GI Cancer Pharmacology

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What are the antimetabolite drugs for GI cancer:
- Capecitabine
- 5-FU
- Gemcitabine
What is the name of the drug that is an oral prodrug for 5-fluorouracil

Capecitabine (an antimetabolite)
Which antimetabolite drug is more frequently used for pancreatic cancer?

Gemcitabine
What is the MOA of antimetabolites?

They are cell cycle specific for S phase
Which of the 5-FU metabolites can impact RNA synthesis?

FUTP
(5-FU metabolite)_____inhibits thymidylate synthase and _____ interferes with DNA processing
- FdUMP
- FdUTP
FdUMP inhibits _________ and depletes nucleosides needed for DNA

Thymidylate synthase (TS)
FdUTP is incorporated into DNA and interferes with _______

DNA Processing
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)
Which drug comes with a black box warning for increased INR?

Capecitabine – because it is a CYP 2C9 inhibitor and interacts with Warfarin
Common toxicity of capecitabine and 5FU:
- Myelosuppression
- Mucositis/stomatitis, Conjunctival irritation
- Finger/ toe nails changes, sensitivity to sunlight
Which antimetabolite has major toxicities that include hand-foot syndrome and cardiac toxicity?

Capecitabine and 5FU
What is the MOA of Gemcitabine?

Inhibition of ribonucleic reductase and incorporation into DNA
Which drug can result in thrombocytopenia, especially with increased infusion of >60 mins?

Gemcitabine
Which drug requires a dose adjustment for renal function?

Capecitabine (an antimetabolite)
VEGF inhibitors:
- Bevacizumab
- Ramucirumab
- Ziv-Aflibercept
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
Side effect of VEGF inhibitors (Bevacizumab, Ramucirumab, Ziv-Aflibercept)?
- Hypertension
- Thromboembolism
- Non-GI fistula
Which drug can cause hypertension?

VEGF inhibitors (Bevacizumab, Ramucirumab, Ziv-Aflibercept) because it messes with angiogenesis
Which drug comes with a black box warning for GI perforations, wound dehiscence and hemorrhage?

VEGF inhibitors: (Bevacizumab, Ramucirumab, Ziv-Aflibercept)
What are agents of EGFR inhibitors?
- Cetuximab
- Panitumumab
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
What is EGFR? Which mutation can it result?
- Epidermal growth factor
- Can result in K-ras wild type mutation
Which drug can have dermatologic toxicity side effect and magnesium wasting?

EGFR inhibitors (Cetuximab, Panitumumab)
Which drug can lead to infusion reactions and cardiopulmonary arrest?

Cetuximab (an EGFR inhibitor)
Skin rash/lesion as a side effect is associated with ____-

EGFR inhibitors (Cetuximab, Panitumumab)
True/false: VEGF inhibitor can cause HTN and that can be managed with the usual antihypertensives

True
What are agents of tyrosine kinase inhibitors:
- Erlotinib
- Regorafenib
What is the MOA of TKI?

Prohibit phosphorylation of intracellular tyrosine kinase residue by blocking ATP binding sites
Erlotinib is the tyrosine kinase inhibitor of _______

EGFR
Major toxicities of Erlotinib:
- Interstitial lung disease
- Renal failure
- Hepatotoxicity
- GI perforation
- Hemolytic anemia
True/false: Regorafenib is metabolized by CYP3A4 and should be used separately from antacid and PPIs

False; that’s for erlotinib
Which TKI affects angiogenesis/ VEGF? EGFR?
- Regorafenib- VEGF
- Erlotinib- EGFR
Which TKI can cause hand-foot syndrome?

Regorafenib
What are common side effects of erlotinib?

Rash and diarrhea
Erlotinib should be taken with/on _________. Regorafenib should be taken with/on_______
- An empty stomach
- Low fat breakfast

Author

lykthrnn

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Card Set

GI Cancer Pharmacology

Description

GI Final- Pharmacology

Updated

2019-05-23T17:39:16Z

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