Anticancer drugs Flashcards

1
Q

Bendamustine

A

Alkylating agent - Nitrogen mustard

Interfere with cellular replication by forming cross-linkages between DNA strands.

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2
Q

Busulfan

A

Alkylating agent

Interfere with cellular replication by forming cross-linkages between DNA strands.

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3
Q

Carmustine

A

Alkylating agent - Nitrosourea

Interfere with cellular replication by forming cross-linkages between DNA strands.

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4
Q

Chlorambucil

A

Alkylating agent - Nitrogen mustard

Interfere with cellular replication by forming cross-linkages between DNA strands.

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5
Q

Cyclophosphamide

A

Alkylating agent - Nitrogen mustard

Interfere with cellular replication by forming cross-linkages between DNA strands.

Immunosuppressant properties are considered to be due to cytotoxic effect on lymphocytes.

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6
Q

Dacarbazine

A

Alkylating agent - Triazene

Interfere with cellular replication by forming cross-linkages between DNA strands.

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7
Q

Ifosfamide

A

Alkylating agent - Nitrogen mustard

Interfere with cellular replication by forming cross-linkages between DNA strands.

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8
Q

Melphalan

A

Alkylating agent - Nitrogen mustard

Interfere with cellular replication by forming cross-linkages between DNA strands.

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9
Q

Procarbazine

A

Alkylating agent

Interfere with cellular replication by forming cross-linkages between DNA strands.

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10
Q

Temozolomide

A

Alkylating agent - Triazene

Interfere with cellular replication by forming cross-linkages between DNA strands.

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11
Q

Thiotepa

A

Alkylating agent

Interfere with cellular replication by forming cross-linkages between DNA strands.

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12
Q

Daunorubicin

A

Anthracycline

Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines

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13
Q

Doxorubicin

A

Anthracycline

Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines

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14
Q

Epirubicin

A

Anthracycline

Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines

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15
Q

Idarubicin

A

Anthracycline

Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines

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16
Q

Mitozantrone

A

Anthracycline

Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines

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17
Q

Brentuximab vedotin

A

Antibody-drug conjugate

Conjugate of an antibody (which binds to CD30 on tumour cells) and monomethyl auristatin E (MMAE), a microtubule disrupting agent that induces cell cycle arrest and apoptosis.

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18
Q

Enfortumab vedotin

A

Antibody-drug conjugate

Conjugate of an antibody (which binds to nectin‑4 on tumour cells) and monomethyl auristatin E (a microtubule disrupting agent that induces cell cycle arrest and apoptosis).

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19
Q

Gemtuzumab ozogamicin

A

Antibody-drug conjugate

Conjugate of an antibody (which binds to CD33 on tumour cells) and a cytotoxic agent (N‑acetyl-gamma-calicheamicin, which induces double-stranded DNA breaks and apoptosis).

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20
Q

Inotuzumab ozogamicin

A

Antibody-drug conjugate

Conjugate of an antibody (which binds to CD22 on tumour cells) and a cytotoxic agent (N‑acetyl-gamma-calicheamicin, which induces double stranded DNA breaks and apoptosis).

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21
Q

Sacituzumab govitecan

A

Antibody-drug conjugate

Conjugate of an antibody (which binds to Trop‑2 on tumour cells) and SN‑38 (a topoisomerase I inhibitor and the active metabolite of irinotecan).

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22
Q

Trastuzumab deruxtecan

A

Antibody-drug conjugate

Conjugate of trastuzumab and deruxtecan (a topoisomerase I inhibitor). The actions of deruxtecan result in DNA damage and apoptosis and add to those of trastuzumab.

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23
Q

Trastuzumab emtansine

A

Antibody-drug conjugate

Conjugate of trastuzumab and DM1 (a cytotoxic microtubule inhibitor). The actions of DM1 result in cell cycle arrest and apoptosis and add to those of trastuzumab.

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24
Q

Alemtuzumab

A

Binds to CD52 antigen, which is found on the surface of most B and T lymphocytes, monocytes, macrophages and some granulocytes. Lysis of CD52-positive cells follows via a number of mechanisms.

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25
Q

Atezolizumab

A

Blocks the programmed death ligand 1 (PD‑L1) from binding to its receptors (PD‑1 and B7.1), reactivating cytotoxic T lymphocytes and the anti-tumour immune response.

