andexanet alfa   

GtoPdb Ligand ID: 7576

Synonyms: Andexxa® | coagulation factor Xa (recombinant), inactivated-zhzo | Ondexxya® | PRT064445 | PRT4445 | r-antidote
andexanet alfa is an approved drug (FDA (2018), EMA (2019))
Comment: Andexanet alfa is a recombinant modified human Factor Xa (FXa) protein that acts as a mimetic of endogenous human factor Xa, and which was developed as a universal antidote to reverse thhe anticoagulant effects of direct or indirect FXa inhibitors. Information regarding the invention of andexanet alfa is available in patent WO2009042962 [2].
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Bioactivity Comments
In enzyme assays using purified human plasma factor Xa, andexanet alfa reverses the inhibitory activity of betrixaban, rivaroxaban and apixaban inhibition on factor Xa activity with KDs of 0.53, 1.53 and 0.58nM respectively [1]
Selectivity at ligand targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
apixaban Hs Inhibitor Binding 9.2 pKd - 1
pKd 9.2 (Kd 5.8x10-10 M) [1]
Description: Enzyme assays using purified human plasma fXa, inhibited by apixaban.
rivaroxaban Hs Inhibitor Binding 8.8 pKd - 1
pKd 8.8 (Kd 1.53x10-9 M) [1]
Description: Enzyme assays using purified human plasma fXa, inhibited by rivaroxaban.