fibrosis, nephrotoxicity, CHF (temporary)

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10
Q

ifosfamide

A

cross-link DNA at N7 guanine
requires liver bioactivation
acroelin: hemorrhagic cystitis
CNS toxicity, renal/urotoxic

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11
Q

mechlorethamine

A 
cross-link DNA at N7 guanine
spontaneous rearrangement (NO metabolic activation needed)
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12
Q

melphalan

A

cross-link DNA at N7
spontaneous rearrangement (NO metabolic activation)
lung fibrosis

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13
Q

busulfan

A

oral or IV
cross-links DNA
hepatic veno-occlusive, lung fibrosis, Addison-like adrenal insufficiency (hyperpigmentation)

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14
Q

BCNU

A 
carmustine: paranteral
cross-link DNA
carbamoylate: no cross-resistance with other alkylating agents
cross BBB
req. bioactivation
hepatic "veno-occlusive"
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15
Q

CCNU

A 
lomustine: oral
cross-link DNA
cross BBB
req. bioactivation
CNS toxicity: seizures, dementia
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16
Q

dacarbazine

A

methylating agent

req. metabolic activation

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17
Q

procarbazine

A

methylating agent
req. activation
disulfarim-like effect, weak MAO inhibition, male infertility

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18
Q

cisplatin

A

Intrastrand DNA links
spontaneous activation in aqueous
nephrotoxicity, ototoxicity, peripheral neuropathy
CNS toxicity

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19
Q

carboplatin

A

Intrastrand DNA links
spontaneous activation in aqueous
peripheral neuropathy, thrombocytopenia

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20
Q

allopurinol

A

Tx: tumor lysis syndrome
inhibit xanthine oxidase: hypoxanthine to uric acid
prophylaxis of hyperuricemia
increases toxicity of mercaptopurine

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21
Q

rasburicase

A

Tx: tumor lysis syndrome

catalyzes urate oxidase: uric acid to allantoin

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22
Q

doxorubicin

A

intercalate with DNA: inhibition of DNA-dependent RNA synthesis,
stabilize DNA-topo-II complex: topo-II inhibition, generate free radicals from semiquinone
cardiotoxicity
extravasional necrosis
red urine
more active in solid tumors than daunorubicin

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23
Q

MESNA

A

protect against acreolein: prevent hemorrhagic cystitis adjuvant: cyclophosphamide, ifosfomide

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24
Q

vincristine

A 
M phase
binds B-tubulin and blocks polymerization into microtubules (+ end)
cumulative neurotoxicity (peripheral neuropathy), paralytic ileus
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25
Q

vinblastine

A

M phase
binds B-tubulin and blocks polymerization into microtubules (+ end)
myelosuppresion: leukopenia, less peripheral neuropathy

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26
Q

topotecan

A

stabilizes DNA-topo I complex: inhibition of of topoisomerase I
renal elimination

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27
Q

irinotecan

A

stabilizes DNA-topo I complex: inhibition of of topoisomerase I
longer t1/2 than topotecan
hepatic elimination
avoid in Gilbert: UGT polymorphisms (defective)
diarrhea (loperamide), AchE inhibtion (atropine)

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28
Q

etoposide

A

oral
S and G2 phase
topoisomerase II inhibitor

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29
Q

paclitaxel

A

M phase
binds B-tubulin and antagonizes disassembly of microtubules (B-subunit)
hand foot syndrome,
more peripheral neuropathy than docataxel, hypersensitivity
admin with: cremaphor

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30
Q

docataxel

A

M phase
Binds a B-tubulin and antagonizes disassembly of microtubules (B-subunit)
edema-fluid retention, peripheral neuropathy, hand-foot syndrome
Greater potency than paclitaxel
admin with: polysorbate 80 or cremaphor

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31
Q

daunorubicin

A

intercalate with DNA: inhibition of DNA-dependent RNA synthesis,
stabilize DNA-topo-II complex: topo-II inhibition, generate free radicals from semiquinone
cardiotoxicity
extravasational necrosis
red urine

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32
Q

idarubicin

A

intercalate with DNA: inhibition of DNA-dependent RNA synthesis,
stabilize DNA-topo-II complex: topo-II inhibition, generate free radicals from semiquinone
cardiotoxicity
extravasional necrosis
red urine

