Pharmacology: Antineoplastics III - 2

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kyleannkelsey
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Pharmacology: Antineoplastics III - 2
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2014-04-19 15:34:21
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Pharmacology Antineoplastics III
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Pharmacology: Antineoplastics III - 2
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Pharmacology: Antineoplastics III - 2
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  1. Does Sorafenib (Nexavar) cause QT prolongation?
    No
  2. What is the MOA of Sunitinib (Sutent)?
    • Multiple receptor tyrosine kinases inhibitor
    • Inhibits cellular growth and tumor metastasis
  3. What is the indication for Sunitinib (Sutent)?
    • Advanced renal cell carcinoma (main one to know)
    • Gastrointestinal stromal tumors
  4. What are the SEs for Sunitinib (Sutent)?
    Fatigue, hypertension, cardiac dysfunction/QT prolongation
  5. What are the DDIs for Sunitinib (Sutent)?
    CYP3A4 DDIs
  6. Does Sunitinib (Sutent) cause myelosupression?
    No
  7. Does Sunitinib (Sutent) cause QT prolongation?
    Yes
  8. Which Ras/Map Kinase Pathway Inhibitors cause QT prolongation?
    Sunitinib
  9. What is the indication of pazopanib (Votrient)?
    Advanced renal cell carcinoma
  10. What is the indication for vandetanib (Caprelsa)?
    Advanced medullary thyroid cancer
  11. What is the MOA for Vemurafenib (Zelboraf)?
    • Inhibits SER-THR kinase with a BRAFv600 mutation
    • (mutation = Valine to Glutamic acid)
  12. What are the indications for Vemurafenib (Zelboraf)?
    Metastatic melanoma
  13. What are the SE for Vemurafenib (Zelboraf)?
    • QT prolongation
    • Hypersensitivity
    • Secondary malignancies
  14. What drugs are m TOR kinase inhibitors?
    Temsirolimus or Everolimus
  15. Temsirolimus (Torisel) is a prodrug to what other drug?
    Sirolimus
  16. What is the MOA of Temsirolimus (Torisel)?
    • Inhibits protein kinase that regulates cell growth/proliferation, mTOR
    • Leads to G1 arrest and apoptosis
  17. What is the indication for Temsirolimus (Torisel)?
    Advanced stage renal cell carcinoma
  18. What are the SE for Temsirolimus (Torisel)?
    Hypersensitivity, immunosuppression, hyperglycemia, hyperlipidemia, hypertriglyceridemia, Bone marrow supression
  19. What are the DDIs for Temsirolimus (Torisel)?
    CYP3A4 DDIs
  20. What is the indication for everolimus (Aftinitor)?
    Advanced cell renal carcinoma
  21. What is the MOA for everolimus (Aftinitor)?
    • Inhibits protein kinase that regulates cell growth/proliferation, mTOR
    • Leads to G1 arrest and apoptosis
  22. What are the SE for everolimus (Aftinitor)?
    Hypersensitivity, immunosuppression, hyperglycemia, hyperlipidemia, hypertriglyceridemia, bone marrow suppression
  23. What is the Anaplastic lymphoma kinase inhibitor?
    crizotinib (Xalkori)
  24. What are the indications for crizotinib (Xalkori)?
    Advanced non-small cell lung cancer (NSCLC)
  25. What is the MOA for crizotinib (Xalkori)?
    Inhibits anaplastic lymphoma kinase (ALK) (tyrosine kinase) positive cancer cells
  26. What are the SE for crizotinib (Xalkori)?
    QT problems, visual disturbances (critical one to watch out for this)
  27. What is the MOA for bortezomib (Velcade)?
    • 26S Proteasome inhibitor
    • Accumulation of proteins through proteasome inhibition leads to apoptosis and increased sensitivity to radiation and traditional anticancer drugs
  28. What are the indication for bortezomib (Velcade)?
    • Multiple myeloma (most important)
    • Mantle cell lymphoma
  29. What are the SE for bortezomib (Velcade)?
    GI effects, bone marrow suppression, constipation, peripheral neuropathy and fever
  30. What drugs inhibit angiogenesis?
    • Bevacizumab (Avastin)
    • Thalidomide (Thalomid)
    • Lenalidomide (Revlimid)
