Antineoplastics Flashcards

1
Q

Cyclophosphamide

A

Nitrogen mustards
Alkylating agents
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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2
Q

Ifosfamide

A

Nitrogen mustards
Alkylating agents
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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3
Q

Mechlorethamine

A

Nitrogen mustards
Alkylating agents
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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4
Q

Melphalan

A

Nitrogen mustards
Alkylating agents
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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5
Q

Chlorambucil

A

Nitrogen mustards
Alkylating agents
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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6
Q

Procarbazine

A

Methylhydrazine derivative
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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7
Q

Busulfan

A

Alkyl sulfonate
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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8
Q

Carmustine

A

Nitrosureas
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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9
Q

Streptozocin

A

Nitrosureas
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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10
Q

Bendamustine

A

Nitrosureas
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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11
Q

Dacarbazine

A

Triazene
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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12
Q

Temozolomide

A

Triazene
Alkylating agent
covalent linkages DNA&raquo_space;inter/intrastrand crosslinking
CCNS

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13
Q

Cisplatin

A

Platinum coordination complexes
Not really an alkylating agent, forms covalent bonds with DNA
CCNS

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14
Q

Carboplatin

A

Platinum coordination complexes
Not really an alkylating agent, forms covalent bonds with DNA
CCNS

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15
Q

Oxaliplatin

A

Platinum coordination complexes
Not really an alkylating agent, forms covalent bonds with DNA
CCNS

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16
Q

Methotrexate

A

Folic acid analog
Inhibits DHF reductase&raquo_space; nonthymidylate or purine nucleotide synthesis
CCS- S phase

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17
Q

Pemetrexed

A

Folic acid analog
Inhibits DHF reductase&raquo_space; no thymidylate or purine nucleotide synthesis
CCS- S phase

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18
Q

Fluorouracil (5-FU)

A

Pyrimidine analog
Prodrug, blocks thymidylate synthetase&raquo_space; no thymidylate synthesis. Active compounds incorporated into DNA and RNA&raquo_space; no DNA synthesis, no RNA processing, no translation
CCS- S phase

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19
Q

Capecitabine

A

Pyrimidine analog

CCS- S phase

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20
Q

Cytarabine

A

Pyrimidine analog
Inhibits DNA polymerase alpha and beta, blocks DNA synthesis and repair, incorporates into DNA and interferes with chain elongation and ligation
CCS- S phase

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21
Q

Gemcitabine

A

Pyrimidine analog

CCS- S phase

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22
Q

5-aza-cytidine

A

Pyrimidine analog

CCS- S phase

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23
Q

Deoxy-5-aza-cytabine

A

Pyrimidine analog

CCS- S phase

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24
Q

Mercaptopurine

A

Purine analog
Incorporated into triphosphates&raquo_space;inhibits purine, DNA, RNA synthesis
CCS-S phase

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25
Q

Pentostatin

A

Purine analog
Incorporated into triphosphates&raquo_space;inhibits purine, DNA, RNA synthesis
CCS-S phase

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26
Q

Fludarabine

A

Purine analog
Incorporated into triphosphates&raquo_space;inhibits purine, DNA, RNA synthesis
CCS-S phase

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27
Q

Clofarabine

A

Purine analog
Incorporated into triphosphates&raquo_space;inhibits purine, DNA, RNA synthesis
CCS-S phase

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28
Q

Nelarabine

A

Purine analog
Incorporated into triphosphates&raquo_space;inhibits purine, DNA, RNA synthesis
CCS-S phase

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29
Q

Thioguanine (6-TG)

A

Purine analog
Incorporated into triphosphates&raquo_space;inhibits purine, DNA, RNA synthesis
CCS-S phase

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30
Q

Vinblastine

A

Vinca alkaloid
Natural product
Binds B tubulin and inhibits microtubule assembly, destabilize
CCS-M phase

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31
Q

Vincristine

A

Vinca alkaloid
Natural product
Binds B tubulin and inhibits microtubule assembly, destabilize
CCS-M phase

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32
Q

Vinorelbine

A

Vinca alkaloid
Natural product
Binds B tubulin and inhibits microtubule assembly, destabilize
CCS-M phase

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33
Q

Paclitaxel

A

Taxane
Natural product
Binds B tubulin and promotes microtubule formation and stabilization
CCS-M phase

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34
Q

Docetaxel

A

Taxane
Natural product
Binds B tubulin and promotes microtubule formation and stabilization
CCS-M phase

35
Q

Etoposide

A

Epipodophyllotoxin
Natural product
Inhibits topoisomerase II&raquo_space; DNA damage by strand breakage
CCS- G2-S Phase

36
Q

Teniposide

A

Epipodophyllotoxin
Natural product
Inhibits topoisomerase II&raquo_space; DNA damage by strand breakage
CCS- G2-S Phase

37
Q

Topotecan

A

Camptothecin
Natural product
Inhibits topoisomerase I&raquo_space; DNA damage and block replication and transcription
CCS

38
Q

Irinotecan

A

Camptothecin
Natural product
Inhibits topoisomerase I&raquo_space; DNA damage and block replication and transcription
CCS

