Factor Xa

Abelacimab (MAA868), a fully human IgG1 monoclonal antibody that binds to and blocks the activation of FXI, is an anticoagulant used in the study of thromboembolic diseases.

EMD-503982 is a potential Factor Xa and Factor VIIa inhibitor with potential anticancer and antitumor activity for the study of thromboembolic and neurological disorders.

Apixaban (BMS-562247-01) is an orally active anticoagulant that inhibits coagulation factor Xa, directly preventing the conversion of prothrombin to thrombin and the formation of cross-linked fibrin clots.

Heparin sodium is a sulfated polysaccharide, which belongs to the family of glycosaminoglycans. It is utilized as an anticoagulant and interacted with diverse proteins for numerous important biological activities.Heparin sodium salt (Sodium heparinate) significantly inhibits exosome-cell interactions.

Asundexian (BAY-2433334) is a potent and orally active inhibitor of the coagulation factor FXIa that directly and reversibly binds to the active site of FXIa, thereby inhibiting its activity.Asundexian has an IC50 of 1 nM for human FXIa in buffer.Asundexian has antitumor activity and may be useful in studies of Acute ischemic stroke, transient ischemic attack and ischemic stroke.

Garadacimab (CSL312) is a potent whole-human IgG4 monoclonal antibody targeting activation factor XII (FXIIa). Garadacimab can be used to study hereditary angioedema.

Rivaroxaban (BAY 59-7939) is an orally bioavailable oxazolidinone derivative and a direct inhibitor of coagulation factor Xa with anticoagulant activity. Upon administration, it selectively binds to both free factor Xa and factor Xa within the prothrombinase complex, interfering with the conversion of prothrombin (factor II) to thrombin and preventing cross-linked fibrin clot formation. Rivaroxaban does not affect existing thrombin levels.

Denecimig (Mim8) is a bispecific and humanized IgG4κ antibody mimicking activated coagulation factor VIII with anti-FIXa and anti-FX arms, which is used for the treatment of hemophilia A and coagulation disorders primarily by facilitating the assembly of activated coagulation factors IXa (FIXa) and X (FX) on platelet membranes, stimulating activation of FX, and arresting bleeding.

Fondaparinux sodium (SR-90107A) is an antithrombin-dependent factor Xa inhibitor with antithrombotic activity.

Zifaxaban (TY-602) is an orally active, competitive and selective inhibitor of factor Xa (FXa) with an IC50 of 11.1 nM for human FXa.Zifaxaban has a very high affinity, more than 10,000-fold higher than that of other serine proteases.Zifaxaban can be used to study arterial and venous thrombosis.

Enoxaparin sodium is a low-molecular-weight heparin (LMWH) that has recently been approved by the US FDA for use in patients with medically managed ST-segment myocardial infarction (STEMI), or STEMI with subsequent percutaneous coronary intervention (PCI)

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE [2]. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients [4].

LY 517717 is an orally active inhibitor of coagulation factor Xa with antithrombotic activity for the study of venous thromboembolism (VTE).

Otamixaban (FXV673) is a selective and highly effective Xa inhibitor that inhibits the generation of thrombin and can be used to study acute coronary syndrome.

Bismuth subgallate (Dermatol Puder) is an astringent and antiseptic and is applied to skin diseases such as eczema.

Letaxaban (TAK-442) is a small molecule Xa factor inhibitor that can be used to study polar coronary syndromes and thrombotic blockages.

Osocimab (BAY 1213790) is a potent anti-FXIa antibody with a Ki value of 2.4 nM and an EC50 value of 0.2 nM.Osocimab may reduce thrombosis through FXI inhibition.Osocimab is often used as an XI factor inhibitor, has an inhibitory effect on thrombin generation, has an anticoagulant effect, and is used in the study of thromboembolic diseases. Thromboembolic Diseases

Edoxaban (Lixiana) (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with K i s of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and is able to be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K i s of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3].

Darexaban (Tanexaban, YM-150) is a direct inhibitor of Factor Xa.Darexaban and Darexaban glucuronide selectively and competitively inhibit FXA and inhibit prothrombin activity at the site of blood clot (thrombus) formation. This leads to a reduction in blood clot formation in a dose-dependent manner. Reducing clotting will reduce blockages in blood flow, which may reduce the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.

Gabexate mesylate (FOY) is a serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

Coumarin is a chemical compound/poison found in many plants, notably in high concentration in the tonka bean, woodruff, and bison grass. It has clinical value as the precursor for several anticoagulants, notably warfarin.

Eribaxaban (PD348292) is an orally available factor Xa inhibitor for the prevention and treatment of venous thromboembolism.

Naroparcil, an orally available thioglycoside analog of 4-methylumbelliferyl β-D-xyloside, showed antithrombotic effects in the Wessler sludge model of venous thrombosis (jugular vein).Naroparcil enhanced the formation of the thrombin heparin cofactor II complex, induced dermatophyte sulfate-like substances in plasma from treated rabbits appearance, but reduced the formation of thrombin antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin.