Factor Xa inhibitors bind Va:Xa

Stable Identifier
Reaction [binding]
Homo sapiens
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Factor Xa (aka Factor X heavy chain), a cleavage product of coagulation factor X (F10), is a vitamin K-dependent glycoprotein able to convert prothrombin to thrombin during the blood clotting process. Factor Xa is a target for direct oral anticoagulant (DOAC) drugs that are direct factor Xa inhibitors (the so-called 'xabans') which are used in the treatment and prevention of thromboembolic disorders (Galanis et al. 2014, Nutescu et al. 2016). Rivaroxaban (brand name Xarelto) binds to and inhibits both free factor Xa and factor Xa bound in the prothrombinase complex (Va:Xa) (Roehrig et al. 2005). Rivaroxaban was the first medically approved drug of this class (Abrams & Emerson 2009, Misselwitz et al. 2011). Other 'xabans' such as apixaban (Bhanwra & Ahluwalia 2014), edoxaban (Minor et al. 2015), eribaxaban (Bondarenko et al. 2013) and betrixaban (Zhang et al. 2009) share a similar mechanism of action to rivaroxaban (Nutescu et al. 2016).
Literature References
PubMed ID Title Journal Year
23683607 Efficacy and toxicity of factor Xa inhibitors

Montana, M, Rathelot, P, Vanelle, P, Bondarenko, M, Curti, C

J Pharm Pharm Sci 2013
25855704 Edoxaban, a Novel Oral Factor Xa Inhibitor

Armbruster, AL, Minor, C, Tellor, KB

Ann Pharmacother 2015
19297154 Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor

Su, T, Bauer, SM, Li, W, Lambing, JL, Woolfrey, J, Scarborough, RM, Wu, Y, Arfsten, AE, Huang, W, Park, G, Fan, J, Kanter, J, Hutchaleelaha, A, Goldman, EA, Probst, GD, Hollenbach, SJ, Zhang, P, Jia, ZJ, Edwards, ST, Clizbe, LA, Bao, L, Zhu, BY, Pandey, A, Song, Y, Sinha, U, Wong, PW, Wang, L

Bioorg. Med. Chem. Lett. 2009
24554904 The new factor Xa inhibitor: Apixaban

Bhanwra, S, Ahluwalia, K

J Pharmacol Pharmacother 2014
16161994 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

Lampe, T, Straub, A, Roehrig, S, Reinemer, P, Pohlmann, J, Perzborn, E, Schlemmer, KH, Pernerstorfer, J

J. Med. Chem. 2005
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