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Pharmacotherapy IV > Exam 3 Cancer MOAs > Flashcards

Exam 3 Cancer MOAs Flashcards

1
Q

Tamoxifen

A

SERM prodrug

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2
Q

Raloxifen

A

SERM without endometrial cancer risk

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3
Q

Fulvestrant

A

SERD no agonist effects

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4
Q

Anastrozole

A

Nonsteroidal aromatase inhibitor

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5
Q

Letrozole

A

Nonsteroidal aromatase inhibitor

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6
Q

Exemestane

A

Steroidal aromatase inhibitor

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7
Q

Medroxyprogesterone acetate

A

protesterone agonist inhibits estrogen dependent proliferation in endometrial cancer

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8
Q

Leuprolide

A

GnRH agonist (breast and prostate cancer)

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9
Q

Goserelin

A

GnRH agonist (breast and prostate cancer)

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10
Q

Abarelix

A

GnRH antagonist

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11
Q

Degarelix

A

GnRH antagonist

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12
Q

Bicalutamide

A

Androgen antagonist

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13
Q

Nilutamide

A

Androgen antagonist

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14
Q

Enzalutamide

A

Very potent androgen antagonist

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15
Q

Abiraterone

A

Irreversible inhibitor of early hormone synthesis, used for prostate cancer and increases cholesterol

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16
Q

Finasteride

A

5-a reductase inhibitor, type II only

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17
Q

Dutasteride

A

5-a reductase inhibitor, type I and II

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18
Q

Gefitinib

A

Type I EGFR kinase inhibitor

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19
Q

Erlotinib

A

Type I EGFR kinase inhibitor

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20
Q

Afatinib

A

Covalent EGFR kinase inhibitor

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21
Q

Osmeritinib

A

Covalent T790M mutant EGFR kinase inhibitor

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22
Q

Lapatinib

A

Reversible inhibitor of EGFR and HER2

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23
Q

Sorafenib, axitinib, regorafenib, nitedanib, lenvatinib

A

Inhibit VEGFR

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24
Q

Crizotinib

A

Type II inhibitor of cMET (HGF receptor) and ALK fusion kinase

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25
Q

Cabozantinib

A

Type II inhibitor of cMET, RET, and VEGFR2 can overcome some resistance mutations to crizotinib

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26
Q

Imatinib

A

Type II inhibitor of Philadelphia chromosome ABL tyrosine kinase, PDGFR, and c-Kit.

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27
Q

Nilotinib

A

Inhibitor of BCR-Abl (philadelphia chromosome) mutants that are resistant to imatinib

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28
Q

Ponatinib

A

Inhibits all major mutant forms of BCR-Abl including T315I

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29
Q

Dasatinib

A

Inhibits BCR-Abl and Src oncogene

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30
Q

Bosutinib

A

Inhibits BCR-Abl and Src oncogene

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31
Q

Sorafenib

A

General kinase inhibitor (Raf, VEGFR, p38 MAPK), not used much for melanoma due to V600 mutation

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32
Q

Vemurafenib

A

Inhibits V600E mutant B-Raf kinase in MAPK/MEK/ERK pathway, BUT ACTIVATES WILD TYPE

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33
Q

Dabrafenib

A

Inhibits BRAF-V600 kinase, STILL ACTIVATES WILD TYPE

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34
Q

Trametinib

A

ONLY type III allosteric inhibitor, targets MEK1 and MEK2 kinases, inhibits downstream signaling in wild type cells activated by dabrafenib.

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35
Q

Idelalisib

A

Inhibits PI3k lipid kinase!

