Targeted Cancer Drugs Flashcards

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
Q

What are the toxicities associated with panitumumab?

A

infusion reaction

Skin rash with sun

26
Q

What is the MOA of bevacizumab?

A

Anti-angiogenesis, neovascularization

27
Q

What are the toxicities associated with bevacizumab?

A

HTN
CHF
Pulmonary Hemorrhage
GI perforation

28
Q

What is the MOA of rituximab?

A

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
Q

What are the toxicities associated with rituximab?

A

Infusion reaction
+ve B-cell depletion (lasts several months)
Lymphopenia

30
Q

What is the MOA of ofatumumab?

A

Apoptosis, ADCC, CDC

31
Q

What are the toxicities associated with ofatumumab?

A

Infusion reaction
Infections
Progressive leukoencephalopathy
Neutropenia

32
Q

What is the MOA of ipilmumab?

A
  • 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
Q

What is notable about ipilmumab?

A

ONLY immunostimulant

34
Q

What 2 TKIs (tyrosine kinase inhibitors) are associated with CV dysfunction?

A

Lapatinib

Nilotinib

35
Q

List the mTOR inhibitors?

A

sirolimus
everolimus
temsirolimus

36
Q

What mTOR inhibitors are used to treat advanced renal cell cancer?

A

temsirolimus and everolimus

37
Q

Name the protein that, when affected by the ubiquitin proteosome pathway, leads to the inhibition of NF-kappaB, apoptosis, growth inhibition, and reduced angiogenesis.

A

IkappaB

38
Q

Name the protein that, when affected by the ubiquitin proteosome pathway, leads to G1-S cell cycle arrest and apoptosis.

A

cyclin dependent kinases

39
Q

Name the protein that, when elevated by the ubiquitin proteosome pathway, leads to apoptosis via p21 upregulation and BAX overexpression.

A

P53

40
Q

Name the protein that, when elevated by the ubiquitin proteosome pathway, overcomes Bcl-2 overexpression.

A

Bax

41
Q

Name the protein that, when affected by the ubiquitin proteosome pathway, leads to disordered signaling that leads to apoptosis?

A

cyclins

42
Q

Name the proteins that, when accumulated by the ubiquitin proteosome pathway, leads to apoptosis?

A

damaged cellular proteins

43
Q

What are the toxicities associated with Bortezomib?

A
Hypotension
Cardiotoxicity
Severe sensory and motor peripheral neuropathy**
Hematologic and hepato-toxicity
Pregnancy risk category D
44
Q

What mutation is found in TKIs that prevents appropriate binding of first-generation drugs? Where is this mutation?

A

T3151

mutation is in the ATP binding domain

45
Q

What are the common adverse effects associated with TKIs?

A

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
Q

Which TKI’s produce peripheral neuropathy?

A

Sunitinib
Sorafenib
Pazopanib
Vemurafenib

47
Q

What TKI targets ALK and HGFR?

A

Crizotinib

48
Q

What TKI targets SCR, Bcr-abl, c-KIT, and PDGFR?

A

Dasatinib

49
Q

What 2 TKIs specifically target EGFR only?

A

Erlotinib

Gefitinib

50
Q

What 2 TKIs target Bcr-abl, c-KIT, and PDGFR?

A

Imatinib

Nilotinib

51
Q

What TKI targets EGFR AND HER2?

A

Lapatinib

52
Q

What 2 TKIs targets VEGFR, c-KIT, and PDGFR?

A

Pazopanib

Sunitinib

53
Q

What TKI targets BRAF, VEGFR, and PDGFR?

A

Sorafenib

54
Q

What TKI targets BRAF only?

A

Vemurafenib

55
Q

What TKI drugs target EGFR?

A

Erlotinib
Gefitinib
Lapatinib

56
Q

What TKI drugs target PDGFR?

A
Imatinib
Nilotinib
Pazopanib
Sunitinib
Sorafenib
Dasatinib