Tìm theo
Brentuximab vedotin
Các tên gọi khác (1) :
  • cAC10-vcMMAE
Thuốc Gốc
Biotech
CAS: 914088-09-8
ATC: L01XC12
CTHH: C6476H9930N1690O2030S40
PTK: 149.2–151.8 kDa
Brentuximag vedotin or Adcetris® is an antibody-drug conjugate that combines an anti-CD30 antibody and the drug monomethyl auristatin E (MMAE). It is an anti-neoplastic agent used in the treatment of Hodgkin lymphoma and systemic anaplastic large cell lymphoma. Brentuximag vedotin was approved in 2011, and in January 2012, the drug label was revised to include a boxed warning of progressive multifocal leukoencephalopathy and death following JC virus infection.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6476H9930N1690O2030S40
Phân tử khối
149.2–151.8 kDa
Dược Lực Học : Brentuximag vedotin causes apoptosis of tumor cells by preventing cell cycle progression of the G2 to M phase through disruption of the cytosolic mictrotuble network.
Cơ Chế Tác Dụng : Brentuximag vedotin or Adcetris® is an antibody-drug conjugate that combines an anti-CD30 antibody and the drug monomethyl auristatin E (MMAE). It is an anti-neoplastic agent used in the treatment of Hodgkin lymphoma and systemic anaplastic large cell lymphoma. Brentuximag vedotin was approved in 2011, and in January 2012, the drug label was revised to include a boxed warning of progressive multifocal leukoencephalopathy and death following JC virus infection. Brentuximab vedotin is composed of 3 parts: a chimeric human-murine IgG1 that targets CD30, monomethyl auristatin E (MMAE),which is a microtubule disrupting agent, and a protease-susceptible linker that covalently links the antibody and MMAE. The IgG1 antibody enables brentuximab vedotin to target tumor cells expressing CD30 on their cell surface then brentuximab vedotin gets internalized into the cell. Once inside, the linker is cleaved releasing MMAE which binds disrupts the microtuble network.
Dược Động Học :
▧ Absorption :
Brentuximab vedotin is administered only as an intravenous infusion so absorption is 100%.
▧ Volume of Distribution :
The steady state volume of distribution is 6-10 L.
▧ Protein binding :
MMAE has a plasma protein binding range of 68-82%, and highly-protein bound drugs are not likely to displace it.
▧ Metabolism :
Only a small fraction of MMAE is metabolized primarily via oxidation by CYP3A4 and CYP3A5.
▧ Route of Elimination :
MMAE is eliminated by the feces (with 72% unchanged) and urine.
▧ Half Life :
The terminal half-life is 4-6 days.
▧ Clearance :
MMAE is cleared by the liver but not quantitative studies have been performed.
Độc Tính : The most severe toxic reaction seen in patients is progressive multifocal leukoencephalopathy. Other toxicities include bone marrow suppression, infusion reactions, peripheral neuropathy, Stevens-Johnson syndrome, and tumor lysis syndrome.
Chỉ Định : Used in the treatment of Hodgkin lymphoma and systemic anaplastic large cell lymphoma.
Tương Tác Thuốc :
  • Bleomycin Pulmonary toxicity of bleomycin may be increased. Avoid combination.
  • Etravirine Brentuximab, when used concomitantly with etravirine, may experience a decrease in serum concentrations. The levels of an active metabolite of brentuximab, monomethyl auristatin E, may decrease. It is recommended to monitor efficacy of brentuximab therapy.
  • Natalizumab Avoid combination due to the increased risk of concurrent infection.
  • Pimecrolimus Avoid combination due to the potential enhancement of toxic effects of immunosuppressants
  • Tacrolimus Avoid combination due to the potential enhancement of toxic effects of immunosuppressants.
Liều Lượng & Cách Dùng : Injection, powder, for solution - Intravenous - 1.8 mg/kg (maximum dose: 180 mg) every 3 weeks
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08870
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D09587
Wikipedia
http://en.wikipedia.org/wiki/Brentuximab_vedotin
RxList
http://www.rxlist.com/adcetris-drug.htm
Drugs.com
http://www.drugs.com/mtm/brentuximab-vedotin.html
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