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Flashcards in Targeted Cancer Drugs Deck (56):
1

What drug targets VEGF?

Bevacizumab

2

What drugs target EGFR?

Cetuximab and Panitumumab

3

What drugs targets CD20?

Rituximab and Ofatumumab

4

What drug targets HER-2?

Trastuzumab

5

What drug targets CTLA-4?

Ipilimumab

6

What drug targets 26-S proteosome inhibitor?

Bortezomib

7

What type of drug is Bortezomib?

small molecule inhibitor ("ib" ending)

8

What are the indications for bevacizumab?

colorectal cancer
non small cell lung cancer

9

What are the indications for cetuximab?

colorectal cancer
head and neck cancer

10

What are the indications for panitumumab?

colorectal cancer

11

What are the indications for rituximab?

chronic lymphocytic leukemia
non-Hodgkin's lymphoma

12

What are the indications for trastuzumab?

breast cancer

13

What are the indications for ipilimumab?

melanoma

14

What are the indications for ofatumumab?

chronic lymphocytic leukemia

15

What are the indications for bortezomib?

multiple myeloma

16

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

EGFR/HER1

17

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

HER2/Neu

18

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

K-Ras
(also N- and H-Ras)

19

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

B-Raf

20

What is the MOA of trastuzumab?

Apoptosis, ADCC

21

What are the toxicities associated with trastuzumab?

Cardiomyopathy
Infusion Reaction

22

What is the MOA of cetuximab?

Apoptosis, ADCC

23

What are the toxicities associated with cetuximab?

infusion reaction
Skin rash with sun

24

What is the MOA of panitumumab?

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