A synthetic small molecule antidote for anticoagulants

Bakhru, Sasha; Laulicht, Bryan; Jiang, Xuan; Chen, L.; Grosso, Michael; Morishima, Yasuo; Brown, Karen; Masumoto, Hiroshi; Costin, James; Steiner, Solomon S.

doi:10.1093/eurheartj/eht308.1078

Cited by 13 publications

(2 citation statements)

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“…21 PER977 is a synthetic molecule that can bind to multiple NOACs and has been shown to decrease bleeding in animals. 22 The safety and efficacy of this antidote in humans are currently under investigation. 21 Another slight inconvenience is that recommended apixaban treatment is BID, whereas other NOACs are taken once daily (rivaroxaban or edoxaban).…”

Section: Discussionmentioning

confidence: 99%

A Meta-Analysis of Randomized Controlled Trials of the Risk of Bleeding With Apixaban Versus Vitamin K Antagonists

Touma

Filion

Atallah

et al. 2015

The American Journal of Cardiology

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Section: Discussionmentioning

confidence: 99%

A Meta-Analysis of Randomized Controlled Trials of the Risk of Bleeding With Apixaban Versus Vitamin K Antagonists

Touma

Filion

Atallah

et al. 2015

The American Journal of Cardiology

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“…These drugs were developed as hemostatic agents for bleeding and bleeding deficiencies, not as reversal agents for direct FXa inhibitors [98,99]. Additionally, the synthetic small-molecule PER977 (Perosphere, Danbury CT, USA) [100,101], PRT064445 (Andexanet alfa, Portola Pharmaceuticals, South San Francisco, CA, USA), a human recombinant FXa modified to be catalytically inactive [102], and the dabigatran-specific antibody fragment idarucizumab [103,104] are under investigation as reversal agents.…”

Section: Reversalmentioning

confidence: 99%

Target-specific oral anticoagulants and the hospitalist

Deitelzweig

Amin

2015

Hospital Practice

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As a class, the target-specific oral anticoagulants (TSOACs) are at least as effective as warfarin, often with superior safety for the prevention of stroke in patients with nonvalvular atrial fibrillation (AF) and the treatment of acute venous thromboembolism (VTE) and prevention of recurrent VTE. Currently, dabigatran, the direct thrombin inhibitor, along with rivaroxaban and apixaban, direct factor Xa inhibitors, has been approved in multiple countries for these indications. Edoxaban, which has received approval for the abovementioned indications in Japan, has demonstrated efficacy and safety comparable to or better than warfarin in Phase III clinical trials and is under further regulatory consideration. It is anticipated that the use of TSOACs will increase as practitioners and healthcare systems gain familiarity with these drugs and adopt their use into clinical practice. This review will provide a brief overview of the TSOAC Phase III clinical trials for prevention of stroke and systemic embolic events in patients with AF and the Phase III clinical trials for the prevention of recurrent VTE, discuss current treatment guidelines, address how TSOACs may help meet national safety goals, and provide clinical decision-making guidance regarding the use of TSOACs for hospitalists.

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Approaches to prevent bleeding associated with anticoagulants: current status and recent developments

Kalathottukaren

Haynes

Kizhakkedathu

2017

Drug Deliv. and Transl. Res.

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Anticoagulants are widely used for the prophylaxis and treatment of cardiovascular disorders and to prevent blood clotting during surgeries. However, the major limitation associated with anticoagulant therapy is bleeding; all the current anticoagulants do have a bleeding risk. The propensity to bleed is much higher among the elderly population and patients with renal insufficiency. Therefore, there is an utmost and urgent clinical need for a highly efficient, nontoxic antidote with excellent anticoagulant reversal activity. This will significantly improve the safety of anticoagulation therapy. This review summarizes the current options and approaches to reverse anticoagulation activity of clinically used anticoagulants. We start with an introduction to thrombosis and then summarize the details of current clinically available anticoagulants and their mechanisms of action and limitations. This is followed by current practices in anticoagulant neutralization including the details of the only clinically approved unfractionated heparin antidote, protamine; recent advances in the development of antidotes against heparin-based drugs; and direct oral anticoagulants (DOACs).

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A synthetic small molecule antidote for anticoagulants

Cited by 13 publications

References 0 publications

A Meta-Analysis of Randomized Controlled Trials of the Risk of Bleeding With Apixaban Versus Vitamin K Antagonists

A Meta-Analysis of Randomized Controlled Trials of the Risk of Bleeding With Apixaban Versus Vitamin K Antagonists

Target-specific oral anticoagulants and the hospitalist

Approaches to prevent bleeding associated with anticoagulants: current status and recent developments

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