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study guide Flashcards

1
Q

5-fluorouracil (5-FU):
Target:
Class:
CC phase:
DL SE:

A

thymidylate synthase
antimetabolite (uridine analog)
S
myelosuppression

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2
Q

5-FU rescue

A

thymidine

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3
Q

5-FU drug synergy

A

Leucovorate

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4
Q

5-FU unique resistance mechanism

A

downregulation of enzyme that convert 5-FU to F-dUMP

increase thymidylate synthase

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5
Q

5-FU genetic testing

A

5% of pop has polymorphism that results in deficiency of DPD

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6
Q

Cytarabine (Ara-C)
Target:
Class:
CC phase:
DL SE:

A
  • Comp inh of DNA polymerase alpha
  • antimetabolite (cytosine analog)
  • S phase
  • myelosuppression
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7
Q

Cytarabine (Ara-C) synergy

A

tetrahydrouridine (cytidine deaminase inhibitor)

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8
Q

Cytarabine (Ara-C) resistance mechanisms

A

downregulation of enzymes that upregulate cytidine deaminase

downregulation of influx transporters

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9
Q

6-Mercaptopurine (6-MP)
Target:
Class:
CC phase:
DL SE:

A
  • multiple enzymes in de novo purine synthesis (blocks synth of purine nucleotides)
  • antimetabolite (purine analog, thio-analog of adenine)
  • S
  • myelosuppression, hematologic toxicity
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10
Q

what drug increases 6-MP toxicity?

A

allopurinol

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11
Q

unique mechanisms resistance 6-MP

A

loss of HGPRT (activating enzyme)

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12
Q

6-MP genetic testing

A

TPMT polymorphism loss of function

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13
Q

methotrexate
Target:
Class:
CC phase:
DL SE:

A
  • DHFR inhibitor
  • antifolate
  • S
  • myelosuppression
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14
Q

methotrexate rescue

A

Leucovorin

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15
Q

methotrexate resistance mechanism

A

amplification of DHFR or resistant mutation of DHFR

decreased polyglutamation

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16
Q

Chlorambucil
Target:
Class:
CC phase:
DL SE:

A
  • dna crosslinker
  • alkylator
  • all phases
  • myelosuppression, carcinogenic, teratogenic
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17
Q

unique resistance mechanisms chlorambucil

A

increase glutathione
increased GST
second malignancies

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18
Q

all antimetabolites/antifolates work in which phase of cell cycle

A

s

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19
Q

T or F:
all alkylators have risk of second malignancies

A

true

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20
Q

cyclophosphamide:
Target:
Class:
CC phase:
DL SE:

A
  • DNA crosslinker
  • alkylator (prodrug)
  • all phases
  • hemorrhagic cystitis
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21
Q

what do you give if cyclophosphamide causes hemorrhagic cystitis

A

mesna

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22
Q

Mitomycin C
Target:
Class:
CC phase:
DL SE:

A
  • bifunctional adducts on DNA
  • alkylator (aziridine)
  • all phases
  • myelosuppression
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23
Q

Cisplatin
Target:
Class:
CC phase:
DL SE:

A
  • covalent crosslinkers of G and A causing strand breaks (forms intrastrands)
  • platinum compound
  • all phases
  • bone marrow, nephrotoxicity (proximal tubule)
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24
Q

T or F:
Cisplatin has a risk of second malignancies

A

true

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25
Q

irinotecan
Target:
Class:
CC phase:
DL SE:

A
  • topo I
  • topo I inhibitor
  • S phase
  • UGT1A1 polymorphism
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26
Q

irinotecan unique resistance mechanisms

A

PGP overexpression
MRP overexpression
Glutathione-S-Transferase overexpression*
Topoisomerase downregulation or mutation to prevent inhibitor binding

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27
Q

Doxorubicin:
Target:
Class:
CC phase:
DL SE:

A
  • topo II (intercalates and inhibits double strand re-ligation)
  • topo II inhibitor
  • Non-specific but greater G2/M activity
  • cardiotoxicity bc of free radical damage, also tissue damage with extravasation
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28
Q

what drug prevents doxorubicin cardiotoxicity

A

dexrazoxane

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29
Q

unique resistance mechanism doxorubicin

A

glutathione-s-transferase overexpression

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30
Q

bleomycin
Target:
Class:
CC phase:
DL SE:

