Monoclonal Antibodies Flashcards

(119 cards)

1
Q

Muromonab-CD3 side effects

A

mild flu-like symptoms, anaphylactic reactions, CNS toxicities, side effects due to suppression of the immune system (increased risk of infection and cancer)

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2
Q

Ustekinumab (Stelara) therapeutic uses

A

Psoriasis

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3
Q

Certolizumab (Cimzia)

A

pegylated humanized Fab’ fragment of a TNF-α monoclonal antibody (NO Fc region)

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4
Q

Golimumab (Simponi) side effects

A

Serious and sometimes fatal infections

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5
Q

Brentuximab vedotin (Adcatris) therapeutic uses

A

classical Hodgkin lymphoma and systemic anaplastic large cell lymphoma

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6
Q

Trastuzumab emtansine (Kadcyla) side effects

A

nausea, fatigue, headache, constipation, musculoskeletal pain, increased liver enzymes, and thrombocytopenia

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7
Q

What test should be performed BEFORE administering Vedolizumab(Entyvio)

A

Pre-existing infection including tuberculosis

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8
Q

Abciximab (Centorex, Reopro) MOA

A

Antithrombotic—helps to prevent blood clots—the Fab fragment binds to glycoprotein receptor of human platelets and inhibits aggregation
Directed against GP IIb/IIIa receptors which are integrin family of adhesion molecules
Steric hindrance of the receptor itself as opposed to direct binding to RGD binding site of the receptor
Inhibits monocyte adhesion
Inhibits vitronectin receptors (present in serum) which mediate blood coagulation as well as endothelial and smooth muscle cell proliferation

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9
Q

Ipilimumab (Yervoy)

A

Human antibody

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10
Q

Muromonab-CD3 therapeutic uses

A

Prevent acute rejection

Used to deplete T cells from donor bone marrow prior to bone marrow transplantation

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11
Q

Alirocumab (Praluent) side effects

A

injection site bruising, flu like symptoms, nose and throat irritation, GI symptoms, muscle pain, and urinary tract infection

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12
Q

Brentuximab vedotin (Adcatris) side effects

A

Chemotherapy-induced peripheral neuropathy is one of the adverse effects of the drug.

Other side effects include, nausea, vomiting, diarrhea, cough, anemia, fatigue, upper respiratory tract infection, fever, rash, thrombocytopenia, and neutropenia.

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13
Q

Ustekinumab (Stelara)

A

Human IgG1alpha monoclonal antibody

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14
Q

Ofatumumab (Arzerra)

A

Human monoclonal antibody

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15
Q

Abciximab (Centorex, Reopro) side effects

A

nausea, vomiting, dizziness, and irritation at the injection site, occasional breathing trouble, rapid or abnormal heart beat, chest pain, swelling of feet or ankles

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16
Q

Nivolumab (Opdivo)

A

Human monoclonal antibody (IgG4)

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17
Q

Ibritumomab (Zevalin)

A

Murine monoclonal antibody

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18
Q

Abciximab (Centorex, Reopro) therapeutic uses

A

emergency care in patients with heart disease caused by poor blood flow in the arteries of heart (Ischaemic cardiac complications)

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19
Q

Reslizumab (Cinqair) administration

A

Once every 4 weeks (IV infusion can take up tp 50mins)

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20
Q

Natalizumab (Tysabri) MOA

A

specific for α-4 integrin

interferes with the cellular traffic through the cellular lining of blood-brain barrier and intestines, and as a consequences produces its anti-inflammatory effects

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21
Q

Daclizumab (Zinbryta) therapeutic uses

A

Kidney transplantation

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22
Q

Panitumumab (Vectibix) MOA

A

binds to epidermal growth factor receptors (EGFR aka:HER-1) resulting in the inhibition of signal transduction pathways

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23
Q

Muromonab-CD3 MOA

A

Binds to the CD3, antigen is blocked and cannot bind to the antigen-recognition complex
Antibody binds to T lymphocytes—total circulating T cells are depleted from the blood and when the T cells reappear, the CD3 and antigen recognition complex are absent

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24
Q

Ibritumomab (Zevalin) therapeutic uses and how is it administered

A

treatment of relapsed or refractory low grade, follicular, or transformed B cell non-Hodgkin’s lymphoma and in patients with rituximab refractory follicular non-Hodgkin’s lymphoma

Administered in two steps:

  1. patient initially receives a single infusion of rituximab which is administered to get rid of the majority of B cells (CD20 receptors) and to limit toxicity from radiation
  2. The immunoconjugate linked to Indium 111 is then transfused
  3. 7-9 days after the infusion a second infusion of rituximab is given followed by the administration of the immunoconjugate linked to Yttrium 90
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25
Tocilizumab(Actemra) MOA
Inhibit IL-6 *receptors* | —binds to soluble as well as membrane bound interleukin-6 receptors
26
Nivolumab (Opdivo) therapeutic uses
unseceptible or metastatic melanoma, which no longer responds to other treatments advanced squamous cell carcinoma of head and neck and squamous non-small cell lung cancer (not a cure—just prolongs life) Late stage liver, renal, bladder and colorectal cancer it is used to prolong life The inhibition of PD-1 system produces natural anti-cancer response
27
Benefits of antibodies that target CD20 receptors
Mature B cells go through some final changes to become plasma cells which are the cells that secrete antibodies—Stem cells and Plasma cells do NOT express CD20 When you use a drug that targets CD20 it has a lot of benefits because you are not destroying stem cells and therefore do not require bone marrow transplant and you are not destroying plasma cells so the body will continue to make some antibodies and the patient will not be completely Immunocompromised
28
Belimumab (Benlysta) therapeutic uses
Systemic lupus erythematosus
29
Palvizumab (Synagis) therapeutic uses
Directed against RSV | prevention of serious lower respiratory infection caused by respiratory syncytial virus (RSV)
30
Rituximab (Rituxan) MOA
IgG1 specific antibody for CD20 receptor contains human constant region and murine heavy and light chains variable regions Fab domain of the antibody binds to CD20 marker on B cells Fc domain recruits immune effector cells and mediators for B cell lysis—lysis can be achieved by antibody-dependent cell mediated cytotoxicity and apoptosis
31
Infliximab (Remicade)
Chimeric antibody
32
Centuximab (Erbitux) therapeutic uses
treatment of head, neck and colorectal cancers and in combination with radiation therapy it is indicated for the treatment of squamous cell carcinoma (locally or regionally advanced). However, it is not given in combination with radiation to patients who did not exhibit a good response to platinum-based therapy (cannot give with KRAS then this will not work) For metastatic colorectal carcinoma expressing EGFR it is administered in combination with irinotecan, provided that the patients are refractory to irinotecan-based chemotherapy
33
Ixekizumab (Taltz)
Humanized monoclonal antibody
34
Tocilizumab(Actemra) side effects
upper respiratory infection, common cold, HA, and high BP
35
Brentuximab vedotin (Adcatris) MOA
After binding to the cell surface of the target cell, it is internalized by endocytosis and selectively targets the tumor cells
36
Bevacizumab (Avastin) side effects
*GI perforation*, *hemorrhage*, hypertension*, *complications with wound healing*, nephritic syndrome, congestive heart failure and thromboembolic events
37
Daclizumab (Zinbryta) MOA
binds to alpha subunit of IL-2 *receptors*—prevents the binding of IL-2 to its receptors **Since alpha chain is not expressed on resting T cells, entire immune response may not be suppressed**
38
Trastuzumab emtansine (Kadcyla) MOA
Mertansine enters tumor cells, binds to tubulin and kills them and as a result, it kills the cell
39
Trastuzumab emtansine (Kadcyla)
Conjugated antibody made up of Trastuzumab linked to cytotoxic agent Mertansine
40
Certolizumab (Cimzia) MOA
neutralizes membrane-bound and soluble human TNFα in a dose-dependent manner. Most potent antibody against TNF alpha b/c it is only a fragment and can reach the tissue It has a high affinity for TNF-α but does NOT induce antibody-dependent cellular cytotoxicity, complement activation, or apoptosis in T cells or macrophages.
41
Ixekizumab (Taltz) therapeutic uses
Moderate to severe psoriasis in adults
42
Trastuzumab (Herceptin)
Humanized monoclonal antibody (CDR grafted IgG1)
43
Infliximab (Remicade) MOA
Inhibits TNF alpha Neutralizes the effects of TNF alpha which includes its effects on IL-1 and IL-6 Reduces infiltration of inflammatory cells into the inflamed areas of joints Suppresses the expression of adhesion molecules. Decreases IL-6 levels. Inhibits acute phase response.