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36
Q

Ibrutinib

A

Covalent inhibitor of BTK, downstream of B cell receptor

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37
Q

Sunitinib

A

Type II inhibitor of VEGFR

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38
Q

Pazopanib

A

General tyrosine kinase inhibitor

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39
Q

Vandetanib

A

Inhibits VEGFR, EGFR, and RET

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40
Q

Sirolimus

A

Inhibits mTORC1 and mTORC2 serine-threonine kinase to block IL-2 signal transduction

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41
Q

Everolimus

A

Inhibits mTOR1 (only) serine-threonine kinase to block IL-2 signal transduction

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42
Q

Trastuzumab

A

Mab binds HER2/ErbB2, inhibiting function and killing cell

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43
Q

Pertuzumab

A

Binds HER2/ErbB2, inhibits dimerization

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44
Q

Cetuximab

A

Binds EGFR, will not work if KRAS mutation or constitutively active

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45
Q

Panitumumab

A

Binds EGFR, not if KRAS mutation

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46
Q

Rituximab

A

Binds CD20 on B cells

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47
Q

Ofatumumab/obinutuzumab

A

Binds CD20 on B cells

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48
Q

Bevacizumab

A

Binds VEGF LIGAND and prevents blocking to VEGFR

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49
Q

Ramucirumab

A

Binds VEGF RECEPTOR

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50
Q

Ado-trastuzumab emtansine

A

ADC that localizes metransine to HER2 overexpressing cells and has Herceptin function as well

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51
Q

Brentuximab vedotin

A

Binds CD30 on lymphoma cells, releases microtubule inhibitor and causes immune response

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52
Q

Ipilimumab

A

Binds CTLA-4 receptor, reversing inhibition on cytotoxic T cells. Stimulates immune system.

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53
Q

Pembrolizumab/Nivolumab

A

Binds PD1 RECEPTOR on T cells, stopping inhibitory signal and activating T cells.

54
Q

Atezolizumab

A

Binds PD1 LIGAND on tumor cells and macrophages, stopping inhibition and activating immune system.

55
Q

Blinatumomab

A

Recombinant protein binds T cell receptor directly to CD19 on B cells, allowing T cell to kill B cell

56
Q

Aldesleukin

A

IL-2 stimulates inflammation and cell killing

57
Q

Interferon a

A

Inhibits cell proliferation and enhances immune response

58
Q

Aflibercept

A

Fusion protein of VEGF receptor plus Fc of IgG sequesters VEGF ligand

59
Q

Romidepsin

A

Prodrug of HDAC inhibitor, which leads to re-expression of tumor suppressor genes. Can reactivate DNA viruses

60
Q

Vorinostat

A

HDAC inhibitor re-expresses tumor suppressor genes, can reactivate DNA viruses

61
Q

Belinostat

A

HDAC inhibitor re-expresses tumor suppressor genes, can reactivate DNA viruses

62
Q

Azacytidine

A

Incorporates into DNA and covalently binds DNMT enzyme, reactivates tumor suppressor genes.

63
Q

Decitabine

A

DNMT inhibitor reactivates tumor suppressor genes

64
Q

Tretinoin

A

Binds retinoic acid receptor to inhibit proliferation and induce differentiation

65
Q

Bexarotene

A

Retinoid agonist for retinoid receptor, vit D receptor, PPAR, and thyroid receptor. Induces differentiation

66
Q

Thalidomide (pomalidomide, lenalidomide)

A

Blocks bFGF and VEGF effects

67
Q

Bortezomib

A

Reversible proteasome inhibitor

68
Q

Carfilzomib

A

Irreversible proteasome inhibitor, NO neuropathy

69
Q

Vismodegib/sonidegib

A

Inhibit smoothened from activating GLI1 in Hedgehog pathway for basal cell carcinoma

70
Q

Venetoclax

A

Inhibits protein-protein interaction for BCL-2, a protein that prevents apoptotic proteins from working.

