Bevacizumab

Better Known as: Avastin Marketed By: Genentech & Roche Major Indication: Colorectal Cancer Drug Class: Vascular Endothelial Growth Factor Inhibitor - Monoclonal Antibody Date of FDA Approval (Patent Expiration): 2004 (2019) 2009 Sales: $4.8 Billion Importance: It is one of the best selling cancer treatments in history. Despite being effective against colorectal cancer, post-approval studies after accelerated approval revealed that Avastin was ineffective in treating breast cancer. Many question the $90,000/year bill to take Avastin when it extends life on average only 10 months. See Pharmaceutical Drugs for more information about other drugs and disorders Mechanism of Action Vascular Endothelial Growth Factor (VEGF) is a signal protein often over-expressed in cancerous cells. It is responsible for activating Vascular Endothelial Growth Factor Receptors (VEGFRs) to accelerate angiogenesis and vasculogenesis. Accelerated angiogenesis creates the overly developed blood vessel system common to all tumors, providing oxygen and nutrients to the prodigal tumors. Bevacizumab binds to VEGF, preventing it from interacting with VEGFR, thus halting accelerated angiogenesis in tumors, preventing the cancer from growing rapidly. Pharmacokinetics VEGF Inhibitor Pharmacokinetics Parameter Bevacizumab Tmax (hr) 5.17 Cmax (ng/ml) 284000 Bioavailability (%) 100 T1/2 (days) 20 AUC (ug/ml/hr) 97488 IC50 (nM) .9 Clearance (L/h) .0096 Dosage (mg/kg) 10

spinqualitylabelsall models Model Bevacizumab, also known as Avastin (PDB code 1igt) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image