Asundexian (BAY2433334) is a reversible inhibitor of the active site of Factor XIa. Asundexian inhibits the activity of FXIa by directly, efficiently, and reversibly binding to its active site. the IC50 of human FXIa in Asundexian inhibition buffer is 1 nM.
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Ashkan Shoamanesh, et al. Lancet. Factor XIa inhibition with asundexian after acute non-cardioembolic ischaemic stroke (PACIFIC-Stroke): an international, randomised, double-blind, placebo-controlled, phase 2b trial
 Sunil V Rao, et al. Circulation. A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction
 Jonathan P Piccini, et al. Lancet. Safety of the oral factor XIa inhibitor asundexian compared with apixaban in patients with atrial fibrillation (PACIFIC-AF): a multicentre, randomised, double-blind, double-dummy, dose-finding phase 2 study
|Related Factor Xa Products|
5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects.
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
FXIa-IN-1 (compound EP-7041) is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.
FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases (Ki = 0.3 nM).
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