71
Q

Omacetaxine

A

Inhibits protein translation at ribosome

72
Q

Asparaginase

A

Degrades circulating asparagine, starving cancer cells that are deficient in asparagine synthetase

73
Q

Denosumab

A

Mimics osteoprotegrin, binds RANKL prevents from inducing osteoclast proliferation

74
Q

Allopurinol

A

inhibits xanthine oxidase, preventing buildup of uric acid and tumor lysis syndrome

75
Q

Rasburicase

A

Enzyme that breaks down uric acid preventing tumor lysis syndrome

76
Q

Filgrastim

A

G-CSF promotes granulocyte production (neutropenia)

77
Q

Sargramostim

A

GM-CSF promotes granulocyte progenitor production (more broad stimulation of granulocytes)

78
Q

Oprelvekin

A

Increases platelet production

79
Q

Epoetin

A

Stimulates RBC production

80
Q

Olaparib

A

PARP inhibitor stops repair of DNA in cells with BRCA mutation

81
Q

Palobociclib

A

Cdk4/6 kinase inhibitor blocks progression of tumor from G1-S phase, reducing proliferation

82
Q

Mustine

A

Old nitrogen mustard DNA alkylating agent

83
Q

Bendamustine

A

Nitrogen mustard with better tolerability, only partial cross resistance to other alkylating agents

84
Q

Chlorambucil

A

Nitrogen mustard alkylating agent

85
Q

Melphalan

A

Nitrogen mustard alkylating agent

86
Q

Cyclophosphamide

A

Prodrug nitrogen mustard alkylating agent converted to active form within tumor cell. Less bone marow toxicity d/t elevated ALDH in bone marrow cells. Hemorrhagic cystitis

87
Q

Ifosfamide

A

Prodrug nitrogen mustard with hemorrhagic cystitis, increased CNS toxicity over cyclophos

88
Q

Mesna

A

Thiol that accumulates in urine to neutralize toxic cyclophosphamide metabolites

89
Q

Carmustine

A

Nitrosurea alkylating agent converted to diazonium ion within tumor cell, penetrates BBB

90
Q

Lomustine

A

Nitrosurea alkylating agent converted to diazonium ion within tumor cell, penetrates BBB

91
Q

Busulfan

A

Alkyl sulfonate alkylating agent, “busulfan lung”

92
Q

Dacarbazine

A

Monoalkylating agent blocks replication enzyme function via creation of methyldiazonium ion

93
Q

Temozolomide

A

Becomes methyldiazonium without liver activation, alkylates DNA and inhibits replication. Crosses BBB!

94
Q

Cisplatin

A

Platinum compound forms intrastrand DNA crosslinks, active aquo form favored within cell. Dose-limiting NEPHROTOXICITY, minimal myelosuppression

95
Q

Carboplatin

A

Platinum compound forms intrastrand DNA crosslinks, active aquo formed slowly within cell. SIGNIFICANT MYELOSUPPRESSION, minimal nephrotoxicity

96
Q

Oxaliplatin

A

Platinum DNA intrastrand crosslinker, dose-limiting SENSORY NEUROPATHY, minimal nephrotoxicity

97
Q

Mitomycin C

A

Aziridine-containing product similar to nitrogen mustard, forms monoadducts and crosslinks. MYELOSUPPRESSION

98
Q

Radium 223 dichloride

A

Absorbed into bone, radiates bone metastasis

99
Q

Procarbazine

A

Somehow inhibits DNA, RNA, and protein synthesis, not cross resistant with alkylating agents.

100
Q

5-fluorouracil

A

Covalently binds to thymidylate synthase and causes thymineless death. Also incorporated into RNA and interferes with function. Leucovorate and thymidine pre-treatment increase efficacy.
DPD polymorphism causes life threatening toxicity

101
Q

Fluorodeoxyuridine

A

Deoxyribonucleoside 5-FU inhibits thymidine synthesis

102
Q

Capecitabine

A

Orally active prodrug of 5-FU, activated in liver, tissue, and tumor

103
Q

Cyrosine arabinoside

A

Nucleoside with arabinose sugar, competitively inhibits DNA polymerase, incorporated into DNA and inhibits polymerization.

104
Q

Gemcitabine

A

Nucleoside analog is incorpotated into DNA but HALTS chain elongation.

