Targeted Cancer Drugs Flashcards

(56 cards)

1
Q

What drug targets VEGF?

A

Bevacizumab

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2
Q

What drugs target EGFR?

A

Cetuximab and Panitumumab

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3
Q

What drugs targets CD20?

A

Rituximab and Ofatumumab

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4
Q

What drug targets HER-2?

A

Trastuzumab

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5
Q

What drug targets CTLA-4?

A

Ipilimumab

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6
Q

What drug targets 26-S proteosome inhibitor?

A

Bortezomib

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7
Q

What type of drug is Bortezomib?

A

small molecule inhibitor (“ib” ending)

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8
Q

What are the indications for bevacizumab?

A

colorectal cancer

non small cell lung cancer

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9
Q

What are the indications for cetuximab?

A

colorectal cancer

head and neck cancer

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10
Q

What are the indications for panitumumab?

A

colorectal cancer

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11
Q

What are the indications for rituximab?

A

chronic lymphocytic leukemia

non-Hodgkin’s lymphoma

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12
Q

What are the indications for trastuzumab?

A

breast cancer

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13
Q

What are the indications for ipilimumab?

A

melanoma

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14
Q

What are the indications for ofatumumab?

A

chronic lymphocytic leukemia

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15
Q

What are the indications for bortezomib?

A

multiple myeloma

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16
Q

What oncogene is a growth factor receptor commonly found in glioblastoma, lung, and breast cancer?

A

EGFR/HER1

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17
Q

What oncogene is a growth factor receptor commonly found in breast, ovarian, and gastric cancer?

A

HER2/Neu

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18
Q

What oncogene functions as a G protein (signal transduciton) and is commonly found in multiple tumor types?

A

K-Ras

also N- and H-Ras

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19
Q

What oncogene functions in signal transduciton and is commonly found in multiple tumor types (and melanomas)?

A

B-Raf

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20
Q

What is the MOA of trastuzumab?

A

Apoptosis, ADCC

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21
Q

What are the toxicities associated with trastuzumab?

A

Cardiomyopathy

Infusion Reaction

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22
Q

What is the MOA of cetuximab?

A

Apoptosis, ADCC

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23
Q

What are the toxicities associated with cetuximab?

A

infusion reaction

Skin rash with sun

24
Q

What is the MOA of panitumumab?

A

Apoptosis, ADCC

25
What are the toxicities associated with panitumumab?
infusion reaction | Skin rash with sun
26
What is the MOA of bevacizumab?
Anti-angiogenesis, neovascularization
27
What are the toxicities associated with bevacizumab?
HTN CHF Pulmonary Hemorrhage GI perforation
28
What is the MOA of rituximab?
Apoptosis, ADCC, CDC, vaccination Binds to the surface of CD20 (gulates an early step(s) in the activation process for cell cycle initiation and differentiation), on the surface of B-cell precursors and mature B-lymphocytes.
29
What are the toxicities associated with rituximab?
Infusion reaction +ve B-cell depletion (lasts several months) Lymphopenia
30
What is the MOA of ofatumumab?
Apoptosis, ADCC, CDC
31
What are the toxicities associated with ofatumumab?
Infusion reaction Infections Progressive leukoencephalopathy Neutropenia
32
What is the MOA of ipilmumab?
* Binds to the CTL A4 receptor on T-cells and prevents binding of CD80/CD86 * Positively regulates T-cell activation and proliferation. * Thus, the effects of this drug are presumed to be indirect, through T-cell mediated antitumor immune response.
33
What is notable about ipilmumab?
ONLY immunostimulant
34
What 2 TKIs (tyrosine kinase inhibitors) are associated with CV dysfunction?
Lapatinib | Nilotinib
35
List the mTOR inhibitors?
sirolimus everolimus temsirolimus
36
What mTOR inhibitors are used to treat advanced renal cell cancer?
temsirolimus and everolimus
37
Name the protein that, when affected by the ubiquitin proteosome pathway, leads to the inhibition of NF-kappaB, apoptosis, growth inhibition, and reduced angiogenesis.
IkappaB
38
Name the protein that, when affected by the ubiquitin proteosome pathway, leads to G1-S cell cycle arrest and apoptosis.
cyclin dependent kinases
39
Name the protein that, when elevated by the ubiquitin proteosome pathway, leads to apoptosis via p21 upregulation and BAX overexpression.
P53
40
Name the protein that, when elevated by the ubiquitin proteosome pathway, overcomes Bcl-2 overexpression.
Bax
41
Name the protein that, when affected by the ubiquitin proteosome pathway, leads to disordered signaling that leads to apoptosis?
cyclins
42
Name the proteins that, when accumulated by the ubiquitin proteosome pathway, leads to apoptosis?
damaged cellular proteins
43
What are the toxicities associated with Bortezomib?
``` Hypotension Cardiotoxicity Severe sensory and motor peripheral neuropathy** Hematologic and hepato-toxicity Pregnancy risk category D ```
44
What mutation is found in TKIs that prevents appropriate binding of first-generation drugs? Where is this mutation?
T3151 | mutation is in the ATP binding domain
45
What are the common adverse effects associated with TKIs?
rash, fatigue, N/V, dyspnea, stomatitis, anorexia (many produce varying degrees of blood dyscrasias) (some produce QT prolongation--which if taken with a drug that also does this, may lead to arrhythmia)
46
Which TKI's produce peripheral neuropathy?
Sunitinib Sorafenib Pazopanib Vemurafenib
47
What TKI targets ALK and HGFR?
Crizotinib
48
What TKI targets SCR, Bcr-abl, c-KIT, and PDGFR?
Dasatinib
49
What 2 TKIs specifically target EGFR only?
Erlotinib | Gefitinib
50
What 2 TKIs target Bcr-abl, c-KIT, and PDGFR?
Imatinib | Nilotinib
51
What TKI targets EGFR AND HER2?
Lapatinib
52
What 2 TKIs targets VEGFR, c-KIT, and PDGFR?
Pazopanib | Sunitinib
53
What TKI targets BRAF, VEGFR, and PDGFR?
Sorafenib
54
What TKI targets BRAF only?
Vemurafenib
55
What TKI drugs target EGFR?
Erlotinib Gefitinib Lapatinib
56
What TKI drugs target PDGFR?
``` Imatinib Nilotinib Pazopanib Sunitinib Sorafenib Dasatinib ```