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33
Q

bleomycin

A

G2 phase
free radical formation: oxidizes deoxyribose of thymidylate and other nucleotides
single and double DNA strand breaks
pulmonary fibrosis, hyperpigmentation

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34
Q

pegaspargase

A

degrades asparagine: starve protein synthesis

pancreatitis

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35
Q

lanalidomide

A

thalidomide derivative
inhibits tumor cell proliferation, cell adhesion to stroma, and angiogenesis
enhances NK cell activity
peripheral neuropathy

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36
Q

dexrazoxane

A

inhibitor of iron-mediated free radical generation; iron chlelator
protect against cardiotoxicity of doxirubicin and daunorubicin

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37
Q

leucovorin

A

folinic acid that converts to THF without DHFR

adjuvant: methotrexate to protect from myelosuppresion
adjuvant: enhance response to 5-FU by increasing TS complex

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38
Q

liposomal doxorubicin

A

less cardiotoxicity

hand foot syndrome instead

39
Q

bevacizumab

A

VEGF inhibitor: esp. important in large solid tumors that are outgrowing their blood supply
HTN, CHF, pulmonary hemorrhage, GI perforation
Tx: colorectal cancer and non-small cell lung cancer

40
Q

cetuximab

A

EGFR
infusion rxn, skin rash with sun
Tx: colorectal cancer, head and neck cancer

41
Q

panitumumab

A

EFGR
infusion rxn, skin rash with sun
Tx: colorectal cancer

42
Q

rituximab

A

CD20 inhibitor: depletion of B cells
Tx: chronic lymphocytic leukemia and non-hodgkin’s lymphoma
+ve B cell depletion, lymphopenia, progressive multifocal leukoencephalopathy

43
Q

trastuzumab

A

bind Her-2 and down regulate: CdK inhibitor p27 accumulates: cell cycle arrest
cardiomyopathy, infusion reaction
Tx: breast cancer
cardiotoxicity

44
Q

ipilimumab

A

CTLA-4 inhibitor: T cell activation and proliferation

Tx: melanoma

45
Q

ofatumumab

A

CD20
Tx: chronic lymphocytic leukemia
infection, progressive leukoencephalopathy, neutropenia

46
Q

boretezomib

A

IV
26-S proteosome inhibitor: prevents IkB-alpha degredation: keeps NFkB inhibited
Tx: multiple myeloma
cardiotoxicity, peripheral neuropathy, hepatotoxicity, hypotension

47
Q

vismodegib

A

oral SMO inhibitor
hedgehog pathway inhibitor
Tx: basal cell carcinoma

48
Q

T-DM1

A

Her-2 inhibitor and delivery of cytotoxic agent

49
Q

pertuzumab

A

block heterodimerization of Her-2 and Her-3

50
Q

Mab administration

A

IgG
NOT orally active drugs: large MW protein; IV or SC
potential poor penetration of solid tumors
infusion reactions: anaphylaxis, angiodema, pulmonary toxicity; HTN; pancytopenia

51
Q

Tyrosine kinase inhibitor

A

-nib
oral: vary bioavailability with food or CYP3A4
binds ATP binding domain: resistance diminishes therapeutic window
SE: disrupt endocrine function, blood dycrasias, QT prolongation
TK (EGFR)-> RAS-> BRAF->MEK-> ERK/MAPK

52
Q

temsirolimus

A

mTOR inhibitor: decrease angiogenesis, cell proliferation and metabolism
Tx: renal cancer

53
Q

sirolimus

A

mTOR inhibitor:decrease angiogenesis, cell proliferation and metabolism

54
Q

everolimus

A

mTOR inhibitor

Tx: renal cancer

55
Q

resistance to alkylating agents

A

increased repair

56
Q

stimuli for N/V

A
  1. chemotrigger zone
  2. GI tract
  3. psychological
57
Q

adjuvant therapy

A

chemotherapy used after surgery or radiation

58
Q

neo-adjuvant therapy

A

chemotherapy used before surgery or radiation

59
Q

Amifostine

A

adjuvant: cisplatin to prevent nephrotoxicity

free radical scavenger

60
Q

drug cocktail for prophylaxis of N/V

A

serotonin antagonist, NK-1 antagonist, corticosteroid

61
Q

azathioprine

A

metabolized into 6-MP

62
Q

hydroxyurea

A

S phase
free radical scavenger: inhibits ribonucleotide reductase: inhibits DNA syn.
NO conversion of ribonucleotides to deoxyribonucleotides
desquamative interstitial penumonitis, skin toxicities

