Factor Xa inhibitors, direct

General information

The direct inhibitors of factor Xa are short polysaccharides [ ]. They include rivaroxaban [BAY 59-7939; 5-chloro-N-(({(5S)-2-oxo-3-(4-(3-oxomorpholin-4-yl)phenyl)-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide)], apixaban, edoxaban, otamixaban, and DX-9065 [(+)-2S-2-[4-[[(3S)-1-acetimidoyl-3-pyrrolidinyl]oxy]phenyl]-3-(7-amidino-2-naphthyl) propanoic acid hydrochloride pentahydrate].

Direct inhibitors of factor Xa bind to factor Xa with 1:1 stoichiometry and block the interaction of factor Xa with its substrates. Their action is reversible and they not only inhibit free factor Xa but also inactivate factor Xa bound to platelets within the prothrombinase complex.

The indirect factor Xa inhibitors fondaparinux and idraparinux are covered in a separate monograph.