44
Centuximab (Erbitux) MOA
specific for epidermal growth factor receptors (HER1) which are expressed on epithelial tissue as well as on the tumors of the colon, rectum, head and neck Causes inhibition of EGF-mediated signal transduction events including the phosphorylation and activation of various kinases associate with EGFR The inhibition of binding of EGF to its receptors suppresses cell growth and decreases in the production of matrix metalloproteinase and vascular endothelial growth factor (VEGF)
45
Tocilizumab(Actemra)
Humanized antibody
46
umab
Human antibody
47
Panitumumab (Vectibix) therapeutic uses
colorectal cancer in patients who have not responded well to standard chemotherapy Mutations called KRAS and NRAS and BRAF —If there is a mutation in KRAS or NRAS then this antibody will not work (must test the mutations before giving the drug)
48
Reslizumab (Cinqair)
Humanized monoclonal antibody
49
Ibritumomab (Zevalin) side effects
anemia, thrombocytopenia, neutropenia, *increased risk of infection* (monitor for infection for at least one year), allergic reactions including the bronchospasm and angioedema and GI discomfort There is also some risk of secondary malignancy
50
Brentuximab vedotin (Adcatris)
composed of a chimeric monoclonal antibody brentuximab, which is specific for CD30 molecules and is attached to an antimitotic agent monomethyl auristatin E
51
Trastuzumab (Herceptin) administered with what other drugs
lapatinib or paclitaxel
52
Ipilimumab (Yervoy) MOA
binds to CTLA-4 (cytotoxic T lymphocyte-associated antigen 4) which is expressed on the surface of helper T cells and transmits inhibitory signals to T cells. It is also found on regulatory T cells CTLA-4 binds to CD80 and CD86 (B7) on antigen presenting cells CTLA-4 regulates T cell responses in fighting disease The antibody blocks the function of CTLA-4, resulting in a sustained immune response that attacks the cancer cells (Immune response will continue without stoping)
53
Muromonab-CD3
100% mouse antibody
54
Nivolumab (Opdivo) side effects
fatigue, shortness of breath, lack of appetite, GI symptoms, and musculoskeletal pain
55
Natalizumab (Tysabri)
Humanized monoclonal antibody
56
Bevacizumab (Avastin) MOA
directed against vascular endothelial growth factor (VEGF) receptors present on endothelial cells VEFG promotes the proliferation of endothelial cells and formation of new blood vessels—inhibit formation of new blood vessels which will inhibit angiogenesis and the tumor dies
57
Panitumumab (Vectibix)
Fully human monoclonal antibody (IgG2)
58
Daclizumab (Zinbryta)
Humanized antibody
59
omab
100% murine antibody
60
Trastuzumab emtansine (Kadcyla) therapeutic uses
Specific for patients who are afflicted with HER2-positive metastatic breast cancer, and have been previously treated with Herceptin (NOT first line therapy) patients who have already been treated for metastatic breast cancer or have re-developed tumor within six months of therapy
61
Basiliximab (Simulect)
Chimeric monoclonal antibody
62
Natalizumab (Tysabri) side effects
progressive multifocal leukoencephalopathy (PML), which is an opportunistic infection caused by John Cunningham (JC) virus
63
Tocilizumab(Actemra) therapeutic uses
administered subcutaneously for moderate to severe rheumatoid arthritis and systemic juvenile idiopathic arthritis. could be administered with or without methotrexate
64
Ofatumumab (Arzerra) side effects
flu-like symptoms, upper respiratory infection, lower respiratory infection, rash, neutropenia and anemia
65
Centuximab (Erbitux)
Chimeric monoclonal antibody (IgG1)
66
Ixekizumab (Taltz) MOA
Inhibits IL-17A and IL-17A/F | IL-17 stimulates proliferation and activation of keratinocytes
67
Ofatumumab (Arzerra) therapeutic uses
chronic lymphocytic leukemia which is refractory to fludarabine and Alemtuzumab
68
Rituximab (Rituxan)
Chimeric monoclonal antibody
69
Golimumab (Simponi) MOA
Inhibits tumor necrosis factor α, and used as an immunosuppressive drug
70
Ixekizumab (Taltz) CI with what infection
Tuberculosis
71
Bevacizumab (Avastin)
Humanized monoclonal antibody (IgG1)
72
Trastuzumab (Herceptin) therapeutic uses
aggressive metastatic breasts cancer who over express HER-2
73
Reslizumab (Cinqair) side effects
anaphylactic reaction, chest tightness, wheezing, light- headedness, itches, and rash
74
Trastuzumab (Herceptin) side effects
