Antineoplastics VI Flashcards
Size reached when a tumor must develop a blood supply?
1-2 mm in diameter
Rebound angiogenesis is associated with stopping what drug?
Bevaciximab
VEGF inhibitor?
Bevacizumab
Inhibitors of VEGF-R and PDGF-R?
Pazopanib
Sorafenib
Sunitinib
FGF inhibitor?
Thalidomide/Lenolinomide
Interferon
mTor inhibitors?
Everolimus
Temsiroliumus
Side effects of Bevacizumab?
GI perforation
wound dihiscence
worsen CAD?
Blocks Raf?
SoRAFenib
Blocks c-KIT?
Pazopanib
Sunitinib
What is c-KIT?
oncogenic tyrosine kinase
Two reasons to think about drug-drug interactions with STI’s (pazopanib, sorafinib, sunitinib)?
highly plasma protein bound
CYP3A4 metabolism
Specific toxicity for Pazopanib:
severe hepatotoxicity
QT prolongation–torsades de points
GI perforation
Hypertension
Specific Toxicity for Sorafenib?
hemorrhage
HTN
Specific toxicity for sunitinib?
skin discoloration, hand-foot syndrome
How do mTor inhibitors reduce cell growth and proliferation?
Everolimus, Temsirolimus
- mTor regulates synthesis of cyclin D1 which controls progression through G1/S phase checkpoint
- mTor increases expression of amino acid and glucose transporters involved in glycolysis to produce ATP
How do mTor inhibitor affect angiogenesis?
Everolimus, Temsirolimus
-decrease synthesis and release of angiogenic growth factors (VEGF, PDGF)
Pharmacokinetics of Everolimus, Temsirolimus?
CYP3A4 metabolism
**substrate for P-glycoprotein—>MDR
Toxicities of Everolimus, and Temsirolimus?
Hypersensitivity
increased risk of lymphoma
angioedema
kidney arterial and venous thrombosis
delays in wound healing
hyperlipidemia
nephrotoxicity and proteinuria
male infertility
Drug that causes phocomelia (short limbs):
Thalidomide
Read website and try to figure out regimen chart on last PPT slide.
Read up.
