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Cancer Chemotherapy 2 Flashcards

1
Q

antimetabolites general MOA

A

compounds that mimic endogenous biochemicals required for DNA, RNA synthesis or function of key enzymes

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2
Q

what drugs are antimetabolites

A

Methotrexate (folic acid)
5-fluorouracil (pyrimidines)
6-mercaptoprurine (purines)

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3
Q

how do folic acid and methotrexate differ

A

methotrexate has an extra methyl group

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4
Q

methotrexate MOA

A

resembles folic acid and binds to DHFR

1000x affinity for DHFR than folate

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5
Q

what drugs are folic acid analogs

A

methotrexate
trimetrexate
pemetrexed

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6
Q

pemetrexed is a newer derivative of methotrexate and is better why?

A

it can directly inhibit individual enzymes in purine synthesis pathway (Thymidylate sythase, GAR and AICAR formyltransferases) as well as DHFR

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7
Q

folic acid analogs inhibit what phase of the cell cycle

A

CCS-S phase

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8
Q

what are the toxic side effects of folic acid analogs

A

hepatotoxicity
pulmonary toxicity
Oral and GI ulceration

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9
Q

how can one minimize the toxic effects of folate depletion in normal cells

A 
Leucovorin rescue (only affects non-tumor cells)
administered 24-36 hours after methotrexate
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10
Q

capecitabine is a prodrug that gets converted to what by carboxyesterases and cytidine dreaminess in the liver

A

5-FU

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11
Q

capecitabine and gemcitabine are analogs of what

A

pyrimidine

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12
Q

5-FU effects the cell cycle when

A

CCNS; C1 and S-phases

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13
Q

5-FU MOA

A

decreased DNA synthesis by inhibiting thymidylate sythase
incorporation into DNA (unstable)
incorporation into RNA (altered function)

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14
Q

what toxicities are associated with 5-FU

A

oral and GI ulceration

stomatitis and diarrhea (stop medication)

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15
Q

cytarabine effects the cell cycle when

A

CCS-S phase

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16
Q

Gemcitabine effects the cell cycle when

A

CCNS

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17
Q

MOA of cytarabine

A

inhibits DNAPol-alpha

incorporation into DNA

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18
Q

what drug inhibits DNAPol-alpha

A

cytarabine

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19
Q

what is the active form of 5-FU

A

5-FdUMP

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20
Q

what two drugs inhibit thymidylate sythase

A

5-FU

pemetrexed (PEM)

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21
Q

the metabolism of 6-mercaptopurine is inhibited by what

A

allopurinol

gotta lower dose in ppl w/ gout on this drug

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22
Q

MOA of 6-mercaptopurine

A

inhibits synthesis of adenine and guanine by blocking the conversion of inosinate to purine precursors

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23
Q

what drug is a potent “pseudo-feedback inhibitor or purine biosynthesis”