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26
Q

Avelumab

A

Binds programmed death ligand 1 (PD‑L1) and stops it from binding to its receptors (PD‑1 and B7.1), reactivating cytotoxic T lymphocytes and the anti-tumour immune response.

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27
Q

Bevacizumab

A

Recombinant humanised monoclonal antibody; binds human vascular endothelial growth factor (VEGF) inhibiting formation of new blood vessels, reducing vascularisation and growth of tumours.

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28
Q

Blinatumomab

A

Recombinant bispecific antibody construct that binds to CD19 on B cells and CD3 on T cells, forming a link that results in the activation of T cells to eliminate CD19-positive B cells.

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29
Q

Cemiplimab

A

Inhibits the programmed death 1 (PD‑1) receptor from binding to its ligands (PD‑L1 and PD‑L2) on tumour cells, reactivating cytotoxic T lymphocytes and anti-tumour immunity.

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30
Q

Cetuximab

A

Binds to the epidermal growth factor receptor (EGFR), thereby inhibiting proliferation and inducing apoptosis of tumour cells that over-express EGFR.

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31
Q

Daratumumab

A

Binds CD38 protein which is highly expressed on plasma cell clones in multiple myeloma and light chain amyloidosis, leading to cell death.

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32
Q

Durvalumab

A

Binds programmed death ligand 1 (PD‑L1) and stops it from binding to its receptors (PD‑1 and B7.1), reactivating cytotoxic T lymphocytes and the anti-tumour immune response.

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33
Q

Elotuzumab

A

Binds SLAMF7 protein which is highly expressed on multiple myeloma cells, leading to cell death.

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34
Q

Ipilimumab

A

Binds to the cytotoxic T lymphocyte-associated antigen 4 (CTLA‑4) resulting in an enhanced T cell mediated immune response which leads to tumour cell death.

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35
Q

Nivolumab

A

Inhibits the programmed death 1 (PD‑1) receptor from binding to its ligands (PD‑L1 and PD‑L2) on tumour cells, reactivating cytotoxic T lymphocytes and anti-tumour immunity.

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36
Q

Obinutuzumab

A

Recombinant humanised monoclonal antibody that binds to CD20 on B lymphocytes resulting in cell lysis.

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37
Q

Panitumumab

A

Binds to the epidermal growth factor receptor (EGFR) resulting in inhibition of cell growth, induction of apoptosis and decreased production of inflammatory cytokines and vascular growth factor.

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38
Q

Pembrolizumab

A

Inhibits the programmed death 1 (PD‑1) receptor from binding to its ligands (PD‑L1 and PD‑L2) on tumour cells, reactivating cytotoxic T lymphocytes and anti-tumour immunity.

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39
Q

Pertuzumab

A

Recombinant humanised monoclonal antibody that binds to human epidermal growth factor receptor 2 (HER2) preventing its pairing with other members of the HER family. This arrests cell growth and induces apoptosis. Pertuzumab also activates an immune response that lyses tumour cells.

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40
Q

Rituximab

A

Binds to CD20 on B lymphocytes.

In cancer, it starts an immune response that lyses normal and malignant B cells. In chronic inflammatory diseases (eg rheumatoid arthritis), it suppresses immune response and inflammation by reducing T cell activation and resulting cytokine production.

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41
Q

Siltuximab

A

Binds to interleukin‑6 (IL‑6), inhibiting signalling pathways involved in B‑lymphocyte and plasma cell proliferation, and in inflammatory and immune responses.

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42
Q

Trastuzumab

A

Recombinant humanised monoclonal antibody that binds to human epidermal growth factor receptor 2 (HER2) and inhibits the proliferation of tumour cells that over-express HER2. Trastuzumab also activates an immune response that lyses tumour cells.

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43
Q

Azacitidine

A

Antimetabolite - Pyrimidine antagonist

Pyrimidine nucleoside analogue of cytidine. Appears to cause hypomethylation of DNA and have direct cytotoxic effects on abnormal haemopoietic cells in bone marrow.

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44
Q

Capecitabine

A

Antimetabolite - Pyrimidine antagonist

Converted to fluorouracil by a 3‑step process in which the final step is more active in malignant than normal cells.

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45
Q

Cladribine

A

Antimetabolite - Purine antagonist

Purine antimetabolite that inhibits DNA repair and synthesis, particularly in lymphocytes and monocytes.

