Tìm theo
Cabozantinib
Các tên gọi khác (9 ) :
  • BMS 907351
  • BMS907351
  • Cabozantinib (S)-malate
  • Cabozantinib L-malate
  • cabozantinib s-malate
  • Cometriq
  • XL 184
  • XL-184
  • XL184
Thuốc Gốc
Small Molecule
CAS: 849217-68-1
Cabozantinib was approved in 2012 and is a non-specific tyrosine kinase inhibitor. It is marketed as COMETRIQ™, which is indicated for the treatment of metastatic medullary thyroid cancer. It's label includes a black box warning of gastrointestinal perforations, fistulas, and hemorrhage.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ hòa tan
COMETRIQ is practically insoluble in water.
Dược Lực Học : Cabozantinib suppresses metastasis, angiogenesis, and oncognesis by inhibiting receptor tyrosine kinases.
Cơ Chế Tác Dụng : Cabozantinib was approved in 2012 and is a non-specific tyrosine kinase inhibitor. It is marketed as COMETRIQ™, which is indicated for the treatment of metastatic medullary thyroid cancer. It's label includes a black box warning of gastrointestinal perforations, fistulas, and hemorrhage. Cabozantinib inhibits specific receptor tyrosine kinases such as VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, RET, MET, and TIE-2.
Dược Động Học :
▧ Absorption :
After oral administration, peak plasma concentration was achieved in 2-5 hours.
▧ Volume of Distribution :
The volume of distribution is 349L.
▧ Protein binding :
Cabozantinib has extensive plasma protein binding (≥ 99.7%).
▧ Metabolism :
Cabozantinib is metabolized mostly by CYP3A4 and, to a minor extent, by CYP2C9. Both enzyme produce an N-oxide metabolite.
▧ Route of Elimination :
Cabozantinib is eliminated mostly by the feces (54%) and also by the urine (27%).
▧ Half Life :
Cabozantinib has a long half-life of 55 hours.
▧ Clearance :
At steady state, the clearance is 4.4 L/hr.
Độc Tính : Cabozantinib has a black box warning of serious gastrointestinal fistulas and perforations, and potentially fatal hemoptysis and gastrointestinal hemorrhage.
Chỉ Định : For the treatment of metastatic medullary thyroid cancer.
Tương Tác Thuốc :
  • Etravirine Cabozantinib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid this combination if alternative are available. If concurrent use is not avoidable, it is recommended to increase the dosage of cabozantinib by 40mg (without exceeding 180mg/day).
  • St. John's Wort Avoid combination. May decrease concentration of cabozantinib. Also avoid all other strong CYP3A4 inducers.
Liều Lượng & Cách Dùng : Capsule - Oral - EQ 20MG BASE
Capsule - Oral - EQ 80MG BASE
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : EXELIXIS
    Sản phẩm biệt dược : COMETRIQ
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08875
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D10062
Wikipedia
http://en.wikipedia.org/wiki/Cabozantinib
RxList
http://www.rxlist.com/cometriq-drug.htm
Drugs.com
http://www.drugs.com/mtm/cabozantinib.html
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