Factor Xa inhibitors binds Xa

Stable Identifier
R-HSA-9015111
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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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). Rivaroxaban (brand name Xarelto) was the first medically approved drug of this class (Abrams & Emerson 2009, Misselwitz et al. 2011). Rivaroxaban binds to and inhibits both free factor Xa and factor Xa bound in the prothrombinase complex (Roehrig et al. 2005). 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
25855704 Edoxaban, a Novel Oral Factor Xa Inhibitor

Minor, C, Tellor, KB, Armbruster, AL

Ann Pharmacother 2015
23683607 Efficacy and toxicity of factor Xa inhibitors

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

J Pharm Pharm Sci 2013
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

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

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

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

J. Med. Chem. 2005
Participants
Participant Of
Disease
Name Identifier Synonyms
pulmonary embolism 9477 pulmonary embolus, pulmonary artery embolism
Authored
Reviewed
Created