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46
Q

Clofarabine

A

Antimetabolite - Purine antagonist

Purine antimetabolite that inhibits DNA repair and synthesis and induces apoptosis.

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47
Q

Cytarabine

A

Antimetabolite -Pyrimidine antagonist

Pyrimidine nucleoside analogue of cytidine. Cytarabine is converted intracellularly to a nucleotide that inhibits DNA synthesis.

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48
Q

Decitabine with cedazuridine

A

Antimetabolite - Pyrimidine antagonist

Decitabine is pyrimidine analogue that causes DNA hypomethylation leading to reactivation of tumour suppressor genes and apoptosis. Cedazuridine increases the oral bioavailability of decitabine (by inhibiting cytidine deaminase).

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49
Q

Fludarabine

A

Antimetabolite - Purine antagonist

Purine antimetabolite that inhibits DNA synthesis and induces apoptosis. Also reduces RNA and protein synthesis.

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50
Q

Fluorouracil

A

Antimetabolite - Pyrimidine antagonist

Pyrimidine antimetabolite which, following intracellular conversion to active metabolites, interferes with DNA and RNA synthesis.

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51
Q

Gemcitabine

A

Antimetabolite - Pyrimidine antagonist

Pyrimidine nucleoside analogue of cytidine. Gemcitabine is metabolised intracellularly to active nucleosides that inhibit DNA synthesis and induce apoptosis.

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52
Q

Hydroxycarbamide/ hydroxyurea

A

Antimetabolite

Inhibits DNA synthesis by interfering with the conversion of ribonucleotides to deoxyribonucleotides.

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53
Q

Mercaptopurine

A

Antimetabolite - Purine antagonist

Purine antimetabolite. Mercaptopurine is metabolised to thioguanine nucleotides which interfere with purine synthesis, impairing lymphocyte proliferation, cellular immunity and antibody responses. Cross-resistance with tioguanine occurs.

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54
Q

Methotrexate

A

Antimetabolite - Folic acid antagonist

Folic acid antagonist. Inhibits DNA synthesis and cell replication by competitively inhibiting the conversion of folic acid to folinic acid.

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55
Q

Pemetrexed

A

Antimetabolite - Folic acid antagonist

Inhibits key folate-dependent enzymes necessary for the synthesis of purine and thymidine nucleotides essential for cell replication.

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56
Q

Raltitrexed

A

Antimetabolite - Folic acid antagonist

Folate analogue that directly inhibits thymidylate synthetase. This interferes with thymidylic acid formation and in turn with the synthesis of DNA.

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57
Q

Tioguanine

A

Antimetabolite -Purine antagonist

Purine antimetabolite. Tioguanine is metabolised to thioguanine nucleotides which interfere with purine synthesis and formation of DNA and RNA. Cross-resistance with mercaptopurine occurs.

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58
Q

Trifluridine with tipiracil

A

Antimetabolite - Pyrimidine antagonist

Trifluridine is a thymidine analogue which interferes with DNA function in cancer cells, preventing their proliferation. Tipiracil increases the oral bioavailability of trifluridine (inhibits thymidine phosphorylase).

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59
Q

Apalutamide

A

Nonsteroidal Anti-androgens

Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.

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60
Q

Biclutamide

A

Nonsteroidal Anti-androgens

Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.

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61
Q

Darolutamide

A

Nonsteroidal Anti-androgens

Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.

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62
Q

Enzalutammide

A

Nonsteroidal Anti-androgens

Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.

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63
Q

Flutamide

A

Nonsteroidal Anti-androgens

Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.

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64
Q

Cyproterone

A

Steroidal Anti-androgen

Competitively inhibit the binding of androgen at androgen receptors. Cyproterone (a steroidal anti-androgen) also has progestogenic effects that result in decreased production of testosterone.

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65
Q

Anastrozole

A

Aromatase inhibitor

Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to estriol and estradiol. Aromatase inhibitors reduce tissue estrogen concentration.

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66
Q

Exemestane

A

Aromatase inhibitor

Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to estriol and estradiol. Aromatase inhibitors reduce tissue estrogen concentration.

67
Q

Letrozole

A

Aromatase inhibitor

Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to estriol and estradiol. Aromatase inhibitors reduce tissue estrogen concentration.

