Tìm theo
Tenecteplase
Các tên gọi khác (4 ) :
  • t- PA
  • t-plasminogen activator
  • Tissue-type plasminogen activator precursor
  • tPA
fibrinolytic agents, thrombolytic agents
Thuốc Gốc
Biotech
CAS: 191588-94-0
ATC: B01AD11
ĐG : F Hoffmann-La Roche Ltd. , http://www.roche.com
CTHH: C2561H3919N747O781S40
PTK: 58951.2000
Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C2561H3919N747O781S40
Phân tử khối
58951.2000
Độ tan chảy
60 °C
Độ kỵ nước
-0.528
Điểm đẳng điện tích
7.61
Dược Lực Học : Tenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Cơ Chế Tác Dụng : Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain. Tenecteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
Dược Động Học :

▧ Half Life :
1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)
▧ Clearance :
* 99 - 119 mL/min [acute myocardial infarction patients]
Chỉ Định : For treatment of myocardial infarction and lysis of intracoronary emboli
Tương Tác Thuốc :
  • Aprotinin Aprotonin may antagonize the effect of Tenecteplase. Monitor for decreased effects of Tenecteplase.
  • Drotrecogin alfa Increased risk of bleeding.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Ginseng Increased risk of bleeding.
  • Ticlopidine Increased bleeding risk. Monitor for signs of bleeding.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Tnkase 50 mg kit
    Giá bán buôn : USD >3238.76
    Đơn vị tính : kit
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00031
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06070
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50242-038-61
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/L00153
PharmGKB
http://www.pharmgkb.org/drug/PA164776757
Wikipedia
http://en.wikipedia.org/wiki/Tenecteplase
RxList
http://www.rxlist.com/cgi/generic2/tenecteplase.htm
Drugs.com
http://www.drugs.com/mtm/tenecteplase.html
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