Bivalirudin is a DTI that overcomes many limitations seen with indirect thrombin inhibitors. It is a short, synthetic peptide that is potent, highly specific, and a reversible inhibitor of thrombin. Bivalirudin inhibits both circulating and clot-bound thrombin, while also inhibiting thrombin-mediated platelet activation and aggregation. It has a quick onset of action and a short half-life, without binding to plasma proteins (other than thrombin) or red blood cells. Therefore it has a predictable antithrombotic response.
CAT No: 10-101-06
CAS No:128270-60-0 (net)
Synonyms/Alias:BG 8967; Hirulog; Hirulog I; Bivalirudin; Angiomax; Hirulog-1; Hirulog1; Hirulog 1; BG8967; BG 8967; BG-8967; LS-172701; LS172701; LS 172701
Chemical Name:2-[[2-[[2-[[2-[[1-[(2S)-2-[[2-[[2-[[2-[[2-[[2-[[4-amino-2-[[2-[[2-[[2-[[2-[[1-[2-[[1-(2-amino-3-phenylpropanoyl)pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]-4-oxobutanoyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoic acid
Bivalirudin Trifluoroacetate is a synthetic peptide-based anticoagulant compound recognized for its direct thrombin inhibitory activity and unique structural design. Featuring a sequence that enables reversible binding to both the catalytic and anion-binding exosites of thrombin, this molecule offers precise modulation of thrombin activity. Its trifluoroacetate salt form enhances stability and solubility, making it suitable for a variety of research and development settings. Due to its peptide nature, Bivalirudin Trifluoroacetate exhibits high specificity and minimal cross-reactivity, making it a valuable tool in scientific studies focused on coagulation pathways and enzyme kinetics. The compound is widely utilized in preclinical research, pharmaceutical development, and biotechnological innovation, where accurate control of thrombin activity is essential.
Anticoagulation Research: Bivalirudin Trifluoroacetate is extensively employed in laboratory investigations focusing on the mechanisms of blood coagulation and thrombosis. By directly inhibiting thrombin, it enables researchers to dissect the roles of various coagulation factors without the confounding effects of indirect anticoagulants. It serves as a critical reagent in studies that require precise modulation of clot formation, such as in vitro clotting assays, platelet aggregation tests, and the development of new anticoagulant strategies. Its reversible binding properties allow for controlled experimentation, facilitating the exploration of thrombin's involvement in both physiological and pathological processes.
Enzyme Kinetics and Inhibitor Profiling: The compound is a preferred tool in enzyme kinetics studies aimed at elucidating the catalytic mechanisms of serine proteases, particularly thrombin. Researchers utilize it to determine inhibition constants, binding affinities, and the structural basis of enzyme-inhibitor interactions. Its well-characterized mode of action makes it an ideal reference inhibitor in comparative studies, supporting the discovery and optimization of novel thrombin inhibitors. The molecule's specificity also allows for the assessment of selectivity and off-target effects in the development of new therapeutic agents.
Pharmaceutical Formulation Development: Bivalirudin Trifluoroacetate plays a crucial role in the early stages of pharmaceutical formulation research. Scientists leverage its stability and solubility profile to evaluate delivery systems, optimize peptide formulations, and assess compatibility with excipients. It is often incorporated into in vitro release studies and stability testing protocols to predict performance in complex biological environments. This application direction supports the advancement of peptide-based drug delivery technologies and the refinement of formulation strategies for improved therapeutic efficacy.
Biomaterial and Device Coating Studies: The direct thrombin inhibitory activity of this compound makes it valuable in the development of biomaterials and medical device coatings designed to minimize thrombogenicity. Researchers incorporate it into surface modification protocols for stents, catheters, and vascular grafts to evaluate antithrombotic performance in simulated blood flow conditions. The peptide's ability to prevent fibrin deposition and platelet activation is instrumental in the screening and optimization of next-generation biocompatible coatings, supporting innovation in cardiovascular and surgical device engineering.
Diagnostic and Analytical Method Development: Bivalirudin Trifluoroacetate is utilized in the creation and validation of diagnostic assays that require selective inhibition of thrombin activity. It is incorporated into protocols for calibrating coagulation analyzers, developing reference standards, and establishing quality control procedures for laboratory diagnostics. The compound's reproducible effects on thrombin-mediated reactions enable the generation of reliable data in analytical workflows, contributing to the accuracy and consistency of diagnostic platforms used in research and development laboratories.
In summary, Bivalirudin Trifluoroacetate demonstrates exceptional versatility and scientific value across a spectrum of research domains. Its application in anticoagulation research, enzyme kinetics, pharmaceutical formulation, biomaterial innovation, and diagnostic assay development underscores its importance as a specialized tool for advancing our understanding of thrombin biology and supporting the creation of novel biomedical solutions. As a direct thrombin inhibitor with well-defined properties, it continues to facilitate progress in both fundamental research and applied bioscience, driving innovation in anticoagulant strategies, therapeutic development, and analytical technology.
Growing data demonstrate procedural success with bivalirudin in patients with HIT undergoing cardiovascular surgery. However, bivalirudin dosing and goal-activated clotting times varied between the studies and case reports. Bivalirudin represents a viable alternative to heparin in patients with HIT undergoing cardiovascular surgery; however, further trials are warranted to identify optimal dosing and monitoring parameters.
Czosnowski Q A, Finks S W, Rogers K C. Bivalirudin for patients with heparin-induced thrombocytopenia undergoing cardiovascular surgery[J]. Annals of Pharmacotherapy, 2008, 42(9): 1304-1309.
Among the current agents in the class of direct thrombin inhibitors, bivalirudin has seen increased use in cardiovascular medicine over the past decade through its primary indication as an anticoagulant used during percutaneous coronary interventions. Bivalirudin has been further investigated and used as the anticoagulation strategy in the setting of cardiac and endovascular surgical procedures and is frequently utilized in the management of patients with heparin-induced thrombocytopenia. In comparison with heparin, bivalirudin exhibits a low immunogenic profile and provides similar or reduced major bleeding rates as well as a predictable degree of anticoagulation that is dose related. Bivalirudin primarily undergoes dual elimination via proteolytic cleavage and renal elimination, and requires dose adjustment in the setting of severe renal dysfunction. Given the body of supportive data, bivalirudin is likely to continue to figure prominently as a reliable and efficient anticoagulation strategy. Additional agents in the class of direct thrombin inhibitors are under investigation and may find increasing clinical use.
Van De Car D A, Rao S V, Ohman E M. Bivalirudin: a review of the pharmacology and clinical application[J]. Expert review of cardiovascular therapy, 2010, 8(12): 1673-1681.
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