Perzborn, Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl) phenyl]-1,3-oxazolidin-5-yl} methyl) thiophene-2-carboxamide (BAY 59-7939): an oral, direct
factor Xa inhibitor.
Rivaroxaban is an oxazolidinone derivative that inhibits
factor Xa and interrupts both the extrinsic and intrinsic coagulation pathways, thereby inhibiting thrombin formation.
In conclusion, our data demonstrate similar mortality and neurological outcomes and no venous thromboembolic events for patients with
factor Xa inhibitor- and VKA-associated ICH treated with 4F-PCC.
Subsequently, there has been fast-tracking for FDA approval of another 2 candidate medications for reversal of
factor Xa inhibitors, andexanet-a and ciraparantag, and the latter can also reverse the anticoagulant effects of unfractionated heparin and lowmolecular weight heparin, in addition to that of the
factor Xa inhibitors (Table 2).
Another DOAC,
factor Xa inhibitor, did not increase the concentration of free hemoglobin in either brain compartment, but there was a trend in increased free hemoglobin in the cerebellum (Figure 2).
Patients received 3 days of
factor Xa inhibition and then, again using randomization, received either intravenous andexanet alfa or placebo.
The guidelines advise clinicians to evaluate renal function prior to starting any direct thrombin or
factor Xa inhibitors, and to reevaluate at least annually and when clinically indicated.
Rivaroxaban, apixaban and edoxaban are very specific antagonists of activated
factor Xa, which directly converts prothrombin to thrombin, thus leading to clot formation.
Rivaroxaban is an oral, direct
Factor Xa inhibitor that has been developed in recent years.
It is also employed during extracorporeal circulation (vascular surgery and hemodialysis), exhibiting anticoagulant action mainly through potentiation of AT, a serine protease inhibitor (serpin) which controls the coagulation process, especially thrombin and
factor Xa (NADER et al., 2001; QUINSEY et al., 2004).
Fondaparinux, an indirect
factor Xa inhibitor (via antithrombin), can be used instead of LMWHs, such as enoxaparin.