A

6-mercaptopurine

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24
Q

6-mercaptopurine effects the cell cycle where

A

CCS-S phase

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25
What toxicities are associated with 6-mercaptopurine
cholestasis oral and intestinal ulcers
26
ADA inhibitors MOA
inhibit ADA directly or via metabolites- build up of adenosine and dAdenosine nucleotides decreases DNA synthesis by inhibiting ribonucleotide reductase
27
ribonucleotide reductase is inhibited by what drug
ADA inhibitors
28
ADA inhibitors are used to treat what
hairy cell leukemia
29
what drugs are tubulin-binding agents
vinca alkaloids | yew alkaloids
30
what drugs are vinca alkaloids
vincristine vinblastine vinorelbine
31
what drugs are yew alkaloids
Paclitaxel (taxol) | docetaxel
32
MOA of vinca alkaloids (vincristine, vinblastine, vinorelbine)
bind specifically to soluble tubulin to block polymerization | arrests cellular mitosis in metaphase
33
vinca alkaloids (vincristine, vinblastine, vinorelbine) effect the cell cycle when
CCS-M phase
34
what toxicity is associated with vinca alkaloids (vincristine, vinblastine, vinorelbine)
peripheral neuropathy alopecia (hair loss) SAIDH
35
what drugs have SIADH as toxic side effects
``` cyclophosphamide vinca alkaloids (vincristine, vinblastine, vinorelbine) ```
36
MOA of paclitaxel (and docetaxel)
prevents microtubule depolymerization by bind to and stabilizing polymerized tubulin
37
paclitaxel (and docetaxel) effects the cell cycle when
CCS-M
38
what toxic side effects re associated with paclitaxel (and docetaxel)
peripheral neuropathy (dose limiting)
39
which interferon is an anti-cancer drug
IFN-alpha
40
MOA of IFN-alpha
inhibits tumors by regulating the host immune system of the patient direct activity against cancer cells
41
IFN-alpha effects the cell cycle when
CCNS slows G1 to S and S to G2
42
what cancers are hormone responsive
breast, endometrial, prostate
43
MOA of prednisone
anti-inflammatory property and alter immune responses | cause apoptosis in certain leukemia cells
44
prednisone is used to treat what
Hodgkin's disease (MOPP), acute leukemias, relapsed hairy cell leukemia lymphomas manage hemolytic anemia and hemorrhagic complications of lymphomas and CLL
45
what drug is used to manage hemolytic anemia and hemorrhagic complications of lymphomas and CLL
prednisone
46
Progestins (synthetic progesterones and its derivatives) MOA
used in hormone responsive cancers expressing progesterone receptors
47
What drugs are anti estrogens
tamoxifen and toremefine
48
anti estrogens (tamoxifen and toremefine) are used to tread what
estrogen receptor positive breast cancer
49
what is the stipulation with anti estrogens (tamoxifen and toremefine)
tamoxifen is not steroid | both have week estrogen affinity
50
MOA of anti-androgens (cased, eulixin, nilandron)
blocks androgen-induced growth | normally combined with leuprolide or other luteinizing hormone releasing hormone (LHRH) agonist
51
the combination of anti-androgens with leuprolide facilitates what
total androgen ablation
52
leuprolide (LHRH agonist) MOA
blocks release of luteinizing hormone from pituitary gland
53
what does the suffix "mab" stand for
monoclonal antibody
54
what is an example of ligand-independent receptor commonly found in breast cancers
ERBB2/Her2/Neu
55
how are antibodies used in treatment of cancer
block cell surface receptors which promote tumor growth | block receptors which facilitate tumor angiogenesis
56
ERBB1 and ERBB2 promote tumor growth how
constitutively active
57
MOA of Bevuczimab
blocks VEGF and prevents angiogenesis
58
MOA of Denusomab
blocks RANK-RANKL in bone
59
MOA of Traztuzumab
blocker Her2/Neu
60
targeted inhibitors of cancer growth work how
target intracellular growth pathways overexpressed/amplified in cancer
61
Imatinib MOA
blocks Bcr-Abl kinase
62
what drug has a response rate of about 100% in the chronic phase of CML
Imatinib
63
Erlotinib,Geftinib MOA
blocks EGFR signaling
64
Crizotinib MOA
blocks ALK-1 kinase
65
suffix "inib" stands for what
inhibitor
66
drugs that inhibit anti-apoptotic proteins target what
Bcl-2
67
Venetoclax MOA
binds Bcl-2 and inhibits its anti-apoptotic activity
68
venetoclax is approved to treat what
refractory chronic lymphocytic leukemia
69
drugs that target epigenetic signaling target what
histone deacyetylases (HDACs)
70
Vorinostat and Romidepsin are examples of what type of anti-cancer drug
HDAC (histone deacyetylase) inhibitors
71
what is the normal function of PARP-1
rescue cells by base excision repair
72
inhibition of PARP-1 leads to what
cellular apoptosis
73
Olaparib MOA
PARP-1 inhibitor which leads to increased DNA damage, this damage cannot be fixed by homologous recombination with BRCA mutations are present
74
Olaparib is approved for use in what
ovarian cancer that contains BRCA1/BRCA2

Chemotherapy drugs (2 decks)

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