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What are the antineoplastic glucocorticoid receptor specific hormones?
- Prednisone
- Dexamethasone (Decadron)
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What is the MOA for Glucocorticoid antineoplastics (prednisone and dexamethasone)?
- Repress of activate transcription through a nuclear binding process
- Cause apoptosis of lymphocytes
- Have Lympholytic effects
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What are the indications for Glucocorticoid antineoplastics?
- Acute and chronic leukemias
- Breast cancer
- Hodgkin’s Lymphoma
- Non-Hodgkin’s Lymphoma
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What are the SE’s of glucocorticoid antineoplastics?
Truncal obesity, moon face, fragile skin, susceptibility to infections
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How do you D/C Glucocorticoid antineoplastics?
Slowly to avoid adrenal insufficiency
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What is the mechanism of action of Cetuximab?
- Inhibits Tyrosine kinase through inhibition of EGFR receptors
- Eventually causes apoptosis and growth inhibition
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Cetuximab brand name:
Erbitux
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What are the indications for Cetuximab?
- EGFR positive colorectal, head and neck cancers
- Investigational for EGFR over-expressing tumors
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What is Cetuximab (Erbitux) often used in combo wuth>
Irinotecan
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What are the major toxicities of Cetuximab (Erbitux)?
- Severe infusion reactions (b/c giving an antibody)
- Acne-like rash
- Interstitial lung disease
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How do you prevent infusion reactions by Cetuximab (Erbitux)?
Pretreat with an antihistamine
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What type of antibody is Panitumumab (Vectibix)?
Full human
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What is the MOA for Panitumumab (Vectibix)?
- Inhibits Tyrosine kinase through inhibition of EGFR receptors
- Eventually causes apoptosis and growth inhibition
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What is the brand name for Panitumumab?
Vectibix
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What are the side effects of Panitumumab (Vectibix)?
Rare infusion reaction and interstitial lung disease
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What is the only indication for Panitumumab (Vectibix)?
Colorectal cancer
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Why does Panitumumab (Vectibix) have fewer infusion reactions than Cetuximab?
Panitumumab (Vectibix) is a human antibody and Cetuximab is a mouse
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Elortinib (Tarceva) is given by what route?
Oral
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What DDIs does Elortinib (Tarceva) have?
CYP3A4 related
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What is the MOA of Elortinib (Tarceva)?
Cystolic inhibitor of EGFR-TK
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What group of patients does Elortinib (Tarceva) work best in?
Female non-smokers
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What is the indication or Erlotinib?
Non-small cell lung cancer w/ a specific mutation
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What is the black box warning for Erlotinib (Tarveca)?
- GI perforation
- Must stop the drug if this occurs
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Does Erlotinib (Tarveca) cause bone marrow suppression?
No
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What are the SE of Erlotinib (Tarveca)?
- SE are mild
- Mild rash and diarrhea
- Only worrisome one = GI perforation (BB)
- CI in pregnancy
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What drugs work extracellularly on the EGFR?
Pantumamab, Cetuximab and Trastuzimab
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What drugs work intracellularly on the EGFR?
Lapatinib, Gefitinib and Erlotinab
-
What are the drugs that act on ABL used for?
Chronic myolegenous leukemia
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What drugs act on ABL?
Imatinib, Nilotinib and Dasatinib
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Imatinib, Nilotinib, Dasatinib are metabolized by what enzyme?
CYP3A4
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What is the MOA for imatinib (Gleevac)?
Competitive inhibition of ATP binding site on C-ABL, C-Kit ad PDGFR
-
What is the route of administration of imatinib (Gleevac)?
Oral
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What are the DDIs associated with imatinib (Gleevac)?
CYP3A4 related
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What are the indications for imatinib (Gleevac)?
- Chronic myelogenous leukemia (CML)
- GI stromal cell tumors expressing C-KIT
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What are the SE for Imatinib (Gleevec)?
- GI, hepatotoxic, rashes, fatigue, Fluid retention
- Neutropenia/thrombocytopenia (myelosupression)
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What is the MOA of Nilotinib (Tasigna)?
Binds inactive BCR-ABL
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How does the binding affinity of Nilotinib (Tasigna) compare to imatinib (Gleevac)?
Nilotinib (Tasigna) has greater binding affinity
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What are the indicatios for Nilotinib (Tasigna)?\
- CML
- Used against all imatinib resistant clones EXCEPT T3151 mutations
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What are the SE of Nilotinib (Tasigna)?
- Prolongs QT
- (less severe SE overall than imatinib)
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What is the MOA of dasatinib (Sprycel)?
- Binds variety of PKs
- Binds inactive OR active BCR-ABL
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How does the binding affinity of dasatinib (Sprycel) compare to imatinib (Gleevac)?
dasatinib (Sprycel) has greater binding affinity
-
What are the indications for dasatinib (Sprycel)?
- CML
- Used against all imatinib resistant clones EXCEPT T3151 mutations
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What are the SE’s for dasatinib (Sprycel)?
- Prolong QT
- Similar to imatinib
- Myelosupression
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What are the RAS-MAP kinase inhibitors?
- sorafenib
- sunitinib
- vemurafenib
- pazopanib
- vandetanib
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What is the MOA of Sorafenib (Nexavar)?
- Inhibits multiple Tyrosine kinases via inhibition of phosphorylation
- Results in angiogenesis (capillary growth) and metastasis
-
What is the indication for Sorafenib (Nexavar)?
Advanced renal cell carcinoma
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What are the SE for Sorafenib (Nexavar)?
GI, rash, fatigue, hand-and-foot syndrome, HTN
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What are the DDIs for Sorafenib (Nexavar)?
CYP3A4 DDIs
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Does Sorafenib (Nexavar) cause myelosupression?
No
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