Direct thrombin inhibitor Bivalirudin

Use as an anticoagulant in patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA) Bivalirudin

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Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure.

For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.

Bivalirudin mediates an inhibitory action on thrombin by directly and specifically binding to both the catalytic site and anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.

Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.

Bivalirudin Structural Formula:

Diseases and fields of Bivalirudin

Product	Status	Indication of dosage form	Market
Bivalirudin	Commercial	Use as an anticoagulant in patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA)	Overseas Domestic

Specifications

Synthesis mode	chemic synthesis，solid phase synthesis
Categories	APIsPeptides; Biopharmaceuticals
Sales markets	Western Europe; Asia; North America; Central/South America
Supplied from	China
Selling Points	International Approvals/Standards

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