development of ventricular dysfunction and congestive heart failure—left ventricular function must be evaluated in all patients before and during trastuzumab therapy Patients treated with trastuzumab exhibit symptoms of cardiac dysfunction, dyspnea, peripheral edema and reduced ejection fraction. In combination with anthracyclin and cyclophosphamide it exhibits severe cardiomyopathy. It may cause allergic reactions, anaphylaxis and pulmonary events. Chills and fever have also been reported after first infusion.
75
Golimumab (Simponi) therapeutic uses
administered once a month subcutaneously for the treatment of moderate to severe rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, and ulcerative colitis(in adults)
76
Vedolizumab(Entyvio) administration
Zero, two, and six weeks and then every 8 weeks
77
Alemtuzumab (Lematrada) MOA
binds CD52 receptor which is present on the surface of normal and malignant T cells—It mediates its effects via antibody-dependent lysis of target cells (T cells) after binding to CD52 receptors (also neutralizes T cells) CD52 is not present on erythrocytes (RBC)
78
Golimumab (Simponi)
Human monoclonal antibody
79
Ibritumomab (Zevalin) MOA
IgG1 conjugated to a linker—one of the two radiation sources Indium-111 or Yttrium-90 The antibody is directed against CD20 receptor which is not shed from the cell surface and is not internalized after binding to the antibody The antibody is supplied in two vials one containing antibody conjugated to Indium-111 and the other to Yttrium-90. After binding to cells expressing CD20 receptors the antibody delivers radiation which enhances its killing effect and induces apoptosis and the radiation causes further damage to the cells by the formation of the free radicals The B cells recover in about 9 months since CD20 receptor is not expressed on B cell precursors
80
Alemtuzumab (Lematrada)
Humanized antibody (CDR grafted IgG1)
81
Vedolizumab(Entyvio) therapeutic uses
ulcerative colitis and inflammatory disease | Used in patients who do not respond well to anti-TNFα therapies
82
Certolizumab (Cimzia) therapeutic uses
RA and Chron’s
83
Vedolizumab(Entyvio) MOA
Inhibits integrin α4β7 (LPAM-1, lymphocyte Peyer’s patch adhesion molecule 1) Inhibiting the function of integrin α4β7 activity causes anti-inflammatory effect
84
Natalizumab (Tysabri) therapeutic uses
Multiple sclerosis and Chron’s lesions in multiple sclerosis are caused by T lymphocytes passing through the blood-brain barrier through their interaction with the adhesion molecules on endothelial cells (high endothelial venules) By inhibiting the adhesion molecules, we block the migration of cytotoxic and inflammatory cells into the brain or the bowel/GI tract
85
Certolizumab (Cimzia) side effects
decrease body’s ability to fight infection and increase the risk of serious or life-threatening infections, including severe bacterial, fungal, and/or viral infections. GI discomfort, intestinal obstruction, diarrhea, upper respiratory infection, urinary tract infection, and arthralgia
86
Adalimumab (Humira) MOA
binds to TNF alpha and blocks its interaction with p55 and p75 cell surface TNF alpha receptors Modulates biological responses that are induced or regulated by TNF alpha including the changes in the levels of the adhesion molecules Rapidly decreases acute phase proteins, serum cytokines, and metalloproteinase
87
Adalimumab (Humira) cannot be given with what other drugs
TNF alpha inhibitors
88
ximab
Chimeric antibody
89
Infliximab (Remicade) therapeutic uses
treat rheumatoid arthritis and Crohn’s Disease and it may alter other immune cells
90
Belimumab (Benlysta) MOA
inhibits B cell activating factor. B-cell (BAFF) also referred to as B-lymphocyte stimulator, is responsible for the development and survival of B cells (inhibit production of antibodies)
91
Ofatumumab (Arzerra) MOA
specific for CD20 protein—its epitope is distinct from rituximab Inhibits early stage B cell activation and cytotoxic to cells expressing CD20 (ADCC)
92
Basiliximab (Simulect) MOA
binds to IL-2 *receptor* alpha chain (CD-25 antigen) on the surface of activated T lymphocytes (IL-2 receptor *alpha chain* are the high affinity receptors) inhibits IL-2 mediated activation of T cells While in circulation it impairs the response of the immune system to the antigenic challenge
93
Adalimumab (Humaria) therapeutic use
Treat RA and Chron’s disease
94
Palvizumab (Synagis)
CDR grafted antibody
95
Rituximab (Rituxan) side effects
