SR123781A: A New Once-Daily Synthetic Oligosaccharide Anticoagulant for Thromboprophylaxis After Total Hip Replacement Surgery

Lassen, Michael R.; Dahl, Ola E.; Mismetti, Patrick; Zielske, D.; Turpie, Alexander G.G.

doi:10.1016/j.jacc.2008.03.007

Cited by 15 publications

(7 citation statements)

References 20 publications

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“…The hexadecasaccharide was also used in crystal structural studies of the ternary complex of AT-thrombin (factor IIa)-heparin to understand the mechanism of action of the heparin-mediated deactivation of IIa (29,30). Unfortunately, the hexadecasaccharide reportedly failed in a recent clinical trial due to excessive bleeding effects (31).…”

Section: Discussionmentioning

confidence: 99%

Chemoenzymatic Synthesis of Heparin Oligosaccharides with both Anti-factor Xa and Anti-factor IIa Activities

Pempe

Liu

2012

Journal of Biological Chemistry

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Background: Heparin inhibits the activity of factors Xa and IIa in the blood coagulation cascade. Results: A series of size-defined N-sulfated oligosaccharides were synthesized to probe the size requirement for the oligosaccharides displaying anti-IIa activity. Conclusion: Oligosaccharides that display anti-IIa activity are longer than 19 saccharide residues. Significance: The results will direct efforts to prepare synthetic heparin with both anti-Xa and anti-IIa activities.

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Section: Discussionmentioning

confidence: 99%

Chemoenzymatic Synthesis of Heparin Oligosaccharides with both Anti-factor Xa and Anti-factor IIa Activities

Pempe

Liu

2012

Journal of Biological Chemistry

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“…98 SR123781A reduced the rate of VTE in a dose-dependent fashion and the rates of VTE with the 2.0-and 4.0-mg doses (7.0% and 4.4%, respectively) were similar to that with enoxaparin (8.7%). Major bleeding occurred in 0.6% and 5.8% of patients given the 2.0-and 4.0-mg doses of SR123781A, respectively, and in 0.6% of those given enoxaparin.…”

Section: Factor Xa Inhibitorsmentioning

confidence: 74%

New Antithrombotic Drugs

Weitz

Eikelboom

Samama

2012

Chest

280

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“…This heparin mimetic reached phase II-III clinical trials in the prevention of venous thromboembolism (VTE) and in acute coronary syndrome. [32] …”

Section: Longer Oligosaccharidesmentioning

confidence: 99%

Rational Design of Anticoagulant Drugs Using Oligosaccharide Chemistry

Hadri¹,

Petitou²

2011

Chimia

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For a long time, heparin and low molecular weight heparins have been the drugs of choice for the management of thrombosis. Discovery of the antithrombin binding domain in heparin, a critical element in the anticoagulant activity of this polysaccharide, allowed a rational approach based on medicinal carbohydrate chemistry in the design of new anticoagulants. The fully synthetic pentasaccharide fondaparinux that selectively targets blood coagulation factor Xa was first to be developed as a drug. Fondaparinux was followed by various heparin mimicking oligosaccharides prepared with a view to replace polydisperse heparin and low molecular weight heparins by structurally-defined anticoagulants with no unwanted side-effects.

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SR123781A: A New Once-Daily Synthetic Oligosaccharide Anticoagulant for Thromboprophylaxis After Total Hip Replacement Surgery

Abstract: The model based on these dose-finding study results suggests that SR123781A doses ranging from 1.5 to 2.5 mg show a reasonable risk-to-benefit ratio for VTE prevention after major orthopedic surgery.

Cited by 15 publications

References 20 publications

Chemoenzymatic Synthesis of Heparin Oligosaccharides with both Anti-factor Xa and Anti-factor IIa Activities

Chemoenzymatic Synthesis of Heparin Oligosaccharides with both Anti-factor Xa and Anti-factor IIa Activities

New Antithrombotic Drugs

Rational Design of Anticoagulant Drugs Using Oligosaccharide Chemistry

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