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Cology 2 Exam 4 > Antimitotic and Biological response modifiers - Slides 24-43 > Flashcards

Antimitotic and Biological response modifiers - Slides 24-43 Flashcards

1
Q

Our genome codes for how many protein kinases and how many protein phosphatases?

A

550 protein kinases

130 protein phosphatases

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2
Q

What are the two types of protein kinases?

A 
Receptor tyrosine kinases (humans - 90)
Insulin receptor
Epidermal growth factor
Platelet derived growth factor
Fibroblast growth factor
Vascular endothelial growth factor

Enzymatic tyrosine kinases (humans - 32)
MAP
RAS
MEEK

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3
Q

What are Imatinib, Dasatinib, Nilotinib?

A

Myeloid tyrosine kinase inhibitors

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4
Q

What is Imatinib used for?

A

CML (BCR-ABL mutation)

CMML (EVT6-PDGFR mutation)

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5
Q

How does Imatinib work?

A

Decreases myeloid TK’s responsible for cell proliferation

Binds closed BCR-ABL kinase

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6
Q

How is Imatinib administered?

A

Oral

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7
Q

Toxicities with Imatinib?

A

Nausea, vomiting, edema

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8
Q

How does Dasatinib work?

A

2nd generation

Binds both open and kinase

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9
Q

How does Nilotinib compare to Imatinib?

A

More potent

Works in Imatinib resistance!

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10
Q

What are Gefitinib, Erlotinib?

A

Epidermal growth factor Tyrosine Kinase inhibitors (ErbB1 or HER1)

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11
Q

How is Gefitinib administered?

A

Oral

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12
Q

How does Gefinitib work?

A

It blocks ATP binding/activation of the TK

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13
Q

What is Gefitinib used for?

A

Non-small cell lung cancer

EGRF mutants

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14
Q

Toxicities with Gefitinib?

A 
Diarrhea
Rash (50%)
Nausea
Vomiting
Dry skin
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15
Q

What is Erlotinib used for?

A

2nd line metastatic non-small cell lung cancer

Pancreatic and head and neck cancer

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16
Q

Toxicities with Erlotinib?

A

Diarrhea
Rash
Elevated liver enzymes

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17
Q

What is Lapatinib?

A

ErbB1 (HER1), ErbB2 (HER2) tyrosine kinase inhibitor

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18
Q

How does Lapatinib work?

A

It’s taken orally, has an intracellular site of action

Increases time of tumor growth from 4.4 to 8 months when given with Capecitabine

Enters CNS and is effective in CNS metabolism

Metabolized by CYP3A4

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19
Q

Indications for Lapatinib?

A

CNS metastasis

Metastatic breast cancer no longer sensitive to Trastuzumab

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20
Q

Toxicities of Lapatinib?

A

Rash
Nausea
Fatigue
Anorexia

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21
Q

What is Bortezomib?

A

Proteosome inhibitor

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22
Q

MOA of Bortezomib?

A

Inhibits proteosome breakdown of IKB which stays bound to NF-KB to prevent moving into the nucleus
NF-KB is a potent cell survivor promoter gene

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23
Q

Indications for Bortezomib?

A

Approved for multiple myeloma

In trials for other solid tumors

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24
Q

Toxicities of Bortezomib?

A 
Thrombocytopenia (28%)
Fatigue
Neuropathy
Limb pain
Hypotension
CV failure
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25
Q

What is Cetuximab?

A

Antibody to epidermal growth factor receptor (HER1, ErbB1)

26
Q

How is Cetuximab administered?

27
Q

Indications for Cetuximab?

A

EGRF positive metastatic colorectal cancer (40-50% express the mutant receptor and are resistant)

2nd line in head and neck with cisplatin

Being tested in breast, prostate, brain, pancreas, and bladder also expressing HER1

28
Q

Toxicity of Cetuximab?

A

Infusion reaction
Skin rash (75%)
Cardiac arrest

29
Q

What is Panitumab?

A

Recombinant human antibody to extracellular domain of EGRF

30
Q

How is Panitumab administered?

31
Q

Indications for Panitumab?

A

Metastatic colorectal cancer overexpressing EGRF (after 2 previous therapies!!!)

