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Merck
  • Moving toward a more ideal anticoagulant: the oral direct thrombin and factor Xa inhibitors.

Moving toward a more ideal anticoagulant: the oral direct thrombin and factor Xa inhibitors.

Chest (2013-04-03)
Christopher S King, Aaron B Holley, Lisa K Moores
摘要

Thromboembolic diseases are common. Heparins and the vitamin K antagonists have been the mainstay of therapy for > 60 years, but both classes of agents have limitations. The "ideal" anticoagulant should be as effective and safe as heparin and vitamin K antagonists but should also be available in both a parenteral and an oral formulation, have predictable pharmacokinetics, and lack significant toxicities unrelated to the anticoagulant activity. Moreover, it should target a specific coagulation factor and have an antidote that leads to rapid reversal. There are now agents that fulfill some of these criteria. Here we review the pharmacology and effectiveness of the oral activated factor X inhibitors rivaroxaban and apixaban and the oral direct thrombin inhibitor dabigatran. These agents have undergone extensive phase 3 testing and are currently approved for various indications in the United States, Canada, or Europe. Rivaroxaban is approved in the United States for VTE prevention after major orthopedic surgery and for stroke prevention in atrial fibrillation and is approved in Europe and Canada for secondary prevention of VTE. Apixaban is currently under review by the US Food and Drug Administration for stroke prevention and is approved in Europe for VTE prevention following major orthopedic surgery. Dabigatran is approved in the United States for stroke prevention in nonvalvular atrial fibrillation and is being reviewed for secondary prevention of VTE.

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Sigma-Aldrich
Thrombin 来源于人类血浆, lyophilized powder, ≥2,000 NIH units/mg protein (E1%/280, 18.3)
Sigma-Aldrich
凝血酶 来源于牛血浆, lyophilized powder, 40-300 NIH units/mg protein (biuret)
Sigma-Aldrich
Thrombin 来源于人类血浆, lyophilized powder, ≥1,000 NIH units/mg protein (E1%/280, 18.3)
Sigma-Aldrich
凝血酶 来源于牛血浆, lyophilized powder, 600-2,000 NIH units/mg protein (biuret)
Sigma-Aldrich
凝血酶 来源于牛血浆, lyophilized powder, ≥2,000 NIH units/mg protein (E1%/280 = 19.5)
Sigma-Aldrich
凝血酶 来源于牛血浆, ≥60 NIH units/mg protein (biuret)
Sigma-Aldrich
因子X活化(Xa) 来源于牛血浆, aqueous glycerol solution
Sigma-Aldrich
Thrombin 来源于人类血浆, lyophilized powder, Suitable for routine use in the thrombin time test
Sigma-Aldrich
Thrombin 来源于人类血浆, lyophilized powder, 1500-3500 NIH units/mg protein (E1%/280, 18.3), suitable for cell culture
Sigma-Aldrich
凝血酶 人, BioUltra, recombinant, expressed in HEK 293 cells, aqueous solution, ≥95% (SDS-PAGE)
Sigma-Aldrich
Thrombin 来源于人类血浆, lyophilized powder, ≥2800 NIH units/mg protein (E1%/280, 18.3)
Sigma-Aldrich
Thrombin 来源于人类血浆, 400-1000 NIH units/mg protein