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IHO Week 4 > Tyrosine Kinase Inhibitors > Flashcards

Tyrosine Kinase Inhibitors Flashcards

1
Q

What protein function inhibitor drugs target a unique aspect of specific cancer type?

A

L-asparaginase

Imatinib

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2
Q

What protein function inhibitors are less specific and exploit overexertion of a particular protein?

A

Erlotinib

Gefitinib

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3
Q

What protein function inhibitors are targeting rapidly dividing cells and/or angiogenesis?

A

Bortezomib
Vorinostat
Sorafenib
Sunitinib

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4
Q

What are the types of Tyrosine kinase inhibitors?

A
  • Some are Signal Transduction Inhibitors
  • Inhibitors of:
    1. Bcr-Abl
    2. EGFR
    3. HER2
    4. PDGF-R, VEGF-R (not talking about these)
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5
Q

What drugs are tyrosine kinase inhibitors of Bcr-Abl? What cancer type are they used for?

A

-Bosutinib
-Dasatinib
-Imatinib
-Nilotinib
CML (chronic myeloid leukemia)

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6
Q

What drugs are tyrosine kinase inhibitors of EGFR? What type of cancer are they used for?

A

-Cetuximab
-Erlotinib
-Gefitinib
-Panitumumab
Epithelial derived (lung, pancreas, head, neck, breast, prostate, colon, stomach, ovaries, brain)

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7
Q

What drugs are tyrosine kinase inhibitors of HER2? What cancer are these used for?

A

-Pertuzumab
-Trastuzumab [Ado-Trastuzumab, Emtansine]
Breast cancer

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8
Q

What drugs are tyrosine kinase inhibitors of PDGF-R, VEGF-R? (not talking about these) What are these used for?

A

-Pazopanib
-Sorafenib
-Sunitinib
Many different cancers - including glioblastoma, hepatocellular carcinoma, renal cell carcinoma

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9
Q

What doe the -nib ending mean?

A

Signal transduction inhibitor

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10
Q

What are some important general concepts about tyrosine kinases?

A
  • TKs are important regulators of intracellular signal transduction pathways responsible for development and multicellular communication
  • TKs phosphorylate tyrosine residues
  • > 50% of known receptor TKs have been found either mutated or overexpresssed forms that are associated with malignancies
  • Both STI and antibodies have been designed to interfere with the action of specific tyrosine kinases
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11
Q

What drugs target c-kit and fight GIST (gastrointestinal stromal tumor) cancer?

A
  • Dasatanib
  • Imatinib
  • Nilotinib
  • Sunitinib
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12
Q

What is the MOA for Cetuximab/Panitumumab?

A

Inhibitors of EGFR

  • Epithelial Growth Factor Receptor (EGFR) tyrosine kinase is overexposed in a large number of epithelial-derived cancers
  • These drugs are monoclonal antibodies directed against EGFR
  • These drugs prevent actions of EGFR, as well as identifying cells expressing the receptor as foreign (making them targets of cell mediated immunity)
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13
Q

What are the side effects of cetuximab/panitumumab?

A
  • Side effects common to Abs:
  • –Infustion/hypersensitivity reactions: fever, muscle aches, headaches, rashes, anaphylaxis, infusion reactions
  • –Mouse (MO)&raquo_space; Chimeric (XI) > Humanized (ZU) for HAMA reaction
  • –Infections
  • –Unknown effects on immunization, carcinogenesis, mutagenesis, impairment of fertility, pregnancy, nursing infants (human IgG is secreted in milk)
  • Unique toxicities affect skin (rash, photosenstivity, necrotizing fasciitis) and lung (interstitial lung disease)
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14
Q

How do HER1 inhibitors affect cancer?

A

Human Epithelial Growth Factor Receptor 2 tyrosine kinase is overexposed in a large number of aggressive breast cancers
-Mostly used for breast cancers that you can’t use doxorubicin to target!!

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15
Q

What is the mechanism of trastuzumab?

A

Binding of the antibody interferes with HER2 signaling, and identifies the HER2-overexpressing cells as foreign, so that they can be destroyed by the immune system!

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16
Q

What is the mechanism of action of Perfuzumab?

A

It’s considered the first antineoplastic DIMERIZATION INHBIITOR (new drug class) ; it prevents HER2 from dimerizing with other HER receptors (can’t function)

17
Q

What is the mechanism of action of Ado-Trastuzumab Emtansine?

A

It is internalized and undergoes lysosomal degradation to form 2 parts:

  1. Trastuzumab
  2. DM1 - a small molecule inhibitor that disrupts microtubule networks by binding tubulin
18
Q

What is the resistance mechanism developed against HER2 inhibitors?

A

Altering HER2 so that the antibody doesn’t recognize its target!!

19
Q

What are the side effects associated with Trastuzumab (HER2 tyrosine kinase inhibitor)?

A
  1. Side effects common to antibodies:
    - Infustion/hypersenstiviity reactions: fever, muscle aches, headaches, rashes, anaphylaxis, infusion reaction
    - Mouse (MO)&raquo_space; chimeric (XI) > humanized (ZU) for HAMA reaction
    - Infectioins
    - Birth defects/fetal loss
    - Unknown effects on immunization, carcinogenesis, mutagenesis, impairment of fertility, nursing infants
  2. Unique toxicities among antibodies include ventricular dysfunction and congestive heart failure

IHO Week 4 (25 decks)

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