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pharmacology 3.2 > anti-cancer drugs > Flashcards

anti-cancer drugs Flashcards

1
Q

5 types of older anti-cancer drugs

A
  • alkylating agents
  • anti-metabolites
  • plant alkaloids
  • antibiotics
  • topoisomerase inhibitor
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2
Q

4 types of newer anti-cancer drugs

A
  • hormones
  • immune-modulating agents
  • receptor and non-receptor tyrosine kinase inhibitors
  • oncolytic viruses
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3
Q

which phase cell cyle alkylating agents work?

A

on all phases in cell cycle

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4
Q

what alkylating agents do?

A
  1. bind to nucleophilic substances
  2. formation of carbonium ion
  3. intra and interchain cross linking
  4. N7-guanine, N1 and N3-adenine, N3-cytosine
  5. DNA damage and mispairing of nucleotides leading to mutations
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5
Q

what type of cancer for alkylating agents?

A
  • leukaemia
  • non-hodgkin’s lymphoma
  • hodgkin disease
  • m.myeloma
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6
Q

examples of alkylating agents

A
  • cyclophosphamide
  • carmustine
  • lomustine
  • busulphan
  • dacarbazine
  • thiotepa
  • cisplatin
  • carboplatin
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7
Q

which phase of cell cycle antimetabolites work?

A

S phase

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8
Q

what type of cancer for antimetabolites?

A
  • leukaemia
  • breast cancer
  • ovary cancer
  • GI tumours
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9
Q

examples of antimetabolites

A
  • antifolates: methotrexate(DMARD)
  • purine analogs: 6- mercaptopurine, 6- thioguanine, pentostatin
  • pyrimidine analogs: 5- fluorouracil
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10
Q

how antifolates do?

A
  1. methotrexate binds to DHFR
  2. inhibits DHF reduction
  3. depletion of tetrahydrofolate
  4. inhibits DNA synthesis
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11
Q

how purine analogs do? (6- mercaptopurine, 6- thioguanine)

A
  1. converted to fraud nucleotides
  2. inhibits first step in de novo purine synthesis
  3. inhibits DNA/RNA synthesis
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12
Q

how purine analogs do? (pentostatin)

A
  1. inhibits adenosine deaminase
  2. catalyzes adenosine to inosine
  3. interferes with purine metabolism and cell proliferation
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13
Q

how pyrimidine analogs do?

A
  1. converted into nucleotide and form 5-‘FdUMP
  2. 5-FdUMP is a direct inhibitor of thymidylate synthetase
  3. inhibits DNA synthesis
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14
Q

which phase of cell cylce plant alkaloids work?

A

M phase

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15
Q

what type of cancer for plant alkaloids?

A
  • metastatic testicular cancer
  • lymphoma
  • kaposi’s sarcoma
  • breast cancer
  • neuroblastoma
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16
Q

examples of plant alkaloids

A
  • vinca alkaloids (vineristine, vinblastine, vindesine)

- taxanes (paelitaxel, docetaxel

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17
Q

how vinca alkaloids do?

A
  1. bind to tubulin
  2. prevention of spindle formation
  3. arrest metaphase
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18
Q

how taxanes do?

A
  1. bind to microtubules
  2. antagonises microtubule disassembly
  3. arrest in metaphase
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19
Q

examples of antibiotics (anthracyclines)

A
  • doxorubicin
  • daunorubicin
  • idarubicin
  • dactinomycin
  • mitomycin
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20
Q

how antibiotics do?

A
  1. intercalation between DNA bases or binds to DNA-topo II complex
  2. DNA strand breakage
  3. inhibition of topoisomerase II
  4. inhibition of DNA synthesis
21
Q

examples of topoisomerase I inhibitors

A
  • etoposide
  • irinotecan
  • topotecan
22
Q

examples of topoisomerase II inhibitors

A
  • etoposide
  • doxorubicin
  • amsacrine
  • mitoxantrone
23
Q

how topoisomerase inhibitors do?

A
  1. impairing the ability of topo to replicate DNA
  2. enhance the rate of DNA cleavage
  3. inhibits DNA synthesis
24
Q

how hormone works?

A
  • slow down the spread of cancer cells
  • ease pain caused by cancer cells
  • shrink the tumour before surgery to reduce spread
25
Q

examples of anti-oestrogen

A
  • tamoxifen

- fulvestrant

26
Q

how tamoxifen do?

A
  • as competitive partial antagonist of oestrogen receptor

- prevent osteoporosis

27
Q

how fulvestrant do?

A

as antagonist of oestrogen receptor

28
Q

exampes of anti-androgens

A
  • flutamide
  • bicalutamide
  • cyproterone acetate
29
Q

how anti- androgens do?

A

compete with testosterone for binding to androgen receptors in prostate gland

30
Q

examples of aromatase inhibitors

A
  • exemestane
  • anastrozole
  • letrozole
31
Q

how aromatase inhibitors do?

A

inhibiton of oestrogen production from androgens

32
Q

types of hormone therapy

A
  • anti-oestrogen
  • anti-androgens
  • aromatase inhibitors
  • LHRH analogs
  • LHRH antagonist
  • corticosteroids
33
Q

examples of LHRH analogs

A
  • leuprolide
  • goserelin
  • triptorelin
34
Q

how LHRH analogs do?

A
  1. stimulate pituitary’s GnRH receptor
  2. inducing negative feedback inhibition
  3. reduce production of LH and testosterone
35
Q

examples of LHRH antagonists

A
  • abarelix

- degarelix

36
Q

how LHRH antagonist do?

A
  1. reduce levels of LH, FSH and testosterone

2. no initial flare up

37
Q

examples of corticosteroids

A
  • prednisone
  • dexamethasone
  • prednisolone
  • hydrocortisone
38
Q

how corticosteroids do?

A
  1. reduction of ACTH secretion

2. inhibition of lymphocyte proliferation

39
Q

types of immune-modulating agents

A
  • vaccines
  • cytokines
  • immunotherapies overcome tolerance
  • ipilimumab
40
Q

examples of prophylactic vaccines

A
  • gardasil

- cervarix

41
Q

examples of therapeutic vaccines

A
  • cell based vaccines
  • tumour associated antigens
  • peptide vaccines
42
Q

examples of cytokines

A
  • GM-CSF
  • IL-2
  • IL-12
43
Q

example of immunotherapies overcome tolerance

A

treg cell depletion

44
Q

characteristics od ipilimumab

A
  • recombinant monoclonal antibody
  • target at CTLA-4
  • used in malignant melanoma
45
Q

how receptor and non-receptor TK modulators do?

A
  • using small molecule inhibitors that interfere with binding of ATP
  • monoclonal antibodies against receptor TKs or ligands
46
Q

examples of small molecules

A
  • imatinib mesylate (philadephia chr)
  • lapatinib
  • canertinib
  • gefitinib
  • erlotinib
47
Q

examples of moAbs

A
  • trastuzumab
  • cetuximab
  • panitumumab
  • bevacizumab
48
Q

how oncolytic viruses do?

A

viruses inserted into cells to activate antibodies and delivered to tumour

49
Q

why cancer cells cause no production of antibodies?

A

cancer cells cause genetic mutations, resulting in loss of interferon production

pharmacology 3.2 (4 decks)

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