anti-cancer drugs Flashcards
(49 cards)
1
Q
5 types of older anti-cancer drugs
A
- alkylating agents
- anti-metabolites
- plant alkaloids
- antibiotics
- topoisomerase inhibitor
2
Q
4 types of newer anti-cancer drugs
A
- hormones
- immune-modulating agents
- receptor and non-receptor tyrosine kinase inhibitors
- oncolytic viruses
3
Q
which phase cell cyle alkylating agents work?
A
on all phases in cell cycle
4
Q
what alkylating agents do?
A
- bind to nucleophilic substances
- formation of carbonium ion
- intra and interchain cross linking
- N7-guanine, N1 and N3-adenine, N3-cytosine
- DNA damage and mispairing of nucleotides leading to mutations
5
Q
what type of cancer for alkylating agents?
A
- leukaemia
- non-hodgkin’s lymphoma
- hodgkin disease
- m.myeloma
6
Q
examples of alkylating agents
A
- cyclophosphamide
- carmustine
- lomustine
- busulphan
- dacarbazine
- thiotepa
- cisplatin
- carboplatin
7
Q
which phase of cell cycle antimetabolites work?
A
S phase
8
Q
what type of cancer for antimetabolites?
A
- leukaemia
- breast cancer
- ovary cancer
- GI tumours
9
Q
examples of antimetabolites
A
- antifolates: methotrexate(DMARD)
- purine analogs: 6- mercaptopurine, 6- thioguanine, pentostatin
- pyrimidine analogs: 5- fluorouracil
10
Q
how antifolates do?
A
- methotrexate binds to DHFR
- inhibits DHF reduction
- depletion of tetrahydrofolate
- inhibits DNA synthesis
11
Q
how purine analogs do? (6- mercaptopurine, 6- thioguanine)
A
- converted to fraud nucleotides
- inhibits first step in de novo purine synthesis
- inhibits DNA/RNA synthesis
12
Q
how purine analogs do? (pentostatin)
A
- inhibits adenosine deaminase
- catalyzes adenosine to inosine
- interferes with purine metabolism and cell proliferation
13
Q
how pyrimidine analogs do?
A
- converted into nucleotide and form 5-‘FdUMP
- 5-FdUMP is a direct inhibitor of thymidylate synthetase
- inhibits DNA synthesis
14
Q
which phase of cell cylce plant alkaloids work?
A
M phase
15
Q
what type of cancer for plant alkaloids?
A
- metastatic testicular cancer
- lymphoma
- kaposi’s sarcoma
- breast cancer
- neuroblastoma
16
Q
examples of plant alkaloids
A
- vinca alkaloids (vineristine, vinblastine, vindesine)
- taxanes (paelitaxel, docetaxel
17
Q
how vinca alkaloids do?
A
- bind to tubulin
- prevention of spindle formation
- arrest metaphase
18
Q
how taxanes do?
A
- bind to microtubules
- antagonises microtubule disassembly
- arrest in metaphase
19
Q
examples of antibiotics (anthracyclines)
A
- doxorubicin
- daunorubicin
- idarubicin
- dactinomycin
- mitomycin
20
Q
how antibiotics do?
A
- intercalation between DNA bases or binds to DNA-topo II complex
- DNA strand breakage
- inhibition of topoisomerase II
- 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
- impairing the ability of topo to replicate DNA
- enhance the rate of DNA cleavage
- 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
examples of anti-oestrogen
- tamoxifen
| - fulvestrant
26
how tamoxifen do?
- as competitive partial antagonist of oestrogen receptor
| - prevent osteoporosis
27
how fulvestrant do?
as antagonist of oestrogen receptor
28
exampes of anti-androgens
- flutamide
- bicalutamide
- cyproterone acetate
29
how anti- androgens do?
compete with testosterone for binding to androgen receptors in prostate gland
30
examples of aromatase inhibitors
- exemestane
- anastrozole
- letrozole
31
how aromatase inhibitors do?
inhibiton of oestrogen production from androgens
32
types of hormone therapy
- anti-oestrogen
- anti-androgens
- aromatase inhibitors
- LHRH analogs
- LHRH antagonist
- corticosteroids
33
examples of LHRH analogs
- leuprolide
- goserelin
- triptorelin
34
how LHRH analogs do?
1. stimulate pituitary's GnRH receptor
2. inducing negative feedback inhibition
3. reduce production of LH and testosterone
35
examples of LHRH antagonists
- abarelix
| - degarelix
36
how LHRH antagonist do?
1. reduce levels of LH, FSH and testosterone
| 2. no initial flare up
37
examples of corticosteroids
- prednisone
- dexamethasone
- prednisolone
- hydrocortisone
38
how corticosteroids do?
1. reduction of ACTH secretion
| 2. inhibition of lymphocyte proliferation
39
types of immune-modulating agents
- vaccines
- cytokines
- immunotherapies overcome tolerance
- ipilimumab
40
examples of prophylactic vaccines
- gardasil
| - cervarix
41
examples of therapeutic vaccines
- cell based vaccines
- tumour associated antigens
- peptide vaccines
42
examples of cytokines
- GM-CSF
- IL-2
- IL-12
43
example of immunotherapies overcome tolerance
treg cell depletion
44
characteristics od ipilimumab
- recombinant monoclonal antibody
- target at CTLA-4
- used in malignant melanoma
45
how receptor and non-receptor TK modulators do?
- using small molecule inhibitors that interfere with binding of ATP
- monoclonal antibodies against receptor TKs or ligands
46
examples of small molecules
- imatinib mesylate (philadephia chr)
- lapatinib
- canertinib
- gefitinib
- erlotinib
47
examples of moAbs
- trastuzumab
- cetuximab
- panitumumab
- bevacizumab
48
how oncolytic viruses do?
viruses inserted into cells to activate antibodies and delivered to tumour
49
why cancer cells cause no production of antibodies?
cancer cells cause genetic mutations, resulting in loss of interferon production