63
Q

efflux pump names

A
  1. P-gp
  2. BCRP
  3. MRP
64
Q

crempahor

A

surfactant that makes taxes more soluble

hypersensitivity reaction

65
Q

polysorbate 80

A

surfactant that makes docataxel more soluble

less hypersensitivity than cremaphor

66
Q

topotecan

A

stabilizes DNA-topo I complex: inhibition of of topoisomerase I

67
Q

atropine

A

M receptor antagonist

adjuvant: irinotecan if <24hrs

68
Q

loperamide

A

anti-diarrheal

adjuvant: irinotecan if >24hrs

69
Q

tretinoin

A

ATRA: all-trans retinoic acid
oral
chimeric TF that interferes with RARalpha
retinoid acid syndrome: fever, dyspnea, weight gain, pulmonary infiltrates, and pleural or pericardial effusions
cheilitis, hyperlipidemia, dry skin, bone tenderness

70
Q

26S proteasome complex

A

normal-> HIF-1-> degraded by 26S proteasome

low oxygen-> HIF-1 ->VEGF

71
Q

erlotinib

A

TKI: EGFR
Tx: non-small cell lung cancer, pancreatic cancer
photo-sensitivity rash

72
Q

imatinib

A

TKI: BCR-ABL, c-KIT, PDGFR
Tx: chronic myeloid leukemia, chronic eosinophilic leukemia, acute lymphoblastic leukemia, GIST (GI stromal tumors)
fluid retention, thyroid dysfunction

73
Q

getfitnib

A

TKI: EGFR
Tx: non-small cell lung carcinoma
skin rash with sun

74
Q

vemurafenib

A

TKI: BRAF
Tx: metastatic melanoma
hand-foot syndrome

75
Q

crizotinib

A

TKI: ALK, HGFR
Tx: Non-small cell lung carcinoma

76
Q

dasatinib

A

TKI: SRC, BCR-ABL, c-KIT, PDGFR
Tx: chronic myeloid leukemia, acute lymphoblastic leukemia

77
Q

lapatinib

A

TKI: EGFR, HER2
Tx: breast cancer
skin rash with sun

78
Q

nilotinib

A

TKI: BCR-ABL, c-KIT, PDGFR
Tx: chronic myeloid leukemia

79
Q

pazopanib

A

TKI: VEGFR, PRGFR, c-KIT
Tx: soft tissue sarcoma, renal cell carcinoma
hand-foot syndrome

80
Q

sorafenib

A

TKI: BRAF, VEGFR, PDGFR
Tx: renal cell carcinoma, hepatocellular carcinoma
hand-foot syndrome, thyroid dysfunction

81
Q

sunitinib

A

TKI: VEGFR, PDGFR, c-KIT
Tx: GIST, renal cell carcinoma, pancreatic neuroendocrine tumor
hand-foot syndrome, thyroid dysfunction

82
Q

photo-sensitivity

A

cetuximab, panitumumab, erlotinib, getfitinib, lapatinib

83
Q

hand foot syndrome

A

capecitabine, fluorouracil, cytarabine, docetaxel, paclitaxel, liposomal doxorubicin, doxorubicin, sunitinib, sorafenib, pazopanib, vemurafenib

84
Q

lung fibrosis

A

cyclophosphomide, mephalan, busulfan, bleomycin, MTX

85
Q

peripheral neuropathy

A

cisplatin, carboplatin, vincristine, lanalidomide, paclitaxel

86
Q

renal toxicity

A

cyclophosphamide, ifosfamide, cisplatin, (less) carboplatin

87
Q

encephalopathy

  1. with seizures
  2. no seizures
A
  1. ifosfamide, cisplatin

2. capecitabine

88
Q

transient aseptic meningitis

A

IT MTX

89
Q

chronic leukoencephalopathy

A

characterized by headache, confusion, seizures, visual loss

caused by MTX

90
Q

stroke

A

cisplatin

91
Q

hepatic veno-occlusive

A

BCNU, busulfan

92
Q

ototoxic

A

cisplatin

93
Q

hepatic dysfunction

A

thioguanine, 6-MP

SS- CMOD Block 2 (16 decks)

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