  31. What is the MOA for Bevacizumab (Avastin)?
    • Suppresses angiogenesis depriving tumors of blood supply
    • Monoclonal antibody binding to VEGF preventing its binding to vascular receptors
  32. What are the indications for Bevacizumab (Avastin)?
    • Metastatic cancer of the colon or rectum (with 5-FU)
    • Non-squamous non-small cell lung cancer with carboplatin and paclitaxel
  33. What are the SE for bevacizumab (Avastin)?
    • GI perforation
    • disrupted wound healing
    • pulmonary hemorrhage
    • kidney damage
    • hypertensive crisis
    • thromboembolism
    • D/C with any of these symptoms
  34. Does bevacizumab (Avastin) cause myelosupression?
    No
  35. Does resistant develop to bevacizumab (Avastin)?
    No
  36. What is the MOA for Thalidomide (Thalomid)?
    • Suppresses angiogenesis by inhibiting FGF (fibroblast growth factor) and TNF alpha
    • Costimulates T cells (immunomodulator drug)
  37. What is the indication or thalidomide (Thalomid)?
    multiple myeloma
  38. What are the SE for thalidomide (Thalomid)?
    • Well tolerated with exception of
    • neuropathy
    • constipation
    • thromboembolism (risk of MI/stroke)
    • powerful teratogen (CI in pregnancy = STEPS program)
  39. What is the MOA of Lenalidomide (Revlimid)?
    Suppresses angiogenesis by enhanced inhibition of TNF alpha and costimulation of T cells
  40. What are the indications for lenalidomide (Revlimid)?
    multiple myeloma
  41. What are the SE for lenalidomide (Revlimid)?
    • Fewer side effects than thalidomide
    • Teratogenicity
    • Increased myelosuppression
    • Thrombocytopenia
  42. What is the MOA of rituximab (Rituxan)?
    • Monoclonal antibody binds to antigen CD20 found on B-cell precursors and mature B-lymphocytes
    • CD20 regulates = early step in activation of cell cycle initiation and differentiation.
    • Results in apoptosis
    • Immune attack against B cells
  43. What is the Indication for rituximab (Rituxan)?
    • B-cell non-Hodgkin’s lymphoma (NHL)
    • Chronic lymphocytic leukemia (CLL)
  44. What regimen is rituximab (Rituxan) usually combined in?
    CHOP regime
  45. Other than antineoplasm, what can rituximab (Rituxan) be used for?
    Rheumatoid arthritis
  46. What are the SE for rituximab (Rituxan)?
    • Very Severe SE
    • Infusion related events (hypersensitivity, fever, chills),
    • cardiac events
    • lymphopenia
    • reactivation of HBV infections
    • immunosuppression (test for infections prior to use)
  47. What is the MOA for Ibritumomab tiuxetan (Zevalin)?
    • Monoclonal antibody (anti-CD20) ibritumomab linked with the chelator tiuxetan
    • Chelator provides a high affinity site for Indium-111 or Yttrium-90 (beta emitter radioactive isotopes)
    • B cells are killed by radiation
  48. Why is Rituximab is given in two small doses prior to ibritumomab tiuxetan?
    To reduce B cells and reduce nonspecific binding sites
  49. What are the indications for Ibritumomab tiuxetan (Zevalin)?
    non Hodgkin’s Lymphoma (NHL)
  50. What are the SE for ibritumomab tiuxetan (Zevalin)?
    • Same as rituximab
    • Very Severe SE
    • Infusion related events (hypersensitivity, fever, chills),
    • cardiac events
    • lymphopenia
    • reactivation of HBV infections
    • immunosuppression (test for infections prior to use)
    • IN ADDITION: severe bone marrow suppression
  51. What is the MOA for Tositumomab/131I-tositumomab (Bexxar)?
    • Monoclonal antibody tositumomab (anti-CD20) unlinked and linked with the 131I.
    • B cells are killed by immune attack resulting in apoptosis and radiation
  52. What are the indications for tositumomab/131I-tositumomab (Bexxar)?
    Rituximab refractory non Hodgkin’s Lymphoma (NHL)
  53. What are the SE for tositumomab/131I-tositumomab (Bexxar)?
    • Severe bone marrow suppression, hypersensitivity, infusion reactions, GI toxicity, hypothyroidism (due to Iodine)
    • Contraindicated for pregnancy

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