105
Q

6-mercaptopurine

A

Inhibits multiple enzymes in purine synthesis pathway (adenine and guanine). Activated by HGPRT.
Inactivated by TPMT - POLYMORPHISM
Allopurinol increases toxicity

106
Q

6-thioguanine

A

Thio analog of guanine, similar activity to 6-MP (cross resistance).
TMPT polymorphism!
NO interaction with allopurinol

107
Q

Fludarabine/nelarabine/cladribine

A

Arabinose adenosine analog inhibits DNA polymerase and ribonucleotide reducatase – DNA replication and transcription. Activity against cycling and resting cells.

108
Q

Methotrexate

A

Inhibits dihydrofolate reductase, enzyme that activates dietary folate. Inhibits S phase

109
Q

Pralatrexate

A

Inhibits DHFR selectively in cells with RFC-1 transporter (certain cancers), inhibits S phase.

110
Q

Pemetrexed

A

Inhibits DHFR, thymidylate synthase, and glycinamide ribonucleotide formyltransferase, so decreased risk of drug resistance. Inhibits S phase.

111
Q

Leucovorin

A

Reverses effects of DHFR inhibition

112
Q

Hydroxyurea

A

Decreases production of deoxyribonucleotides (DNA synthesis) - S phase

113
Q

Actinomycin C

A

Binds DNA, inhibits transcription and replication. Non cell cycle specific

114
Q

Irinotecan

A

Intercalates with DNA, inhibits topoisomerase I. S phase selective.
UGT1A1 increases risk of toxicity

115
Q

Topotecan

A

Topoisomerase I inhibitor

116
Q

Daunorubicin

A

Anthracycline Topoisomerase II inhibitor causes DS DNA breaks and free radical damage. Non-cell cycle dependent (but G2/M more selective). CARDIOTOXICITY

117
Q

Doxorubicin

A

Anthracycline topo II inhibitor. CARDIOTOXICITY, severe extravasation reaction. Not cell cycle dependent.

118
Q

Epirubicin

A

Anthracycline topo II inhibitor. Faster elimination, so less cardiotoxicity. Not cell cycle dependent.

119
Q

Idarubicin

A

Lipophilic anthracycline topo II inhibitor. Cardiotoxicity. Not cell cycle dependent.

120
Q

Dexrazoxane

A

Analog of EDTA binds iron, blocks free radical-induced cardiotoxicity of anthracycline topo II inhibitors

121
Q

Mitoxantrone

A

Topoisomerase II inhibitor without free radical formation – NO/minimal cardiotoxicity

122
Q

Etoposide/teniposide

A

Epipodophyllotoxin inhibitor of topoisomerase II that does not intercalate DNA. Better for cardiac function. G2/M CELL CYCLE SPECIFIC

123
Q

Bleomycin

A

Intercalates into DNA, causes free radical induced breaks in DNA. PULMONARY toxicity is dose-limiting and cumulative.

124
Q

Vincristine

A

Inhibits microtubule assembly. Dose-limiting NEUROTOXICITY, severe extravasation reaction. M phase specific.

125
Q

Vinblastine

A

Inhibits microtubule assembly. Dose-limiting MYELOSUPPRESSION, less severe neurotoxicity. M phase specific.

126
Q

Vinorelbine

A

Inhibits microtubule assembly. Dose-limiting MYELOSUPPRESSION, mild neurotoxicity. M phase specific.

127
Q

Eribulin

A

Prevents elongation at microtubule ends. Low rate of neurotoxicity.

128
Q

Paclitaxel

A

Blocks depolymerization and segregation of sister chromatids, leading to mitotic arrest. M phase specific. Dose-limiting MYELOSUPPRESSION.

129
Q

Docetaxel

A

Blocks depolymerization and segregation of sister chromatids, leading to mitotic arrest. M phase specific. Dose-limiting MYELOSUPPRESSION.

130
Q

Cabazitaxel

A

Blocks depolymerization and segregation of sister chromatids, leading to mitotic arrest. M phase specific. Dose-limiting MYELOSUPPRESSION. ONLY taxel that is not a Pgp substrate.

131
Q

Epothilone/ixabepilone

A

Promotes tubulin polymerization, stabilizes microtubules. More potent than taxols, not cross resistant. Neurotoxicity common but reversible.

Pharmacotherapy IV (4 decks)

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