Tìm theo
Bevacizumab
Các tên gọi khác (2) :
  • antiVEGF
  • Avastin
angiogenesis inhibitors
Thuốc Gốc
Biotech
CAS: 216974-75-3
ATC: L01XC07
ĐG : F Hoffmann-La Roche Ltd. , http://www.roche.com
CTHH: C6538H10034N1716O2033S44
PTK: 149 kDa
A recombinant humanized monoclonal IgG1 antibody that binds to and inhibits the biologic activity of human vascular endothelial growth factor (VEGF). Bevacizumab contains human framework regions and the complementarity-determining regions of a murine antibody that binds to VEGF. Bevacizumab is produced in a Chinese Hamster Ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin and has a molecular weight of approximately 149 kilodaltons.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6538H10034N1716O2033S44
Phân tử khối
149 kDa
Độ tan chảy
61 °C (FAB fragment), 71 °C (whole mAb)
Dược Lực Học : Bevacizumab is an antineoplastic agent and 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.
Cơ Chế Tác Dụng : A recombinant humanized monoclonal IgG1 antibody that binds to and inhibits the biologic activity of human vascular endothelial growth factor (VEGF). Bevacizumab contains human framework regions and the complementarity-determining regions of a murine antibody that binds to VEGF. Bevacizumab is produced in a Chinese Hamster Ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin and has a molecular weight of approximately 149 kilodaltons. Bevacizumab contains human framework regions with antigen binding regions of a humanised murine antibody that binds to VEGF. Bevacizumab is produced by recombinant DNA technology in a Chinese hamster ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin and is purified by a process that includes specific viral inactivation and removal steps. Bevacizumab 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 in response retardation of metastatic tumor growth occurs.
Dược Động Học :

▧ Volume of Distribution :
Vd: 46 mL/kg
▧ Metabolism :
Most likely removed by opsonization via the reticuloendothelial system when bound to endothelial cells, or by human antimurine antibody production
▧ Half Life :
approximately 20 days (range: 11–50 days)
▧ Clearance :
* 0.26 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] Clearance varies by body weight, gender, and tumor burden. Increased clearance observed in men and in patients with higher tumor burden; however, no evidence of reduced efficacy.
Độc Tính : Category C in pregnancy. No studies on lactating patients: recommended to discontinue the drug or discontinue lactation. No extensive studies in pediatrics. In geriatrics: increased risk of proteinuria, arterial thromboembolic events, as well as GI bleeding and sepsis among others.
Chỉ Định : As part of combination therapy for metastatic colorectal cancer and HER2-negative metastatic breast cancer.
Tương Tác Thuốc :
  • Belimumab Avoid combination due to enhanced adverse effects of bevacizumab
  • Clozapine Avoid combination due to increased adverse effects of clozapine, especially the risk of agranulocytosis.
  • Irinotecan Monitor therapy due to increased adverse effects of irinotecan.
  • Sorafenib Monitor therapy due to increased adverse effects of sorafenib, especially hand-foot skin reaction.
  • Sunitinib Sunitinib may enhance the adverse/toxic effect of bevacizumab. Specifically, the risk for a specific form of anemia, microangiopathic hemolytic anemia (MAHA), may be increased. Bevacizumab may enhance the hypertensive effect of sunitinib. This combination is contraindicated.
Liều Lượng & Cách Dùng : Solution - Intravenous
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00112
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50242-060-01
PharmGKB
http://www.pharmgkb.org/drug/PA130232992
Wikipedia
http://en.wikipedia.org/wiki/Bevacizumab
RxList
http://www.rxlist.com/cgi/generic3/avastin.htm
Drugs.com
http://www.drugs.com/cdi/bevacizumab-solution.html
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