Pharmacology: Antineoplastics IV/V -1

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  1. 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
  2. What are the indications for ipilimumab (Yervoy)?
    Metastatic melanoma, often used with dacarbazine.
  3. What are the SE for ipilimumab (Yervoy)?
    Immune mediated conditions (GI-enterocolitis, hepatitis, neuropathy, rash)
  4. 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
  5. 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
  6. What are the SE for brentuximab vedotin (Adcetris)?
    peripheral neuropathy, neutropenia, infusion reactions.
  7. What are the Histone deactylase (HDAC) inhibitors?
    vorinostat (Zolinza) and romidepsin (Istodax)
  8. 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.
  9. What is the indication for vorinostat (Zolinza) and romidepsin (Istodax)?
    cutaneous T-cell lymphoma
  10. What are the SE for vorinostat (Zolinza) and romidepsin (Istodax)?
    GI, anemia, thrombocytopenia, pulmonary embolism
  11. What are the Immunostimulants?
    • Interferon alfa-2a (Roferon)
    • Interferon alfa-2b (Intron)
    • Aldesleukin
  12. 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
  13. What is the brand name for Interferon alfa-2a?
  14. What is the brand name for Interferon alfa-2b?
  15. 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
  16. What are the adverse effects of vorinostat (Zolinza) and romidepsin (Istodax)?
    Flu-like symptoms
  17. What is EGFR (ErbB1) overexpressed?
    • Non-small cell lung cancer;
    • Head and neck cancer
    • Colon cancer,
    • Pancreatic cancer
  18. What drugs can used to treat EGFR (ErbB1) receptor overexpression?
    • gefitinib, erlotinib
    • cetuximab, panitumumab
  19. What is VEGFR-1,2 overexpressed?
    Advanced renal cell carcinoma
  20. What drugs can used to treat VEGFR-1,2 receptor overexpression?
    sorafenib, sunitinib
  21. What is VEGF ligand overexpressed?
    Breast, colorectal, lung, malignant glioma, non-small cell lung cancer
  22. What drugs can used to treat VEGF ligand receptor overexpression?
  23. What is HER-2/neu (ErbB2) overexpressed?
    Breast cancer
  24. What drugs can used to treat HER-2/neu (ErbB2) receptor overexpression?
    • Trastuzumab,
    • lapatinib
  25. What is PDGFR overexpressed?
    Gastrointestinal stromal tumor (GIST)
  26. What drugs can used to treat PDGFR receptor overexpression?
    Sorafenib, sunitinib
  27. What is FGFR3 overexpressed?
    Multiple myeloma
  28. What drugs can used to treat FGFR3 receptor overexpression?
    thalidomide, lenalidomide (inhibiting
  29. What is c-KIT overexpressed?
    Gastrointestinal stromal tumor (GIST)
  30. What drugs can used to treat c-KIT receptor overexpression?
  31. What is BCR-ABL overexpressed?
    • Chronic myelogenous leukemia (CML)
    • Acute promyelocytic leukemia (APL)
  32. What drugs can used to treat BCR-ABL receptor overexpression causing APL?
  33. What drugs can used to treat BCR-ABL receptor overexpression causing APL?
    Arsenic trioxide, tretinoin
  34. What is asparaginase overexpressed?
    Acute lymphocytic leukemia (ALL)
  35. What drugs can used to treat asparaginase receptor overexpression?
  36. What is CD30 antigen overexpressed?
    Hodgkin’s Lymphoma
  37. What drugs can used to treat CD30 receptor overexpression?
    brentuximab vedotin
  38. What is CD20 antigen overexpressed?
    B-cell non-Hodgkin’s lymphoma (NHL)
  39. What drugs can used to treat X receptor overexpression?
    • rituximab
    • ibritumomab tiuxetan
    • tositumomab/131I-tositumomab
  40. What is CD52 antigen overexpressed?
    Chronic lymphocytic leukemia (CLL)
  41. What drugs can used to treat CD52 antigen receptor overexpression?
  42. What is PMS-RARα fusion protein overexpressed?
    Acute promyelocytic leukemia
  43. What drugs can used to treat PMS-RARα fusion protein receptor overexpression?
    arsenic trioxide, tretinoin
Card Set:
Pharmacology: Antineoplastics IV/V -1
2014-04-19 20:41:10
Pharmacology Antineoplastics IV
Pharmacology: Antineoplastics IV/V -1
Pharmacology: Antineoplastics IV/V -1
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