Discovery and development of direct Xa inhibitors information
Four drugs from the class of direct Xa inhibitors are marketed worldwide. Rivaroxaban (Xarelto) was the first approved FXa inhibitor to become commercially available in Europe and Canada in 2008.[1] The second one was apixaban (Eliquis), approved in Europe in 2011[2] and in the United States in 2012.[3] The third one edoxaban (Lixiana, Savaysa) was approved in Japan in 2011 and in Europe and the US in 2015.[4] Betrixaban (Bevyxxa) was approved in the US in 2017.
^Bhanwra, Sangeeta; Ahluwalia, Kaza (2014-01-01). "The new factor Xa inhibitor: Apixaban". Journal of Pharmacology and Pharmacotherapeutics. 5 (1): 12–4. doi:10.4103/0976-500x.124409. PMC 3917159. PMID 24554904.
^Chan, Lewey; Pisano, Michele (2016-10-03). "Edoxaban (Savaysa): A Factor Xa Inhibitor". Pharmacy and Therapeutics. 40 (10): 651–95. ISSN 1052-1372. PMC 4606855. PMID 26535021.
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factor Xainhibitors, or even dual thrombin and fXainhibitors that have a broader mechanism of action by both inhibiting factor IIa (thrombin) andXa. A...
selective direct factor Xainhibitor with an onset of action of 2.5 to 4 hours. Inhibition of Factor Xa interrupts the intrinsic and extrinsic pathway of the...
heparin and related compounds increase the action of antithrombin on thrombin and factor Xa. A newer class of drugs, the direct thrombin inhibitors, is under...
affinity of antithrombin to thrombin (as well as factor Xa). The direct thrombin inhibitors, a newer class of medication, directly inhibit thrombin by...
free form. These direct factor Xainhibitors can be administered orally, as can dabigatran etexilate, which is a direct thrombin inhibitor. Fondaparinux...
Darexaban (YM150) is a directinhibitorof factor Xa created by Astellas Pharma. It is an experimental drug that acts as an anticoagulant and antithrombotic to...
Otamixaban (INN) is an experimental injectable anticoagulant direct factor Xainhibitor that was investigated for the treatment for acute coronary syndrome...
Several other direct thrombin inhibitors are derived chemically from hirudin. Hirudotherapy Discoveryanddevelopmentofdirect thrombin inhibitors PDB: 4HTC...
(LMWHs) and fondaparinux as anticoagulants. Fondaparinux targets anti-factor Xa activity rather than inhibiting thrombin activity, with the aim of facilitating...
S also binds to Factor Xa, inhibiting the latter from diminishing APC's inactivation of Factor Va.: 2386 The inactivation of Factor VIIIa is not as well...
molecule inhibitorof Factor Xa, a key enzyme involved in blood coagulation. In the United States, the FDA has approved rivaroxaban for the prevention of stroke...
cancer cell potential for invasion and metastasis and with progression of the malignancy. Some sialylation inhibitors can make cancer cells less malignant...
The binding of the heparan sulfate in this pentasaccharide to AT-III inactivates the blood-coagulation factors thrombin and Factor Xa. Heparan sulfates...
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