68
Q

Goserelin

A

Gonadotrophin-releasing hormone agonist

GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum estrogen in females. Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours.

69
Q

Leuprorelin

A

Gonadotrophin-releasing hormone agonist

GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum estrogen in females. Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours.

70
Q

Triptorelin

A

Gonadotrophin-releasing hormone agonist

GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum estrogen in females. Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours.

71
Q

Tamoxifen

A

Selective estrogen receptor modulator

Compete with estrogen for receptor sites in breast tissue (anti-estrogenic effect) inhibiting tumour growth. Also have estrogen agonist activity on endometrium, bone and lipids. Suppression of other growth factors and cytokines may occur.

72
Q

Toremifene

A

Selective estrogen receptor modulator

Compete with estrogen for receptor sites in breast tissue (anti-estrogenic effect) inhibiting tumour growth. Also have estrogen agonist activity on endometrium, bone and lipids. Suppression of other growth factors and cytokines may occur.

73
Q

Abiraterone

A

Inhibits CYP17, reducing androgen synthesis in testicular, adrenal and prostate tumour tissues.

74
Q

Degarelix

A

GnRH antagonist

Inhibits gonadotrophin production, reducing testicular androgen synthesis.

75
Q

Fulvestrant

A

Anti-estrogen

Competitively binds to estrogen receptors resulting in their down-regulation. Inhibits the growth of estrogen receptor-positive tumours.

76
Q

Carboplatin

A

Platinum compound

Platinum compounds are activated within the cell by displacement of chloride ions, leaving positively charged molecules that react with DNA. DNA replication, transcription and cell division are inhibited, ultimately inducing apoptosis. Other mechanisms may also be involved. Platinum compounds are cell cycle nonspecific.

Carboplatin causes more severe myelosuppression than cisplatin, with pronounced effects on platelets.

77
Q

Cisplatin

A

Platinum compound

Platinum compounds are activated within the cell by displacement of chloride ions, leaving positively charged molecules that react with DNA. DNA replication, transcription and cell division are inhibited, ultimately inducing apoptosis. Other mechanisms may also be involved. Platinum compounds are cell cycle nonspecific.

Cisplatin is more emetogenic, nephrotoxic and ototoxic, and causes more neuropathy (often irreversible) than carboplatin.

78
Q

Oxaliplatin

A

Platinum compound

Platinum compounds are activated within the cell by displacement of chloride ions, leaving positively charged molecules that react with DNA. DNA replication, transcription and cell division are inhibited, ultimately inducing apoptosis. Other mechanisms may also be involved. Platinum compounds are cell cycle nonspecific.

79
Q

Bortezomib

A

Proteasome inhibitor

Inhibit proteasomes (which degrade intracellular proteins including those involved in cell cycle control and growth), impairing cell growth which leads to apoptosis.

80
Q

Carfilzomib

A

Proteasome inhibitor

Inhibit proteasomes (which degrade intracellular proteins including those involved in cell cycle control and growth), impairing cell growth which leads to apoptosis.

81
Q

Cabazitaxel

A

Taxane

Promote assembly of tubulin into stable non-functional microtubules, and inhibit disassembly, arresting cell cycles in late G2 and M phase.

82
Q

Docetaxel

A

Taxane

Promote assembly of tubulin into stable non-functional microtubules, and inhibit disassembly, arresting cell cycles in late G2 and M phase.

83
Q

Paclitaxel

A

Taxane

Promote assembly of tubulin into stable non-functional microtubules, and inhibit disassembly, arresting cell cycles in late G2 and M phase.

84
Q

Lenalidomide

A

Thalidomide analogue

Thalidomide and its analogues, lenalidomide and pomalidomide, have multiple modes of action that are not fully understood and may vary depending on the disease. They include induction of apoptosis, anti-proliferative and anti-inflammatory effects, T cell stimulation, and reduced angiogenesis.

85
Q

Pomalidomide

A

Thalidomide analogue

Thalidomide and its analogues, lenalidomide and pomalidomide, have multiple modes of action that are not fully understood and may vary depending on the disease. They include induction of apoptosis, anti-proliferative and anti-inflammatory effects, T cell stimulation, and reduced angiogenesis.

86
Q

Thalidomide

A

Thalidomide analogue

Thalidomide and its analogues, lenalidomide and pomalidomide, have multiple modes of action that are not fully understood and may vary depending on the disease. They include induction of apoptosis, anti-proliferative and anti-inflammatory effects, T cell stimulation, and reduced angiogenesis.

87
Q

Irinotecan

A

Topoisomerase I inhibitor

Inhibit the enzyme topoisomerase I, thereby interfering with coiling and uncoiling of DNA during replication, which inhibits nucleic acid synthesis. Actions are specific for S‑phase.

88
Q

Topotecan

A

Topoisomerase I inhibitor

Inhibit the enzyme topoisomerase I, thereby interfering with coiling and uncoiling of DNA during replication, which inhibits nucleic acid synthesis. Actions are specific for S‑phase.

89
Q

Vinblastine

A

Vinca alkaloid

Bind to tubulin inhibiting its polymerisation and microtubule formation; results in mitotic arrest in metaphase. Cell cycle specific for M phase.

90
Q

Vincristine

A

Vinca alkaloid

Bind to tubulin inhibiting its polymerisation and microtubule formation; results in mitotic arrest in metaphase. Cell cycle specific for M phase.

91
Q

Vinorelbine

A

Vinca alkaloid

Bind to tubulin inhibiting its polymerisation and microtubule formation; results in mitotic arrest in metaphase. Cell cycle specific for M phase.

92
Q

Anagrelide

A

Platelet production inhibitor

Selectively inhibits megakaryocyte maturation, reducing platelet concentration.

93
Q

Arsenic trioxide

A

Not fully understood. Induces partial differentiation and promotes apoptosis of leukaemic cells and may also inhibit angiogenesis.

94
Q

BCG / Mycobacterium bovis

A

Immunostimulant

BCG (bacillus Calmette-Guerin) is live, attenuated Mycobacterium bovis, which produces a local inflammatory reaction, resulting in elimination or reduction of superficial tumour lesions of the bladder.

95
Q

Bleomycin

A

Inhibits DNA and to a lesser extent RNA synthesis, produces single and double strand breaks in DNA possibly by free radical formation.

96
Q

Dactinomycin

A

Complexes with DNA interfering with DNA-dependent RNA synthesis; also has immunosuppressant properties.

97
Q

Eribulin

A

Binds to microtubules inhibiting their growth and induces formation of non-productive tubulin aggregates; arrests cell cycle in G2‑M phase.

98
Q

Etoposide

A

Podophyllotoxin

Inhibits topoisomerase II resulting in DNA strand breaks and inhibition of cell division in the late S and G2 phases of the cell cycle.

99
Q

Everolimus

A

mTOR inhibitor

Binds to the intracellular protein FKBP‑12. The protein–drug complex blocks the activity of mTOR kinase, inhibiting angiogenesis and tumour cell proliferation, growth and survival.

100
Q

Mitomycin

A

Cell cycle nonspecific. Reduced to an active metabolite that cross links DNA, inhibiting its synthesis. At high concentrations, RNA and protein synthesis may also be inhibited.

101
Q

Niraparib

A

Inhibits poly (ADP-ribose) polymerase (PARP) enzymes resulting in DNA damage and apoptosis.

102
Q

Olaparib

A

Inhibits poly (ADP-ribose) polymerase (PARP) enzymes resulting in double-stranded DNA breaks. Tumour cells with mutated non-functional BRCA1 and 2 genes are unable to repair these DNA breaks, resulting in cell death.

103
Q

Pegaspargase

A

Pegaspargase is the pegylated form of E. coli-derived asparaginase. Asparaginase is also known as L‑asparaginase or colaspase.

Asparaginase breaks down L‑asparagine; certain types of leukaemic cells cannot synthesise this essential amino acid and are therefore unable to grow and survive.

104
Q

Romidepsin

A

Inhibits histone deacetylase (HDAC) resulting in altered gene expression, induction of cell differentiation, cell cycle arrest and apoptosis.

105
Q

Selinexor

A

Inhibits the protein exportin 1, leading to reactivation of tumour-suppressing proteins and apoptosis in tumour cells.

106
Q

Sonidegib

A

Binds to smoothened (SMO) transmembrane protein, inhibiting the hedgehog signalling pathway which is abnormally activated in some cancers.

107
Q

Trabectedin

A

Interferes with the cell cycle by binding to DNA and altering its structure, affecting DNA binding proteins and repair pathways.

