Hirudins: From Leeches to Man

Wallis, Robert B.

doi:10.1055/s-2007-999007

Cited by 56 publications

(36 citation statements)

References 70 publications

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“…Hirudin was the first direct thrombin inhibitor to come into common use after its isolation from the salivary glands of the medicinal leech, Hirudo medicinalis. 15 However, concerns about its immunogenicity led to the development of additional direct thrombin inhibitors, including bivalirudin. On the basis of landmark clinical trials in patients with acute coronary syndromes, 16,17 bivalirudin has been licensed as an alternative to UFH in patients undergoing percutaneous coronary intervention for both ST-elevation myocardial infarction and non-ST-elevation myocardial infarction/unstable angina.…”

Section: Parenteral Anticoagulantsmentioning

confidence: 99%

Most Important Outcomes Research Papers on Anticoagulation for Cardiovascular Disease

Bikdeli¹,

Gupta²,

Mody³

et al. 2012

Circ: Cardiovascular Quality and Outcomes

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The following are highlights from the new series, Circulation: Cardiovascular Quality and Outcomes Topic Review. This series will summarize the most important manuscripts, as selected by the Editor, that have been published in the Circulation portfolio. The objective of this new series is to provide our readership with a timely, comprehensive selection of important papers that are relevant to the quality and outcomes, and general cardiology audience. The studies included in this article represent the most significant research in the area of anticoagulation for cardiovascular disease. (Circ Cardiovasc Qual and Outcomes. 2012;5:e65-e74.) T hrombosis is the leading cause of acute coronary syndromes, stroke, and venous thromboembolism.1 Accordingly, anticoagulants have been successfully used in each of these settings. 2,3Since the discovery of unfractionated heparin in the early 1900s, the number of anticoagulant choices has increased at an accelerating rate. For treatment of acute coronary syndromes, these include low-molecular weight heparins, fondaparinux, as well as direct thrombin inhibitors such as bivalirudin. 4 While warfarin and other vitamin K antagonists have long been the dominant oral anticoagulants, novel oral agents such as dabigatran, rivaroxaban, and apixaban have expanded the number of therapeutic options. 5All of these agents have potential pros and cons. For example, unfractionated heparin is relatively inexpensive and easily monitored. However, it may increase bleeding compared with direct thrombin inhibitors such as bivalirudin. Analogously, for patients with atrial fibrillation, warfarin is inexpensive and has a long track record of preventing thromboembolic events; however, it is subject to multiple potential food and drug interactions and requires close monitoring to maintain optimal time in therapeutic range. In contrast, the novel oral anticoagulants have been shown to be noninferior compared with warfarin for stroke prevention in atrial fibrillation without the need for intensive monitoring.6-8 Use of these new agents was also associated with significantly fewer intracranial bleeds and a trend toward reduced mortality that reached statistical significance for apixaban. 8 However, these new options may entail considerable expense, have no currently available antidote, and lack information on long-term efficacy and safety. In the Randomized Evaluation of Long-Term Anticoagulation Therapy (RE-LY) trial, concerns were raised about an increased risk of myocardial infarction in patients taking dabigatran compared with warfarin; this risk was further supported in a subsequent meta-analysis. 9Given the increasing scope of anticoagulant therapy and the introduction of multiple novel agents in recent years with unique efficacy and safety profiles, we have chosen to dedicate this series of Circulation: Cardiovascular Quality and Outcomes clinical summaries to the topic of therapeutic anticoagulation. We have included articles on topics such as the efficacy, safety, and costeffectiveness of bivali...

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Section: Parenteral Anticoagulantsmentioning

confidence: 99%

Most Important Outcomes Research Papers on Anticoagulation for Cardiovascular Disease

Bikdeli¹,

Gupta²,

Mody³

et al. 2012

Circ: Cardiovascular Quality and Outcomes

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show abstract

“…58 Binding is essentially irreversible. The plasma half-life of hirudin is 60 minutes after intravenous injection and 120 minutes after subcutaneous injection.…”

Section: Hirudinmentioning

confidence: 99%

New anticoagulants

Hirsh

O’Donnell

Weitz

2005

Blood

156

100

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“…Hirudin is a directly acting thrombin inhibitor that was originally isolated from the salivary glands of the medical leech Hirudo medicinalis and is now available in recombinant form [1]. Hirudin is a 65-amino acid polypeptide that binds and inhibits thrombin in a bivalent fashion.…”

Section: Bivalirudin: a 'Designer' Hirudinmentioning

confidence: 99%

Developmental Strategies of Novel Anticoagulants*

Pötzsch¹,

Müller²,

Rox³

2006

Transfus Med Hemother

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This minireview discusses developmental approaches of novel anticoagulants. The technology of drug design has been successfully used to modify established anticoagulants in a way that the pharmacological activity and safety is improved. This is exemplified on the development of bivalirudin, a hirudin derivative, and of idraparinux, a synthetic heparin derived from fondaparinux. A second approach includes characterization of human or nonhuman anticoagulant proteins and their subsequent production using recombinant technologies. As an example the nematode anticoagulant protein NAPc2 that was originally isolated from the canine hookworm Ancylostoma caninum is discussed. Finally, the development of aptamers that inhibit activated factor IX is discussed. This example indicates that employment of a novel technology can extend the anticoagulant armamentarium.

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Hirudins: From Leeches to Man

Cited by 56 publications

References 70 publications

Most Important Outcomes Research Papers on Anticoagulation for Cardiovascular Disease

Most Important Outcomes Research Papers on Anticoagulation for Cardiovascular Disease

New anticoagulants

Developmental Strategies of Novel Anticoagulants*

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