39
Q

Doxorubicin

A

Anthracycline
Natural product
Inhibits topoisomerase II, intercalates DNA and blocks synthesis of DNA and RNA, generates O2 free radicals, alter cell membrane fluidity
CCNS

40
Q

Daunorubicin

A

Anthracycline
Natural product
Inhibits topoisomerase II, intercalates DNA and blocks synthesis of DNA and RNA, generates O2 free radicals, alter cell membrane fluidity
CCNS

41
Q

Dactinomycin

A

Antibiotic
Natural product
Binds double strand DNA and intercalates between G-C base pairs, prevents transcription
CCNS

42
Q

Bleomycin

A

Anthracenedione
Natural product
Binds DNA&raquo_space; double and single strand breaks, prevents DNA synthesis
CCS- G2 phase

43
Q

Mitoxantrone

A

Anthracenedione

Natural product

44
Q

Mitomycin

A

Anthracenedione

Natural product

45
Q

Yondelis

A

Echinocandin

Natural product

46
Q

L-Asparaginase

A
Enzyme
Natural product
Hydrolyzes asparagine >> no protein synthesis in cells that can't make their own asparagine
Active against ALL
CCS-G1
47
Q

Pegaspargase

A
Enzyme
Natural product
Hydrolyzes asparagine >> no protein synthesis in cells that can't make their own asparagine
Active against ALL
CCS-G1
48
Q

Hydroxyurea

A

Substituted urea
Inhibits ribonucleoside diphosphate reductase&raquo_space; can’t make deoxyribonucelotides
CCS- S phase

49
Q

Tretinoin

A

Differentiating agent
All trans retinoic acid
Binds nuclear receptors&raquo_space; granulocyte differentiation
Active against Acute promyelocytic leukemia with t(15:17)
CCNS

50
Q

Arsenic Trioxide

A

Differentiating agent
Unknown MOA, degrades PML/RAR alpha chimeric protein and induces apoptosis using caspase and cytochrome C activation
Active against Acute promyelocytic leukemia with t(15:17)
CCNS

51
Q

Vorinostat

A

Histone deacetylase inhibitor
Differentiating agent
Alterations in chromatin structure and transcription factor activation&raquo_space; cell death
CCNS

52
Q

Interferon alpha

A

Biological response modifier
Inhibit cell growth, alter differentiation, interferes with oncogene expression, alters cell surface Ag expression, increases phagocytic activity of macrophages, augments cytotoxic lymphocytes
CCNS

53
Q

Interleukin 2

A

Biological response modifier
Proliferation of activated T cells, secretion of cytokines from NKs and monocytes&raquo_space; increased cytotoxic killing by T cells and NK cell
CCNS

54
Q

Thalidomide

A

Immunomodulator
Anti-angiogenic and immunomodulatory, inhibits TNF alpha signaling
CCNS

55
Q

Lenalidomide

A

Immunomodulator
Anti-angiogenic and immunomodulatory, inhibits TNF alpha signaling
CCNS

56
Q

Leucovorin

A

Methotrexate rescue

57
Q

Mesna

A

Cyclophosphamide recue bladder

58
Q

Sargramostim

A

GMCSF

59
Q

Filgrastim

A

GCSF

60
Q

Pegfilgrastim

A

GCSF

61
Q

Oprelvekin

A

IL-11, thrombopoietic

62
Q

Erythropoietin

A

Erythropoiesis

63
Q

Darbepoeitin

A

Erythropoiesis

64
Q

Ondansetron

A

Serotonin antagonist

65
Q

Imatinib

A

BCR-ABL

also PDGFR, cKit, stem cell factor

66
Q

Dasatinib

A

BCR-ABL

also Src, cKit, PDGFR

67
Q

Nilotinib

A

BCR-ABL

also cKit, PDGFR

68
Q

Gefitinib

A

EGFR

69
Q

Erlotinib

A

EGFR

70
Q

Sorafenib

A

multikinase inhibitor

RAF kinases and cell surface kinase receptors

71
Q

Sunitinib

A

multikinase inhibitor

RAF kinases and cell surface kinase receptors

72
Q

Lapatinib

A

Her2/Neu internal domain

73
Q

Bortezomib

A

Proteosome inhibitor

74
Q

Temsirolimus

A

mTOR inhibitor

Immunosuppresant, inhibit cell cycle and angiogenesis, promotes apoptosis

75
Q

Everolimus

A

mTOR inhibitor

Immunosuppresant, inhibit cell cycle and angiogenesis, promotes apoptosis

76
Q

Rituximab

A

CD20

B lymphocytes

77
Q

Alemtuzumab

A

CD52

B and T lymphocytes, NKs, monocytes, macrophages, come granulocytes

78
Q

Gemtuzumab

A

CD33
internalization of antibody +ozogamicin&raquo_space; DNA ds breaks and cell death
Leukemic blast cells

79
Q

Trastuzumab

A

Her2/Neu

80
Q

Ibritumomab

A

CD20

Combined with a chelator, acts as delivery of radioactive isotopes to cancer cells

81
Q

Tositumomab

A

CD20

Combined with a chelator, acts as delivery of radioactive isotopes to cancer cells

82
Q

Cetuximab

A

EGFR

83
Q

Bevacizumab

A

VEGF