Reactome | Factor Xa inhibitors binds Xa

Factor Xa inhibitors binds Xa

Stable Identifier

R-HSA-9015111

Type

Reaction [binding]

Species

Homo sapiens

Compartment

extracellular region, plasma membrane

ReviewStatus

5/5

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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
23683607	Efficacy and toxicity of factor Xa inhibitors Bondarenko, M, Curti, C, Montana, M, Rathelot, P, Vanelle, P	J Pharm Pharm Sci	2013
25855704	Edoxaban, a Novel Oral Factor Xa Inhibitor Minor, C, Tellor, KB, Armbruster, AL	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 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