Most side effects are felt after the first treatment—immediate side effects include fever, chills and respiratory symptoms; other infusion reactions include nausea, angioedema, headache, hypertension, puritus, uticaria, rash and vomiting
96
Ustekinumab (Stelara) MOA
Inhibits p40 subunit of the IL-12 and IL-23 cytokines. IL-12 is also known as natural killer stimulatory factor or cytotoxic lymphocyte maturation factor. This cytokine is made up of a 40 kDA and a 35 kDA subunit—IL-12 p40 subunit is shared by IL-23. • IL-23 plays an important role in inflammatory response • In conjunction with other cytokines (IL-6, TGFβ) IL-23 stimulates naïve CD4+ T cells to differentiate into TH17 cells and TH22 cells, which are distinct from TH1 and TH2 cells. TH17 cells promote the production of IL-17 which is a pro-inflammatory cytokine that enhances T cell priming and enhance the production of IL-1, IL-6, TNFα, and chemokines
97
Ixekizumab (Taltz) side effects
flu like symptoms, infection, pain at the site of injection, nausea, and oropharyngeal pain
98
Alirocumab (Praluent)
Human monoclonal antibody
99
Centuximab (Erbitux) side effects
immunogenecity, electrolyte depletion and infusion reactions
100
Nivolumab (Opdivo) MOA
It blocks immune checkpoint (immunologic brake) PD-1 (Programed death-1) (PD-1 receptor is present on T cells and B cells) It blocks the activation of PD-1 receptors through their ligand, PD-L1–Binding of PD-L1 to PD-1 receptors causes the inhibition of T cells PD-1, then allows the immune response to be produced in the closed vicinity of the tumor Immune checkpoint—functions as a negative feedback for immune response (downregulate immune response) Inhibit T cell function in secondary lymphoid organs and enhance the function of regulatory T cells Antibody itself is not treating the disease—it is inhibiting the immune checkpoint to allow the immune response to continue without any inhibition
101
Belimumab (Benlysta) side effects
nausea, diarrhea, fever, hypersensitivity, and infusion-site reactions, increased risk of infection
102
Belimumab (Benlysta)
Human monoclonal antibody
103
MOA of Alirocumab (Praluent)
Inhibits PCSK9 which will inhibit degradation of LDL receptors and increase removal of LDL cholesterol from circulation
104
Vedolizumab(Entyvio)
Humanized antibody
105
Infliximab (Remicade) side effects
Infection, cough, back pain, nausea, vomiting
106
Reslizumab (Cinqair) therapeutic uses
Severe asthma and the eosinophilic phenotype (latest onset and very severe) NOT used for an acute asthma attack
107
Adalimumab (Humira) side effects
Infections, neurologic events and malignancies
108
Ipilimumab (Yervoy) therapeutic uses
Malignant melanoma
109
Adalimumab (Humira)
Human antibody
110
Alirocumab (Praluent) therapeutic uses
second line treatment to reduce LDL cholesterol levels and used in patients who do not respond well to diet, exercise, statins or are intolerant to statins
111
zumab
Humanized (human like) or CDR grafted antibody
112
Abciximab (Centorex, Reopro)
Chimeric monoclonal antibody
113
Vedolizumab(Entyvio) side effects
Flu like symptoms, GI problems, liver dysfunction, pain and swelling
114
Reslizumab (Cinqair) MOA
Inhibits IL-5 | IL-5 is responsible for the proliferation, maturation, differentiation, and effector function of eosinophils)
115
Golimumab (Simponi) CI with what other drugs
abatacept kineret other TNFα blockers
116
Trastuzumab (Herceptin) MOA
Binds to human epidermal growth factor type 2 receptor protein (HER-2). HER are transmembrane tyrosine kinase receptors involved in cell growth, differentiation and proliferation of epithelial cells and cytoblasts mutation in the HER-2 receptor causes an increased amount of the growth factor receptor protein on the tumor cell surface which increases proliferation of the cells inhibits the proliferation of tumor cells over expressing HER-2–causes HER-2 receptor down regulation by binding to the receptor and causing endocytosis of some receptors as well as limiting the signal for cell growth. Fc region causes lysis via antibody-dependent cell-mediated cytotoxicity
117
Bevacizumab (Avastin) therapeutic uses
In combination with a standard chemotherapeutic regimen (5-fuouracil-based) it is used for the treatment of patients with malignant *colon or rectal cancer* Some forms of renal, ovarian, lung, and brain cancers
118
Rituximab (Rituxan) therapeutic uses
Non-Hodgkin’s lymphoma. Fifty percent of the patients have responded to the treatment with full or partial remission
119
Alemtuzumab (Lematrada) therapeutic uses
multiple sclerosis and tissue transplantation