Angiogenesis Drugs Flashcards
Unique side effects of IL12
Thrombocytopenia, leukopenia, anemia
Liver problems, stomatitis
IL-12 induces ______ which activates ______ which causes an anti-angiogenic response
IFNg, Inducible protein 10
IFNa works by three mechanisms. What are they?
Decreases FGF (angiogenic)
Inhibits all cell division
Increases MHC I expression on tumor cells
What is a unique side effect to IFNa?
Depression
What is the protein necessary for angiogenesis when it senses nutrients are low?
mTOR
What is the receptor that activates mTOR?
VEGF-R
What is the humanized monoclonal antibody directly targeting VEGF?
Bevacizumab
Along with 5FU, Bevacizumab has been approved for treatment for which cancers?
Metastatic colon cancer, lung cancer, breast cancer
Bevacizumab has also been approved for which non-malignant diseases?
Macular degeneration and diabetic neuropathy
What are the unique side effects of Bevacizumab?
Wound dehiscence, GI perforation, and hemoptysis
These three drugs are inhibitors of VEGF-R and PDGF-R
Pazopanib, Sorafenib, Sunitinib
Pazopanib and sunitinib also block this important protein.
c-KIT
What cancer in particular do Pazopanib, Sorafenib, and sunitinib treat?
Renal cell carcinoma
What enzyme metabolizes these three drugs?
CYP3A4
What are some unique side effects for Pazopanib, Sorafenib, and Sunitinib?
Congestive heart failure, AMI, teratogenic
What two drugs are mTOR inhibitors?
Everolimus, Temsirolimus
What two important cell cycle proteins does mTOR regulate translation of?
Cyclin D1 and p21
What is the mode of resistance to Everolimus and Temsirolimus?
p-Glycoprotein
What are Everolimus and Temsirolimus metabolized by?
CYP 3A4
What specific cancer are mTOR inhibitors used for?
Renal cell carcinoma
Everolimus and Temsirolimus are uniquely toxic in these 4 ways:
Hypersensitivity reactions
Angioedema
Kidney arterial and venous thrombosis
Increased risk of lymphomas and infection
What’s the name of the “birth defect drug” and what is it used for?
Thalidomide, suppresses immune and inflammatory reactions and angiogenesis inhibitor
Thalidomide is the most effective anti-_____ agent known
TNF
What are the two approved diseases treated by thalidomide?
Multiple myeloma and Hansen’s disease
