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Pathway Targeted Therapies Flashcards

1
Q

EGFR Tyrosine Kinase Inhibitors (TKIs)

A

Erlotinib, Gefitinib, Afatinib, Osimertinib

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2
Q

Antibody inhibitors of EGFRs

A

Cetuximab, Panitumumab, Necitumumab

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3
Q

Antibody inhibitors of HER2/Neu

A

Trastuzumab and Pertuzumab

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4
Q

HER2/Neu TKIs

A

Lapatinib and Neratinib

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5
Q

Inhibitors of mutated RAF kinase

A

Vemurafenib and Dabrafenib

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6
Q

Inhibitors of MEK

A

Trametinib and Cobimetinib

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7
Q

Cyclin Dependent Kinase (CDK 4/6 inhibitors)

A

Palbociclib, Abemaciclib, and Ribociclib

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8
Q

Inhibitors of Histone Deacetylase?

A

Panobinostat and Romidepsin

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9
Q

Anti-CTLA4

A

Ipilimumab

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10
Q

Anti-PD1

A

Nivolumab and Pembrolizumab

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11
Q

AntiPDL1

A

Atezolimumab

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12
Q

Inhibitors of BCR-ABL Kinase

A

EGFR TKIs (Imatinib, Dasatinib, Nilotinib)

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13
Q

Drugs targeting Angiogenesis

A

Bevacizumab, Afilbercept, Ramucirumab, TKIs (pazopanib, sorafenib, sunitinib)

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14
Q

What is targeted cancer therapies?

A

drugs that block the growth and spread of cancer by interfering with specific molecules that drive malignant progression of human cancers

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15
Q

Targeted cancer therapy vs. standard chemo

A

acts on specific molecular targets
deliberately chosen to interact with target
cytostatic (block tumor cell proliferation)
Antibody drugs–combine biologic and cytotoxic mechanisms

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16
Q

Targeted Cancer Therapies

A

Growth factors and receptors in cancer
Intracellular Kinases
Tumor host interactions aberrant tumor angiogenesis
restoring immune recognition
targets that control cancer cell behavior

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17
Q

EGFR binding MOA

A

Phosphorylation of downstream adapter proteins (MAPK, PI3K/Akt, and STAT)—>stimulates signaling pathways–>cell growth and proliferation

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18
Q

Epithelial cancers?

A

overexpression of EGFR and mutational activation of EGFR—>dependence of EGFR signaling

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19
Q

Drugs that target the EGFR Pathway?

A

TKIs or monoclonal antibodies

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20
Q

Erlotinib MOA?

A

reversible inhibitor of EGFR TK–>competively inhibits ATP binding as the active site of the kinase

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21
Q

Erlotinib and PPIs?

A

PPIs decrease Elotinib bioavailabilty by 50%

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22
Q

Erlotinib and Warfarin?

A

Poor extrinsic coagulation (elevated INR)

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23
Q

Erlotinib Usage?

A

Advanced or metastatic NSCLC after failure of Platnium based treatment
Approved for patients with EGFR mutations ONLY

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24
Q

Gefitinib absorption?

A

reduced by drugs that cause elevations in gastric pH

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25
Afatinib MOA
Irreversible inhibitor of EGFR and HER2 receptor kinases
26
Afatinib is a substrate of
Pgp
27
what is first line treatment for metastatic NSCLC with EGFR mutations?
Afatinib
28
EGFR gatekeeper residue T790M
prevents binding of TKIs It is an acquired second EGFR mutation
29
Osimertinib (3rd gen) is for?
T790M mutant EGFR treatment-use if resistant to TKI
30
Osimertinib MOA?
irreversible inhibitor of T790M-mutant EGFR
31
C797S is?
A third mutation; resistance to Osimertinib
32
Cetuximab MOA?
Antibody that binds to extracellular domain III EGFR-->prevents ligand dependent signaling and receptor dimerization --blocks cell growth/survival
33
Cetuximab use?
Metastatic colon cancers (KRAS wild type) Head and neck squamous cell carcinoma
34
Cetuximab AE?
infusion reactions fetal harm
35
Cetuximab mediates?
antibody dependent cellular cytoxicity
36
Overexpression of wild-type HER2?
activates the intracellular tyrosine kinase and oncogenic signaling in the absence of activating mutations, coreceptors, or ligands
37
Overexpression of HER2 causes gene amplification of ______ and is in __________
chromosome 17 (aggressive and low response) Human breast cancer
38
Trastuzumab use?
HER2 overexpressing breast and gastric cancer combines with taxanes
39
Trastuzumab AE?
Heart Failure Cardiotoxicity by interruption of HER 2//4 heterodimer signaling
40
Trastuzumab cardiac toxicity can be reduced with _______
Taxanes
41
Trastuzumab MOA?
binds to extracellular domain IV of HER2 and inhibits hetero and homodimerization long T1/2=6 days
42
Pertuzumab MOA?
antibody against extracellular receptor dimerization domain II of HER2 T1/2=18 days
43
Pertuzumab Use?
HER2 positive metastatic and inflammatory early stage breast cancer give with trastuzumab and docetaxel
44
Pertuzumab AE?
Cardiotoxicity: pertuzumab + trastuzumab does NOT cause increase Cause fetal harm with taxanes
45
Lapatinib MOA?
inhibitor of EGFR and HER2 Tyrosine Kinases
46
Lapatinib Use?
Metastatic HER2 + and trastuzumab refractory breast cancer -give with Capecitabine postmenopausal women with hormone receptor + breast cancer =give with letrozole
47
Lapatinib AE
Cardiotoxicity less pronounced
48
Neratinib MOA?
irreversible inhibitor of HER2 and EGFR protein tyrosine kinase
49
BRAF mutation?
in melanoma and substitution of valine to glutamic acid (V600E) or to lysine (V600K)=protein kinase activation
50
BRAF Inhibitors?
Vemurafenib and Dabrafenib -for mutant BRAF melanoma
51
Activated mutant BRAF is an _____________
oncogenic driver
52
Vemurafenib MOA?
inhibitor for mutated BRAF V600E and effective against V600K mutation
53
Vemurafenib USe?
metastatic melanoma with activating BRAF mutations NOT melanoma of wildtype BRAF
54
Vemurafenib AE?
squamous cell carcinoma and keratocanthomas
55
To prevent drug resistance of Vemurafenib?
combo treat with MEK inhibitor (trametinib or Cobimetanib) that acts downstream of BRAF can delay development of resistance
56
Dabrafenib MOA?
inhibits wild-type BRAF and cRAF
57
Dabrafenib Use?
for BRAF V600 E mutation + advanced melanoma Dabrafenib +Trametinib=delays the development of resistance
58
Dabrafenib AE?
cutaneous squamous cell carcinoma Cardiomyopathy
59
Trametinib MOA?
Reversible, allosteric inhibitor of ATP binding to MEK1/2 kinases
60
Trametinib Use?
monotherapy for patients with mutant BRAF V600E/K melanoma
61
For mutant V600E/K metastatic melanoma and mutant V600 E metastatic NSCLC use?
Trametinib + Dabrafenib
62
Trametinib AE?
Does NOT cause cutaneous sarcoma carcinoma Fetal Harm
63
Activation of PI3K/Akt, mTOR, STAT3 can cause?
Trametinib drug resistance by bypassing MEK inhibition
64
Cobimetinib + Vemurafenib
for BRAF V600 E/K mutation
65
CDK 4/6 ?
enhances phosphorylation of Rb-->inactivating Rb--allowing transcription of G1 into S phase
66
Palbociclib MOA?
inhibitor of CDK4 and CDK6
67
Abemaciclib use?
HER2 negative breast cancer
68
Ribocriclib use?
HER2 negative advanced breast cancer
69
Philadelphia chromosome translocation
mutated fusion protein of BCR-ABL an active protein kinase
70
Treatment for Imatinib-resistant ABL mutations?
Dasatinib and nilotinib
71
Inhibitors of BCR-ABL Kinase?
Imatinib =1st gen Dasatinib and Nilotinib=2nd gen
72
Inhibitors of BCR-ABL kinase for? AE?
chronic phase CML Myelosuppression
73
Bevacizumab
antibody targeting VEGF
74
Afilbercept
protein binding VEGF
75
Antibody targeting VEGFR (receptor)?
ramucirumab
76
Small drug inhibitors of VEGFR?
pazopanib, sorafenib, suntinib
77
PARP Inhibitors?
multiple strand breaks in cancer cells BRCA mutations
78
PARP inhibitors?
Olaparib, Rucaparib, Niraparib, Talazoparib -Combine with radiotherapy
79
Olaparib use?
monotherapy for germline BRCA 1/2 mutated advanced ovarian cancer and HER2 negative metastatic breast cancer
80
Rucaparib use?
BRCA mutant ovarian cancer
81
Olaparib + Rucaparib
treat prostate cancer with BRCA 1/2 mutations
82
Gemtuzumab Ozogamicin MOA?
monoclonal antibody CD33, derivative of calicheamicin present on hematopoietic cells of AMLs and myeloid cells with myelodysplastic syndrome
83
Gemtuzumab Ozogamicin Use?
greater than 60 years old with AML first relapse
84
Brentuximab Vedotin Use?
For anti CD30, is a antimitotic drug For Hodgkin Lymphoma and large cell lymphoma
85
Brentuximab Vedotin works on which phase?
M Phase
86
Panobinostat
nonselective pan HDAC inhibitor for multiple myeloma

Oncology (10 decks)

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