Toxicities: Epidermal toxicity (89%), severe infusion reactions, pulmonary fibrosis, electrolyte abnormalities

32
Q

What is Trastuzumab?

A

Recombinant human monoclonal antibody to external domain of human epidermal growth factor 2 (HER2/neu, ErbB2)

33
Q

MOA for Trastuzumab?

A

Antibody prevents the binding of the growth factor, can also down regulate the growth factor receptor

34
Q

Indications for Trastuzumab?

A

Approved for use in metastatic breast tumors over expressing HER2 (ErbB2) oncogene
(30% of breast tumors overexpress)

35
Q

What is BRCA1/BRCA2?

A

Tumor suppressor genes that activate DNA strand break reair mechanisms

BRCA mutations are found in 20-25% of hereditary breast cancer and 10-15% of ovarian cancer

36
Q

How is Trastuzumab administered?

A

Weekly infusion, given with Doxorubicin and Taxol

37
Q

Toxicities with Trastuzumab?

A

Fever, chills occur in the first dose in 40% of patients (treat with APAP, diphenhydramine)

Nausea, vomiting, headache, dizziness, dyspnea, cough, cardiomyopathy

38
Q

What is Bevacizumab?

A

Antibody to vascular-endothelial growth factor (VEGF) - prevents angiogenesis

39
Q

How is Bevacizumab administered?

A

IV infusion or direct injection to the eye (for wet-age related macular degeneration)

40
Q

Indications for Bevacizumab?

A

In combination for metastatic colorectal, breast***, lung, glioblastoma, renal, pancreatic cancers

Macular degeneration too

***FDA removed breast cancer as indication bc there was no survival benefit

41
Q

Toxicities for Bevacizumab?

A 
Severe hypertension
Proteinuria
CHF
Perforations of stomach and GI tract
Bleeding into lungs
Expensive ($8000/month)
42
Q

What are Sunitinib, Sorafenib?

A

Oral VEGF-1,2,3 inhibitors

43
Q

Indications for Sunitinib?

A

Metastatic renal cell cancer, better response than Bevacizumab

44
Q

Indications for Sorafenib?

A

Only drug approved for Hepatocellular cancer

Metastatic renal cancer

45
Q

Toxicities for Sunitinib?

A

Hypothyroidism (40-60%)

Fatigue (50-70%)

46
Q

Toxicities for Sorafenib?

A

Nausea, vomiting, diarrhea, rash

47
Q

What is Rituximab?

A

Chimeric human-murine antibody to CD20 antigen on B-lymphocytes

48
Q

What is Rituximab used for?

A

Non-hodgkin’s lymphoma (90% have the CD20 gene)

CLL

49
Q

What is CD20?

A

It regulates step in cell cycle activation

Blocking CD20 can cause complement mediated lysis, apoptosis, antibody mediated cytotoxicity

50
Q

How is Rituximab administered?

A

Given as 4 weekly infusions

51
Q

Toxicities of Rituximab?

A 
Infusion related flu-like syndrome
N/V
Urticaria
SJS
Bronchospasm
Mild myelosuppression
52
Q

What is Ofatumumab?

A

CD20 monoclonal antibody

53
Q

Indications for Ofatumumab?

A

Used for CLL after failure of Alemetuzumab and Fludarabine

54
Q

Toxicities for Ofatumumab?

A

Immunosuppression
Opportunistic infections
Hypersensitivity reactions

55
Q

What is Alemtuzumab?

A

Binds CD52 antigen on T and B lymphomas

Induces cellular cytotoxicity

56
Q

Indications for Alemtuzumab?

A

B and T cell lymphomas

CLL

57
Q

How is Alemtuzumab administered?

58
Q

Toxicities for Alemtuzumab?

A

Infusion reaction
Decreased T-cells
Opportunistic infections

59
Q

What is Gemtuzumab ozogamacin?

A

Antibody to CD33 antigen linked to Ozagimicin (antitumor antibiotic)

60
Q

Indications for Gemtuzumab ozogamicin?

A

CD33 positive acute myelogenous leukemia (80%) in first relapse

61
Q

Toxicities for Gemtuzumab ozogamicin?

A

Infusion reactions

Hepatic and bone marrow suppression

Cology 2 Exam 4 (16 decks)

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