GI Cancer Pharmacology

  1. What are the antimetabolite drugs for GI cancer:
    • Capecitabine
    • 5-FU
    • Gemcitabine
  2. What is the name of the drug that is an oral prodrug for 5-fluorouracil
    Capecitabine (an antimetabolite)
  3. Which antimetabolite drug is more frequently used for pancreatic cancer?
  4. What is the MOA of antimetabolites?
    They are cell cycle specific for S phase
  5. Which of the 5-FU metabolites can impact RNA synthesis?
  6. (5-FU metabolite)_____inhibits thymidylate synthase and _____ interferes with DNA processing
    • FdUMP
    • FdUTP
  7. FdUMP inhibits _________ and depletes nucleosides needed for DNA
    Thymidylate synthase (TS)
  8. FdUTP is incorporated into DNA and interferes with _______
    DNA Processing
  9. Which drug is used in combination with 5FU to enhance its activity? What is the MOA?
    • Leucovorin
    • Enhances binding of FdUMP to Thymidylate synthase (TS)
  10. Which drug comes with a black box warning for increased INR?
    Capecitabine – because it is a CYP 2C9 inhibitor and interacts with Warfarin
  11. Common toxicity of capecitabine and 5FU:
    • Myelosuppression
    • Mucositis/stomatitis, Conjunctival irritation
    • Finger/ toe nails changes, sensitivity to sunlight
  12. Which antimetabolite has major toxicities that include hand-foot syndrome and cardiac toxicity?
    Capecitabine and 5FU
  13. What is the MOA of Gemcitabine?
    Inhibition of ribonucleic reductase and incorporation into DNA
  14. Which drug can result in thrombocytopenia, especially with increased infusion of >60 mins?
  15. Which drug requires a dose adjustment for renal function?
    Capecitabine (an antimetabolite)
  16. VEGF inhibitors:
    • Bevacizumab
    • Ramucirumab
    • Ziv-Aflibercept
  17. What is the MOA of VEGF inhibitors (Bevacizumab, Ramucirumab, Ziv-Aflibercept)?
    Targets VEGF ligand to prevent it from binding to the VEGF receptor which ultimately result in inhibition of cancer cell angiogenesis
  18. Side effect of VEGF inhibitors (Bevacizumab, Ramucirumab, Ziv-Aflibercept)?
    • Hypertension
    • Thromboembolism
    • Non-GI fistula
  19. Which drug can cause hypertension?
    VEGF inhibitors (Bevacizumab, Ramucirumab, Ziv-Aflibercept) because it messes with angiogenesis
  20. Which drug comes with a black box warning for GI perforations, wound dehiscence and hemorrhage?
    VEGF inhibitors: (Bevacizumab, Ramucirumab, Ziv-Aflibercept)
  21. What are agents of EGFR inhibitors?
    • Cetuximab
    • Panitumumab
  22. What is the MOA of EGFR inhibitor (Cetuximab, Panitumumab)?
    Binds to EGFR and competitively inhibits the binding of EGF which prevents phosphorylation and activation of receptor kinases thereby inhibiting cell growth, metastasis and signal transduction
  23. What is EGFR? Which mutation can it result?
    • Epidermal growth factor
    • Can result in K-ras wild type mutation
  24. Which drug can have dermatologic toxicity side effect and magnesium wasting?
    EGFR inhibitors (Cetuximab, Panitumumab)
  25. Which drug can lead to infusion reactions and cardiopulmonary arrest?
    Cetuximab (an EGFR inhibitor)
  26. Skin rash/lesion as a side effect is associated with ____-
    EGFR inhibitors (Cetuximab, Panitumumab)
  27. True/false: VEGF inhibitor can cause HTN and that can be managed with the usual antihypertensives
  28. What are agents of tyrosine kinase inhibitors:
    • Erlotinib
    • Regorafenib
  29. What is the MOA of TKI?
    Prohibit phosphorylation of intracellular tyrosine kinase residue by blocking ATP binding sites
  30. Erlotinib is the tyrosine kinase inhibitor of _______
  31. Major toxicities of Erlotinib:
    • Interstitial lung disease
    • Renal failure
    • Hepatotoxicity
    • GI perforation
    • Hemolytic anemia
  32. True/false: Regorafenib is metabolized by CYP3A4 and should be used separately from antacid and PPIs
    False; that’s for erlotinib
  33. Which TKI affects angiogenesis/ VEGF? EGFR?
    • Regorafenib- VEGF
    • Erlotinib- EGFR
  34. Which TKI can cause hand-foot syndrome?
  35. What are common side effects of erlotinib?
    Rash and diarrhea
  36. Erlotinib should be taken with/on _________. Regorafenib should be taken with/on_______
    • An empty stomach
    • Low fat breakfast
Card Set
GI Cancer Pharmacology
GI Final- Pharmacology