Tìm theo
Axitinib
Các tên gọi khác (1) :
  • SID103905539
Thuốc Gốc
Small Molecule
CAS: 319460-85-0
ATC: L01XE17
Axitinib is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. Axitinib is marketed under the name Inlyta®, and if one previous systemic therapy for kidney cell cancer has failed, axitinib is indicated.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ hòa tan
In aqueous media with a pH between 1.1 to 7.8, axitinib has a solubility of over 0.2 μg/mL.
pKa
4.8
Dược Lực Học : Axitinib prevents the progression of cancer by inhibiting angiogenesis and blocking tumor growth.
Cơ Chế Tác Dụng : Axitinib is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. Axitinib is marketed under the name Inlyta®, and if one previous systemic therapy for kidney cell cancer has failed, axitinib is indicated. Axitinib selectively blocks the tyrosine kinase receptors VEGFR-1 (vascular endothelial growth factor receptor), VEGFR-2, and VEGFR-3.
Dược Động Học :
▧ Absorption :
After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.
▧ Volume of Distribution :
The volume of distribution is 160 L.
▧ Protein binding :
Plasma protein binding for axitinib is high at over 99% with most protein binding to albumin followed by α1-acid glycoprotein.
▧ Metabolism :
Axitinib undergoes mainly hepatic metabolism. CYP3A4 and CYP3A5 are the main hepatic enzymes while CYP1A2, CYP2C19, and UGT1A1 enzymes are secondary.
▧ Route of Elimination :
Axitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.
▧ Half Life :
Axitinib has a half life of 2.5 to 6.1 hours.
▧ Clearance :
The average clearance of axitinib is 38 L/h.
Độc Tính : Some of the more serious toxic effects seen in patients taking axitinib include, but are not limited to, hypertension, thrombotic events, hemorrhage, and GI perforation.
Chỉ Định : Used in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer.
Tương Tác Thuốc :
  • Clobazam Clobazam decreases levels by affecting CYP3A4 metabolism. Consider alternate therapy.
  • Etravirine Axitinib, when administered concomitantly with etravirine, may experience a decrease in serum concentrations. Recommended to avoid use of this combination.
  • Paclitaxel Avoid combination due to potential for decrease in serum concentration of axitinib.
  • Perampanel Avoid combination with axitinib or other major CYP3A4 drug susbtrates due to the potential decrease in the drug's concentration by perampanel induction of CYP3A4.
  • Phenytoin Avoid combination with phenytoin and other strong, moderate, or weak CYP3A4 inducers due to the likely decreased levels of axitinib.
  • St. John's Wort Avoid combination due to the likely decreased levels of axitinib.
Liều Lượng & Cách Dùng : Tablet - Oral - 1 MG
Tablet - Oral - 5 MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Pfizer
    Sản phẩm biệt dược : Inlyta
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06626
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03218
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0069-0145-01
PharmGKB
http://www.pharmgkb.org/drug/PA164924493
Wikipedia
http://en.wikipedia.org/wiki/Axitinib
RxList
http://www.rxlist.com/inlyta-drug.htm
Drugs.com
http://www.drugs.com/mtm/axitinib.html
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