apixaban has been researched along with Venous-Thrombosis* in 3 studies
3 other study(ies) available for apixaban and Venous-Thrombosis
| Article | Year |
|---|---|
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity.
A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant potency, and compounds 15b, 15c, 20b, 20c, and 22b were further examined for their inhibitory activity against human FXa in vitro. While compounds 15c and 22b were tested for rat venous thrombosis in vivo. The most promising compound 15c, with an IC Topics: Animals; Anticoagulants; Binding Sites; Blood Coagulation; Catalytic Domain; Drug Design; Factor Xa; Factor Xa Inhibitors; Humans; Molecular Docking Simulation; Protein Binding; Pyrazoles; Pyridines; Rabbits; Rats; Structure-Activity Relationship; Venous Thrombosis | 2017 |
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.
Four series of novel and potent FXa inhibitors possessing the 1,2,4-triazole moiety and pyrrole moiety as P2 binding element and dihydroimidazole/tetrahydropyrimidine groups as P4 binding element were designed, synthesized, and evaluated for their anticoagulant activity in human and rabbit plasma in vitro. Most compounds showed moderate to excellent activity. Compounds 14a, 16, 18c, 26c, 35a, and 35b were further examined for their inhibition activity against human FXa in vitro and rat venous thrombosis in vivo. The most promising compound 14a, with an IC Topics: Animals; Binding Sites; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; Factor Xa; Factor Xa Inhibitors; Humans; Models, Molecular; Molecular Structure; Pyrazoles; Pyridones; Pyrroles; Rabbits; Rats; Structure-Activity Relationship; Triazoles; Venous Thrombosis | 2016 |
Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies.
Apixaban is an oral, direct and highly selective factor Xa (FXa) inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases.. We evaluated the in vitro properties of apixaban and its in vivo activities in rabbit models of thrombosis and hemostasis.. Studies were conducted in arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT), electrically mediated carotid arterial thrombosis (ECAT) and cuticle bleeding time (BT) models.. In vitro, apixaban is potent and selective, with a K(i) of 0.08 nm for human FXa. It exhibited species difference in FXa inhibition [FXa K(i) (nm): 0.16, rabbit; 1.3, rat; 1.7, dog] and anticoagulation [EC(2x) (microm, concentration required to double the prothrombin time): 3.6, human; 2.3, rabbit; 7.9, rat; 6.7, dog]. Apixaban at 10 microm did not alter human and rabbit platelet aggregation to ADP, gamma-thrombin, and collagen. In vivo, the values for antithrombotic ED(50) (dose that reduced thrombus weight or increased blood flow by 50% of the control) in AVST, VT and ECAT and the values for BT ED(3x) (dose that increased BT by 3-fold) were 0.27 +/- 0.03, 0.11 +/- 0.03, 0.07 +/- 0.02 and > 3 mg kg(-1) h(-1) i.v. for apixaban, 0.05 +/- 0.01, 0.05 +/- 0.01, 0.27 +/- 0.08 and > 3 mg kg(-1) h(-1) i.v. for the indirect FXa inhibitor fondaparinux, and 0.53 +/- 0.04, 0.27 +/- 0.01, 0.08 +/- 0.01 and 0.70 +/- 0.07 mg kg(-1) day(-1) p.o. for the oral anticoagulant warfarin, respectively.. In summary, apixaban was effective in the prevention of experimental thrombosis at doses that preserve hemostasis in rabbits. Topics: Animals; Carotid Artery Thrombosis; Disease Models, Animal; Dogs; Factor Xa Inhibitors; Hemostasis; Humans; Platelet Aggregation; Pyrazoles; Pyridones; Rabbits; Rats; Thrombosis; Venous Thrombosis | 2008 |