108
Q

Tretinoin

A

Induces differentiation and inhibits cell proliferation in haemopoietic cell lines.

109
Q

Venetoclax

A

Binds to and inhibits the B cell lymphoma 2 (BCL‑2) protein, which is an anti-apoptotic protein over-expressed in certain tumour cells, triggering cell death.

110
Q

Vismodegib

A

Binds to smoothened (SMO) transmembrane protein, inhibiting the hedgehog signalling pathway which is abnormally activated in some cancers.

111
Q

Vorinostat

A

Inhibits histone deacetylase (HDAC) leading to accumulation of acetylated proteins which induces cell cycle arrest, differentiation or apoptosis.

112
Q

Filgrastim

A

G‑CSF

G‑CSFs stimulate production and differentiation of neutrophils from blood precursor cells.

Pegfilgrastim and filgrastim appear to be clinically equivalent, although febrile neutropenia appears less common with pegfilgrastim.

113
Q

Lipegfilgrastim

A

G‑CSF

G‑CSFs stimulate production and differentiation of neutrophils from blood precursor cells.

Pegylated form of filgrastim; pegylation decreases their renal clearance and increases their half-life; clearance increases as neutrophil count increases. Limited data suggest that lipegfilgrastim is non-inferior to pegfilgrastim.

114
Q

Pegfilgrastim

A

G‑CSF

G‑CSFs stimulate production and differentiation of neutrophils from blood precursor cells.

Pegylated form of filgrastim; pegylation decreases their renal clearance and increases their half-life; clearance increases as neutrophil count increases.

Pegfilgrastim and filgrastim appear to be clinically equivalent, although febrile neutropenia appears less common with pegfilgrastim.

115
Q

Amifostine

A

Prodrug is activated to a free sulfhydryl (thiol) metabolite; its higher concentration in normal cells than cancer cells may explain the selective protection of normal cells from toxic effects of anticancer drugs and radiation.

116
Q

Calcium folinate

A

Bypasses inhibition of dihydrofolate reductase by folic acid antagonists, eg methotrexate (folinic acid rescue) reducing their toxicity. Competes for cellular uptake with methotrexate.

Enhances the inhibition of thymidylate synthetase by fluorouracil, increasing its cytotoxicity.

117
Q

Mesna

A

Contains free sulfhydryl (thiol) groups that interact with urotoxic metabolites, including acrolein, of ifosfamide and cyclophosphamide and reduce the incidence of haemorrhagic cystitis and haematuria. Enhances urinary excretion of cysteine, which may increase uroprotective effect.

118
Q

Palifermin

A

Recombinant human keratinocyte growth factor

Binds to keratinocyte growth factor (KGF) receptor on epithelial cells increasing the rate of cell proliferation. KGF receptor has not been found on haemopoietic cancer cells.

119
Q

Plerixafor

A

Reversible antagonist of the CXCR4 chemokine receptor, inhibiting the binding of CD34+ haemopoietic stem cells to marrow stroma, resulting in their mobilisation into the blood stream.

120
Q

Rasburicase

A

Recombinant urate oxidase enzyme that catalyses the enzymatic oxidation of uric acid into allantoin, which is more water soluble than uric acid and less likely to precipitate in the renal tubules.

121
Q

Abemaciclib

A

Kinase inhibitor

Inhibit cyclin-dependent kinases (CDK) 4 and 6

122
Q

Acalabrutinib

A

Kinase inhibitor

Inhibit Bruton’s tyrosine kinase (BTK)

123
Q

Afatinib

A

Kinase inhibitor

Inhibit epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), HER4

124
Q

Alectinib

A

Kinase inhibitor

Inhibit anaplastic lymphoma kinase (ALK) receptor, rearranged during transfection (RET)

125
Q

Asciminib

A

Kinase inhibitor

Inhibit BCR-ABL1

126
Q

Axitinib

A

Kinase inhibitor

Inhibit vascular endothelial growth factor receptor (VEGFR) types 1–3

127
Q

Binimetinib

A

Kinase inhibitor

Inhibit mitogen-activated extracellular kinases (MEK) 1 and 2

128
Q

Brigatinib

A

Kinase inhibitor

Inhibit ALK receptor, ROS1

129
Q

Cabozantinib

A

Kinase inhibitor

Inhibit hepatocyte growth factor receptor (HGFR, MET), VEGFR type 2, AXL

130
Q

Ceritinib

A

Kinase inhibitor

Inhibit ALK receptor

131
Q

Cobimetinib

A

Kinase inhibitor

Inhibit MEK1, MEK2

132
Q

Crizotinib

A

Kinase inhibitor

Inhibit ALK receptor, MET, ROS1

133
Q

Dabrafenib

A

Kinase inhibitor

Inhibit BRAF (including V600E and V600K)

