Direct Xa inhibitor
Direct factor Xa inhibitors are being used clinically. Clinical trials have shown promise for these compounds as substitutes for the currently administered vitamin K antagonists or low molecular weight heparin. Advantages of orally administered direct Xa inhibitors lie in the fact that they have a predictable effect, do not require frequent monitoring or re-dosing, are given through the mouth and not by injection and have few (known) drug interactions. Disadvantages include the currently limited prospective experience and lack of specific antidotes (although research in that field is ongoing, andexanet alfa being a candidate antidote).
A naturally occurring inhibitor of factor Xa was first reported in 1987. Tuszynski et al. discovered antistasin, which was isolated from the extracts of Mexican leech, Haementeria officinalis. Soon after this, another naturally occurring inhibitor, tick anticoagulant peptide (TAP) was isolated from the extract of tick Ornithodoros moubata.
- "Medscape.com". Retrieved 2009-01-23.
- Turpie AG (June 2007). "Oral, direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases". Arterioscler. Thromb. Vasc. Biol. 27 (6): 1238–47. doi:10.1161/ATVBAHA.107.139402. PMID 17379841.
- Cohen M, Bhatt DL, Alexander JH, et al. (May 2007). "Randomized, double-blind, dose-ranging study of otamixaban, a novel, parenteral, short-acting direct factor Xa inhibitor, in percutaneous coronary intervention: the SEPIA-PCI trial". Circulation 115 (20): 2642–51. doi:10.1161/CIRCULATIONAHA.106.653428. PMID 17502577.
- Paccaly A, Ozoux ML, Chu V, et al. (December 2005). "Pharmacodynamic markers in the early clinical assessment of otamixaban, a direct factor Xa inhibitor". Thromb. Haemost. 94 (6): 1156–63. doi:10.1160/TH05-05-0347. PMID 16411387.
- Eriksson BI, Borris LC, Dahl OE, et al. (November 2006). "A once-daily, oral, direct Factor Xa inhibitor, rivaroxaban (BAY 59-7939), for thromboprophylaxis after total hip replacement". Circulation 114 (22): 2374–81. doi:10.1161/CIRCULATIONAHA.106.642074. PMID 17116766.
- Direct Factor Xa Inhibitors as Anticoagulants | PharmaXChange.info – A review and presentation on the available factor Xa inhibitors which can be used as anticoagulants.
- Oral Xa inhibitors – Literature review of the evidence regarding oral Xa inhibitors
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