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1468 details
Primary information
ThPP IDTh1091
Therapeutic Peptide/Protein NameBevacizumab
SequenceDIQMTQSPSSLSASVGDRVTITCSASQDISNYLNWYQQKPGKAPKVLIYF view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight149000
Chemical FormulaC6538H10034N1716O2033S44
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)61 (FAB fr
Half LifeN.A.
DescriptionRecombinant (derived from CHO-gentamycin), humanized, monoclonal IgG1 antibody. It Inhibits the biologic activity of human vascular endothelial growth factor (VEGF) by binding to it. Comprises human framework regions and murine complementarity-determining regions.
Indication/DiseaseAs part of combination therapy for metastatic colorectal cancer and HER2-negative metastatic breast cancer.
PharmacodynamicsBevacizumab prevents or reduces the formation of blood vessels (angiogenesis) thereby preventing or reducing metatstatic disease progressing. Bevacizumab binds VEGF and prevents vascular endothelial growth and endothelial cell proliferation.
Mechanism of ActionBevacizumab binds VEGF and prevents the interaction of VEGF to its receptors (Flt-1 and KDR) on the surface of endothelial cells. This prevents blood vessel proliferation and tumour metastasis.
ToxicityN.A.
MetabolismMost likely removed by opsonization via the reticuloendothelial system when bound to endothelial cells, or by human antimurine antibody production
AbsorptionN.A.
Volume of DistributionN.A.
Clearance0.26 L/day [Male patients who received 1 to 20 mg/kg of Avastin weekly, every 2 weeks, or every 3 weeks] 0.21 L/day [Female patients who received 1 to 20 mg/kg of Avastin weekly, every 2 weeks, or every 3 weeks] 0.25 L/day [Patients with higher tumor burden who received 1 to 20 mg/kg of Avastin weekly, every 2 weeks, or every 3 weeks]* 0.2 L/day [patients with tumor burdens below the median who received 1 to 20 mg/kg of Avastin weekly, every 2 weeks, or every 3 weeks]
CategoriesAngiogenesis Inhibitors
Patents NumberCA2286330
Date of Issue11/06/12
Date of Expiry04/04/22
Drug InteractionN.A.
TargetInterleukin-2 receptor subunit alpha,Interleukin-2 receptor subunit beta,Low affinity immunoglobulin gamma Fc region receptor III-B,Complement C1r subcomponent,Complement C1q subcomponent subunit A,Complement C1q subcomponent subunit B,Complement C1q subcomponent subunit C,Low affinity immunoglobulin gamma Fc region receptor III-A,High affinity immunoglobulin gamma Fc receptor I,Low affinity immunoglobulin gamma Fc region receptor II-a,Low affinity immunoglobulin gamma Fc region receptor II-b,Low affinity immunoglobulin gamma Fc region receptor II-c
Information of corresponding available drug in the market
Brand NameAvastin
CompanyGenentech
Brand DiscriptionAvastin (bevacizumab) is a recombinant humanized monoclonal IgG1 antibody that binds to and inhibits the biologic activity of human vascular endothelial growth factor (VEGF) in in vitro and in vivo assay systems. Bevacizumab contains human framework regions and the complementarity-determining regions of a murine antibody that binds to VEGF. Avastin has an approximate molecular weight of 149 kD. Bevacizumab is produced in a mammalian cell (Chinese Hamster Ovary) expression system in a nutrient medium containing the antibiotic gentamicin. Gentamicin is not detectable in the final product.
Prescribed forMetastatic Colorectal Cancer (mCRC): Avastin is indicated for the first- or second-line treatment of patients with metastatic carcinoma of the colon or rectum. Non-Squamous Non-Small Cell Lung Cancer (NSCLC), glioblastoma with progressive disease in adult patients. Metastatic Renal Cell Carcinoma (mRCC): Avastin is indicated for the treatment of metastatic renal cell carcinoma in combination with interferon alfa. Persistent, Recurrent, Or Metastatic Carcinoma Of The Cervix: Avastin in combination with paclitaxel and cisplatin or paclitaxel and topotecan is indicated for the treatment of persistent, recurrent, or metastatic carcinoma of the cervix.
Chemical NameN.A.
Formulation100 mg product is formulated in 240 mg a,a-trehalose dihydrate, 23.2 mg sodium phosphate (monobasic, monohydrate), 4.8 mg sodium phosphate (dibasic, anhydrous), 1.6 mg polysorbate 20, and Water for Injection, USP. The 400 mg product is formulated in 960 mg a,a-trehalose dihydrate, 92.8 mg sodium phosphate (monobasic, monohydrate), 19.2 mg sodium phosphate (dibasic, anhydrous), 6.4 mg polysorbate 20, and Water for Injection, USP.
Physcial AppearnceSlightly opalescent, colorless to pale brown, sterile, pH 6.2 solution
Route of AdministrationIntravenous infusion
Recommended DosageFirst infusion: Administer infusion over 90 minutes. Subsequent infusions: Administer second infusion over 60 minutes if first infusion is tolerated; Recommended Doses And Schedules: Metastatic Colorectal Cancer (mCRC).The recommended doses are 5 mg/kg or 10 mg/kg every 2 weeks when used in combination with intravenous 5-FU-based chemotherapy. Administer 5 mg/kg when used in combination with bolus-IFL. Administer 10 mg/kg when used in combination with FOLFOX4. Administer 5 mg/kg every 2 weeks or 7.5 mg/kg every 3 weeks when used in combination with a fluoropyrimidine-irinotecan or fluoropyrimidine-oxaliplatin based chemotherapy regimen in patients who have progressed on a first-line Avastin-containing regimen. Non-Squamous Non-Small Cell Lung Cancer (NSCLC): The recommended dose is 15 mg/kg every 3 weeks in combination with carboplatin and paclitaxel. Glioblastoma: The recommended dose is 10 mg/kg every 2 weeks. Metastatic Renal Cell Carcinoma (mRCC): The recommended dose is 10 mg/kg every 2 weeks in combination with interferon alfa. Cervical Cancer: The recommended dose of Avastin is 15 mg/kg every 3 weeks as an Intravenous infusion administered in combination with one of the following chemotherapy regimens: paclitaxel and cisplatin, or paclitaxel and topotecan.
ContraindicationDo not administer as an intravenous push or bolus. Administer only as an intravenous (IV) infusion.. Do not initiate Avastin until at least 28 days following major surgery. Administer Avastin after the surgical incision has fully healed.
Side Effectsheadache, confusion, vision problems, feeling very weak or tired, fainting, and seizure (blackout or convulsions)
Useful Linkhttp://www.rxlist.com/avastin-drug.htm http://www.avastin.com/patient/ http://maculacenter.com/eye-procedures/avastin/
PubMed ID25638326, 25637137, 25631483, 25628268, 25627091, 25624888, 18343240, 18054637, 17409907
3-D StructureTh1091 (View) or (Download)