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What is the MOA of ipilimumab (Yervoy)?
- Blocks the cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) on T cells
- Inhibiting proliferation/differentiation of the immune cells
- T-cell mediated antitumor immune response is activated
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What are the indications for ipilimumab (Yervoy)?
Metastatic melanoma, often used with dacarbazine.
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What are the SE for ipilimumab (Yervoy)?
Immune mediated conditions (GI-enterocolitis, hepatitis, neuropathy, rash)
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What is the MOA of Brentuximab vedotin (Adcetris)?
- Monoclonal antibody that binds CD30
- Linked to a microtubule disrupting agent, monomethyl auristatin E (MMAE) and a protease linker
- The antibody binds to CD30 and internalizes
- MMAE binds to tubulin
- Causes apoptosis and cell cycle arrest
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What are the indication for brentuximab vedotin (Adcetris)?
- Hodgkin’s lymphoma
- after failure of autologous stem cell transplant (ASCT) or 2 prior multi-agent chemotherapy regimens
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What are the SE for brentuximab vedotin (Adcetris)?
peripheral neuropathy, neutropenia, infusion reactions.
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What are the Histone deactylase (HDAC) inhibitors?
vorinostat (Zolinza) and romidepsin (Istodax)
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What is the Mechanism of action of vorinostat (Zolinza) and romidepsin (Istodax)?
- Histone deacetylase (HDAC) inhibitor thereby increasing acetylation of histones and regulatory proteins in the cell nucleus that help control DNA transcription.
- Acetylation increases gene transcription leading to cell-cycle arrest and apoptosis.
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What is the indication for vorinostat (Zolinza) and romidepsin (Istodax)?
cutaneous T-cell lymphoma
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What are the SE for vorinostat (Zolinza) and romidepsin (Istodax)?
GI, anemia, thrombocytopenia, pulmonary embolism
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What are the Immunostimulants?
- Interferon alfa-2a (Roferon)
- Interferon alfa-2b (Intron)
- Aldesleukin
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What is the MOA of Interferon alfa-2a (Roferon) Interferon alfa-2b (Intron)?
- Bind to cell surface receptors causing gene expressions that result in:
- Enhancement of host immune responses
- Direct antiproliferative effects on cancer cells
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What is the brand name for Interferon alfa-2a?
Roferon
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What is the brand name for Interferon alfa-2b?
Intron
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What are the indications for vorinostat (Zolinza) and romidepsin (Istodax)?
- CML in combination with chemotherapy
- Hairy cell leukemia
- Malignant melanoma
- AIDS-related Kaposi’s sarcoma
- Non-Hodgkin’s lymphoma
- Hepatitis C and B
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What are the adverse effects of vorinostat (Zolinza) and romidepsin (Istodax)?
Flu-like symptoms
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What is EGFR (ErbB1) overexpressed?
- Non-small cell lung cancer;
- Head and neck cancer
- Colon cancer,
- Pancreatic cancer
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What drugs can used to treat EGFR (ErbB1) receptor overexpression?
- gefitinib, erlotinib
- cetuximab, panitumumab
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What is VEGFR-1,2 overexpressed?
Advanced renal cell carcinoma
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What drugs can used to treat VEGFR-1,2 receptor overexpression?
sorafenib, sunitinib
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What is VEGF ligand overexpressed?
Breast, colorectal, lung, malignant glioma, non-small cell lung cancer
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What drugs can used to treat VEGF ligand receptor overexpression?
bevacizumab
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What is HER-2/neu (ErbB2) overexpressed?
Breast cancer
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What drugs can used to treat HER-2/neu (ErbB2) receptor overexpression?
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What is PDGFR overexpressed?
Gastrointestinal stromal tumor (GIST)
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What drugs can used to treat PDGFR receptor overexpression?
Sorafenib, sunitinib
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What is FGFR3 overexpressed?
Multiple myeloma
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What drugs can used to treat FGFR3 receptor overexpression?
thalidomide, lenalidomide (inhibiting
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What is c-KIT overexpressed?
Gastrointestinal stromal tumor (GIST)
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What drugs can used to treat c-KIT receptor overexpression?
imatinib
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What is BCR-ABL overexpressed?
- Chronic myelogenous leukemia (CML)
- Acute promyelocytic leukemia (APL)
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What drugs can used to treat BCR-ABL receptor overexpression causing APL?
imatinib
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What drugs can used to treat BCR-ABL receptor overexpression causing APL?
Arsenic trioxide, tretinoin
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What is asparaginase overexpressed?
Acute lymphocytic leukemia (ALL)
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What drugs can used to treat asparaginase receptor overexpression?
asparaginase
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What is CD30 antigen overexpressed?
Hodgkin’s Lymphoma
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What drugs can used to treat CD30 receptor overexpression?
brentuximab vedotin
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What is CD20 antigen overexpressed?
B-cell non-Hodgkin’s lymphoma (NHL)
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What drugs can used to treat X receptor overexpression?
- rituximab
- ibritumomab tiuxetan
- tositumomab/131I-tositumomab
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What is CD52 antigen overexpressed?
Chronic lymphocytic leukemia (CLL)
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What drugs can used to treat CD52 antigen receptor overexpression?
alemtuzumab
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What is PMS-RARα fusion protein overexpressed?
Acute promyelocytic leukemia
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What drugs can used to treat PMS-RARα fusion protein receptor overexpression?
arsenic trioxide, tretinoin
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