A
  • imadazole -> free radical, thiazole -> intercalator
  • dual mechanism cytotoxic agent (topo/micro)
  • G2/M
  • pulmonary (blow/bleo)
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31
Q

vincristine
Target:
Class:
CC phase:
DL SE:

A
  • tubulin -> inhibition of microtubule assembly (tubule polymerization) and microtubule shortening
  • Vinca alkaloid (microtubule destabilizer)
  • M
  • Neurotoxicity, peripheral neuropathy, myelosuppression rarely significant
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32
Q

Eribulin
Target:
Class:
CC phase:
DL SE:

A
  • tubulin -> inhibition of microtubule assembly/elongation
  • microtubule destabilizer
  • M
  • lower neurotoxicity than vinca
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33
Q

Paclitaxel
Target:
Class:
CC phase:
DL SE:

A
  • tubulin -> inhibition of microtubule assembly (depolymerization)
  • taxane -> microtubule stabilizer
  • M
  • myelosuppression, neurotoxicity is reversible
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34
Q

Paclitaxel unique resistance mechanism

A

PgP substrate (except for cabazitaxel)

tubulin mutations

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35
Q

Ixabepilone
Target:
Class:
CC phase:
DL SE:

A
  • tubulin -> inhibition of microtubule disassembly (depolymerization)
  • microtubule stabilizer (epothilone B analog)
  • M
  • reversible myelosuppression
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36
Q

Ixabepilone (is/is not) cross-resistant to taxanes

A

is not

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37
Q

T or F:
Ixabepilone is a poor PgP substrate

A

true

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38
Q

Enzalutamide
Target:
Class:
CC phase:
DL SE:

A
  • androgen receptor
  • full AR antagonist
  • not cell cycle specific
  • none listed
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39
Q

enzalutamide unique resistance mechanism

A

AR mutations that result in castration resistant prostate cancer (CRPC)

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40
Q

Abiraterone
Target:
Class:
CC phase:
DL SE:

A
  • 17-a-hydrolase and C17,20 lyase
  • steroid analog
  • not cell cycle
  • increased cholesterol
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41
Q

tamoxifen
Target:
Class:
CC phase:
DL SE:

A
  • ER
  • SERM
  • not cell cycle specific
  • hot flashes, increased risk of endometrial cancer
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41
Q

fulvestrant
Target:
Class:
CC phase:
DL SE:

A
  • ER
  • SERD (antagonist only)
  • not cell cycle specific
  • n/a
42
Q

tamoxifen random drug interaction thing

A

BC prophylaxis

42
Q

Predinisolone
Target:
Class:
CC phase:
DL SE:

A
  • no target listed?
  • corticosteroid
  • no cell cycle phase
  • no important SE
43
Q

Letrozole
Target:
Class:
CC phase:
DL SE:

A
  • aromatase
  • non-steroidal comp aromatase inhibitor
  • no cell cycle phase shit
  • bone density loss/ fracture
43
Q

Exemestane
Target:
Class:
CC phase:
DL SE:

A
  • aromatase
  • steroidal aromatase inhibitor (suicide inhibitor/irreversible)
  • no cell cycle shit here
  • hot flashes, edema, weight gain, increased cholesterol *
44
Q

Leuprolide
Target:
Class:
CC phase:
DL SE:

A
  • GnRH receptor
  • GnRH analog
  • no phase
  • “flare effects”, hot flashes, sexual dysfxn, gynecomastia
45
Q

Imatinib
Target:
Class:
CC phase:
DL SE:

A
  • BCR-Abl TK
  • type II small molecule Bcr-Abl inhibitor
  • no phase
  • N/V, fluid retention, neutropenia, thrombocytopenia
46
Q

Imatinib genetic testing

A

philadelphia chromosome

47
Q

Ponatinib
Target:
Class:
CC phase:
DL SE:

A
  • Bcr-Abl
  • Bcr-Abl inhibitor
  • no cell cycle shit
  • no important SE
48
Q

Midostaurin:
Target:
Class:
CC phase:
DL SE:

A
  • fms-like TK 3 (FLT3) in AML
  • 1st gen FLT3 inhibitor
  • no phase
  • no crazy SEe
49
Q

Creneolanib
Target:
Class:
CC phase:
DL SE:

A
  • fms-like TK 3 (FLT3)
  • 2nd gen FLT3 inhibitor for AML
  • no cell cycle shit
  • no se listed
50
Q

Quizartinib
Target:
Class:
CC phase:
DL SE:

A
  • FLT3
  • type II FLT3 inhibitor
  • no cell cycle shit
  • no listed SE
51
Q