134
Q

Dasatinib

A

Kinase inhibitor

Inhibit BCR-ABL1, Src family, stem cell factor receptor (c‑Kit), ephrin receptor, platelet-derived growth factor receptor (PDGFR)

135
Q

Encorafenib

A

Kinase inhibitor

Inhibit BRAF (including V600E and V600K)

136
Q

Entrectinib

A

Kinase inhibitor

Inhibit ROS1, tropomyosin receptor kinases (TRK), ALK receptor

137
Q

Erlotinib

A

Kinase inhibitor

Inhibit EGFR

138
Q

Gefitinib

A

Kinase inhibitor

Inhibit EGFR

139
Q

Gilteritinib

A

Kinase inhibitor

Inhibit FLT‑3

140
Q

Ibrutinib

A

Kinase inhibitor

Inhibit BTK

141
Q

Idelalisib

A

Kinase inhibitor

Inhibit phosphatidylinositol 3‑kinase

142
Q

Imatinib

A

Kinase inhibitor

Inhibit BCR-ABL1, c‑Kit, PDGFR

143
Q

Lapatinib

A

Kinase inhibitor

Inhibit EGFR, HER2

144
Q

Larotrectinib

A

Kinase inhibitor

Inhibit TRK

145
Q

Lenvatinib

A

Kinase inhibitor

Inhibit VEGFR types 1–3, fibroblast growth factor receptor (FGFR) types 1–4, PDGFR, c‑Kit, RET

146
Q

Lorlatinib

A

Kinase inhibitor

Inhibit ALK receptor, ROS1

147
Q

Midostaurin

A

Kinase inhibitor

Inhibit VEGFR type 2, PDGFR, c‑Kit, FLT‑3, protein kinase C

148
Q

Nilotinib

A

Kinase inhibitor

Inhibit BCR-ABL1, c‑Kit, ephrin receptor, PDGFR

149
Q

Nintedanib

A

Kinase inhibitor

Inhibit VEGFR types 1–3, PDGFR, FGFR types 1–3

150
Q

Osimertinib

A

Kinase inhibitor

Inhibit EGFR (including T790M mutation)

151
Q

Palbociclib

A

Kinase inhibitor

Inhibit CDK4, CDK6

152
Q

Pazopanib

A

Kinase inhibitor

Inhibit VEGFR types 1–3, PDGFR, c‑Kit

153
Q

Ponatinib

A

Kinase inhibitor

Inhibit BCR-ABL1, c‑Kit, FLT‑3, RET

154
Q

Regorafenib

A

Kinase inhibitor

Inhibit VEGFR types 1–3, PDGFR, c‑Kit, RET; also inhibits Raf kinases

155
Q

Ribociclib

A

Kinase inhibitor

Inhibit CDK4, CDK6

156
Q

Ripretinib

A

Kinase inhibitor

Inhibit PDGFR, c‑Kit

157
Q

Ruxolitinib

A

Kinase inhibitor

Inhibit JAK1, JAK2

158
Q

Sorafenib

A

Kinase inhibitor

Inhibit VEGFR types 2–3, PDGFR, c‑Kit, FLT‑3; also inhibits Raf kinases

159
Q

Sunitinib

A

Kinase inhibitor

Inhibit VEGFR types 1–3, PDGFR, c‑Kit, FLT‑3

160
Q

Tepotinib

A

Kinase inhibitor

Inhibit MET

161
Q

Trametinib

A

Kinase inhibitor

Inhibit MEK1, MEK2

162
Q

Vandetanib

A

Kinase inhibitor

Inhibit VEGFR types 2–3, EGFR, RET

163
Q

Vemurafenib

A

Kinase inhibitor

Inhibit
BRAF V600E and V600K

164
Q

Zanubrutinib

A

Kinase inhibitor

Inhibit BTK