ziv-aflibercept + leucovorin + fluorouracil + irinotecan
Approval Time : Aug. 3, 2012
Direct Target : VEGFA,VEGFB,PGF
Indications : Ziv-aflibercept was approved to be used in combination with FOLFIRI (fluorouracil, leucovorin, irinotecan) for the treatment of metastatic colorectal cancer resistant to or progressing after an oxaliplatin-containing regimen.
Mechanism Of Action :
Ziv-aflibercept acts as a soluble receptor that binds to human VEGF-A (equilibrium dissociation constant KD of 0.5 pM for VEGF-A165 and 0.36 pM for VEGF-A121), to human VEGF-B (KD of 1.92 pM), and to human PlGF (KD of 39 pM for PlGF-2). By binding to these endogenous ligands, ziv-aflibercept can inhibit the binding and activation of their cognate receptors. This inhibition can result in decreased neovascularization and decreased vascular permeability. In animals, ziv-aflibercept was shown to inhibit the proliferation of endothelial cells, thereby inhibiting the growth of new blood vessels. Ziv-aflibercept inhibited the growth of xenotransplanted colon tumors in mice.
Dosage : The recommended dose of ziv-aflibercept is given at 4 mg/kg by IV infusion over 1 hour every 2 weeks in combination with FOLFIRI. It must be administered before any component of FOLFIRI on the day of treatment, and it must be administered through a 0.2-micron polyethersulfone filter.
Related Targets and Diseases
| Drug Name |
Gene |
|
Disease |
|
Negative Genotypes |
Drug Brand |
|
Drug Type |
|