Quizartinib genetic testing thing *

A

specific for internal tandem duplication (ITD) mutations

52
Q

Sirolimus
Target:
Class:
CC phase:
DL SE:

A
  • mTOR (mammalian target of Rapamycin)
  • Rapamycin analogs
  • no cell cycle
53
Q

sirolimus random drug interaction thing

A

inhibits immune response by blocking IL-2 signaling transduction

54
Q

Alectinib
Target:
Class:
CC phase:
DL SE:

A
  • anaplastic TK (ALK)
  • ALK inhibitor
  • no cell cycle shit
  • no crazy SE
55
Q

Alectinib genetic testing thing *

A

Fusion gene of ALK to ELM4

56
Q

Dabrafenib
Target:
Class:
CC phase:
DL SE:

A
  • BRAF-V600
  • 2nd gen BRAF inhibitor
  • no cell cycle
  • no listed SEs
57
Q

Dabrafenib is paired with what other drug for BRAF-V600 mutant metastatic melanoma

A

trametinib

58
Q

Genetic testing thing for dabrafenib

A

BRAF-V600 mutationt

59
Q

Trametinib
Target:
Class:
CC phase:
DL SE:

A
  • MEK1 and MEK2
  • type III allosteric MEK inhibitor
  • no cell cycle shit
  • RASH, diarrhea, lymphedema
60
Q

Acalabrutinib
Target:
Class:
CC phase:
DL SE:

A
  • Brutons TK (BTK)
  • 2nd gen covalent BTK inhibitor
  • no cell cycle shit
  • no listed SE
61
Q

Afatinib
Target:
Class:
CC phase:
DL SE:

A
  • Covalent inhibitor of al ErBb receptors
  • EGFR inhibitor
  • no cell cycle
  • rash
62
Q

Afatinib genetic testing stuff

A

QIAGEN for detection of exon 19 or 21 deletions/mutations

63
Q

gefitinib
Target:
Class:
CC phase:
DL SE:

A
  • EGFR TK
  • 1st gen reversible EGFR inhibitor
  • no cell cycle
  • fatigue, RASH, diarrhea
64
Q

what mutation causes resistance to gefitinib

65
Q

genetic testing gefitinib

A

exon 19 or 21 mutations

66
Q

osimertinib
Target:
Class:
CC phase:
DL SE:

A
  • EGFR TK
  • 3rd gen covalent EGFR inhibitor
  • no cell cycle
  • rash i think
67
Q

Osimertinib genetic testing and fun fact thing

A

t790M mutation, it is effective for this

68
Q

Lapatinib
Target:
Class:
CC phase:
DL SE:

A
  • EGFR and HER2
  • EGFR and HER2 reversible inhibitor, it is a small molecule TKI
  • no cell cycle shit
  • diarrhea, N/V, reversible decrease in cardiotoxicity
69
Q

Lapatinib is commonly combined with what for metastatic breast cancer

A

capecitabine

70
Q

Tucatinib
Target:
Class:
CC phase:
DL SE:

A
  • HER2
  • TK1 HER2 inhibitor
  • no cell cycle
  • reduced SE’s compared to lapatinib or covalent pan-ErBb inhibitors
71
Q

Tucatinib genetic testing

A

HER2+ breast cancer

72
Q

Trastuzumab is combined with what

A

Pertuzumab

73
Q

Trastuzumab/Pertuzumab
Target:
Class:
CC phase:
DL SE:

A
  • HER2
  • Recombinant humanized mAB
  • no cell cycle
  • flu-like sxs, cardiomyopathy
74
Q

what does pertuzumab do that is an important reason it is combined with trastuzumab?

A

it has different binding sites on HER2 and inhibits dimerization

75
Q

Cetuximab
Target:
Class:
CC phase:
DL SE:

A
  • EGFR completely inhibits binding of EGF and TGF-alpha
  • Recombinant chimeric mAB, fully humanized
  • no cell cycle
  • severe infusion reaction, rash, fever
76
Q

bevacizumab
Target:
Class:
CC phase:
DL SE:

A
  • VEGF (ligand), blocks interaction with endothelial receptors
  • recombinant humanized mAB
  • no cell cycle
  • no listed SE’s
77
Q

bevacizumab is used in combo with ______ for 1st line tx of metastatic colorectal cancer

A

5-FU, this drug has no efficacy as a single agent

78
Q

Ramucirumab
Target:
Class:
CC phase:
DL SE:

A
  • VEGF receptor
  • recombinant humanized mAB
  • no cell cycle
  • used in combo with 5-FU
79
Q

Rituximab
*Target:
Class:
CC phase:
DL SE:

A
  • CD20 in normal B lymphocytes and immature pre B cells
  • not sure rn but mAB
  • no cell cycle
  • no se listed
80
Q

Daratumumab
*Target:
Class:
CC phase:
DL SE:

A
  • CD38 on plasma B cells
  • mAB
  • none
  • none listed
81
Q

*Ipilimumab
Target:
Class:
CC phase:
DL SE:

A
  • CTLA-4 receptor -> reverses cytotoxic T lymphocyte inhibition
  • recombinant human mAB
  • none
  • severe immune-mediated adverse effects (inflammatory) (may require steroids)
82
Q

Pembrolizumab
Target:
Class:
CC phase:
DL SE:

A
  • Binds PD-1 receptor expressed on T cells
  • mAB
  • none
  • none listed
83
Q

pembrolizumab genetic testing

A

PDL1 test for tx of NSCLC

84
Q

Atezolizumab
Target:
Class:
CC phase:
DL SE:

A
  • Binds PDL-1 Receptor
  • PDL-1 mAB
  • none
  • none listed
85
Q

Trastuzumab Emtansine
Target:
Class:
CC phase:
DL SE:

A
  • HER2/Neu receptor, emtansine inhibits microtubule assembly
  • ADC, emtansine is cytotoxic
  • none
  • trastuzumab SE’s, emtansine gives thrombocytopenia and hepatotoxicity
86
Q

Trastuzumab Derutexan
Target:
Class:
CC phase:
DL SE:

A
  • HER2/Neu receptor, topo I
  • ADC + topo I inhibitor
  • none
  • trastuzumab effects
87
Q

Blinatumomab
Target:
Class:
CC phase:
DL SE:

A
  • binds CD3 and brings activated T-cell into proximity of CD19
  • BiTE
  • none
  • cytokine release syndrome
88
Q

Mosunetuzumab
Target:
Class:
CC phase:
DL SE:

A
  • CD3 and CD20
  • BiTE
  • none
  • same as other BiTES
89
Q

Teclistamab
Target:
Class:
CC phase:
DL SE:

A
  • CD3 on T-cells and B-cell maturation antigen, BCMA of multiple myeloma cells
  • BiTE
  • none
  • same as other BiTE
90
Q

Taquetamab
Target:
Class:
CC phase:
DL SE:

A
  • CD3, GPRC5D
  • BiTE
  • none
  • other BiTEs
91
Q

Sipuleucel-T
Target:
Class:
CC phase:
DL SE:

A
  • antigen presenting cells activated by ex vivo with PAP-GM-CSF
  • PAP-GM-CSF
  • none
  • flu like sxs, increased risk of stroke
92
Q

CAR-T
Target:
Class:
CC phase:
DL SE:

A
  • T cell activation using CD19 as target
  • chimeric antigen receptor T cells (CAR-T) duh
  • none
  • none listed
93
Q

Olaparib:
Target:
Class:
CC phase:
DL SE:

A
  • PARP to trap to DNA
  • PARP inhibitor
  • none
  • no crazy ones listed
94
Q

think of what fun 2 word thing when you see olaparib

A

synthetic lethality

95
Q

Palbociclib
Target:
Class:
CC phase:
DL SE:

A
  • CDK4/6
  • Kinase inhibitor -> targets kinases directly involved in cell cycle control
  • G1
  • neutropenia, nausea, fatigue, diarrhea, vomiting
96
Q

Palbociclib genetic testing

97
Q

Bortemzomib
Target:
Class:
CC phase:
DL SE:

A
  • 26S proteasome
  • proteasome inhibitor
  • none
  • none listed that are special
98
Q

5-azacytidine
Target:
Class:
CC phase:
DL SE:

A
  • RNA
  • DNMT inhibitor
  • none
  • none listed
99
Q

Venetoclax:
Target:
Class:
CC phase:
DL SE:

A
  • BCL-2, anti apoptotic protein
  • BCL-2 inhibitor
  • none
  • none listed
100
Q

Venetoclax combined with what for AML

A

azacitidine

101
Q

Pomalidomide
Target:
Class:
CC phase:
DL SE:

A
  • IKZF TFs
  • Thalidomide analog
  • none
  • none listed

PHRM 864 (29 decks)

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