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Bivalirudin

Anticoagulants Dosage Adverse reactions and precautions Clinical evaluation Uses
Bivalirudin
Bivalirudin structure
CAS No.
128270-60-0
Chemical Name:
Bivalirudin
Synonyms
BIVALIRUDIN;Bivalirudinum;BITTERMELONP.E;Bivalirudin, TFA;Human Bivalirudin;Bivalirudin Acetate;Bivalirudin Trifluoacetate;BG 8967, Hirulog, Hirulog I;BIVALIRUDIN TRIFLUOROACETATE;Hirulog trifluoroacetate salt
CBNumber:
CB9471951
Molecular Formula:
C98H138N24O33
Formula Weight:
2180.29
MOL File:
128270-60-0.mol

Bivalirudin Properties

storage temp. 
?20°C
form 
powder
color 
white to off-white

SAFETY

WGK Germany  3

Bivalirudin price More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1051 Bivalirudin trifluoroacetate salt ≥97% (HPLC) 128270-60-0 10mg $79.8 2018-11-13 Buy
Sigma-Aldrich SML1051 Bivalirudin trifluoroacetate salt ≥97% (HPLC) 128270-60-0 50mg $324 2018-11-13 Buy
Cayman Chemical 23035 Bivalirudin ≥98% 128270-60-0 5mg $49 2018-11-19 Buy
Cayman Chemical 23035 Bivalirudin ≥98% 128270-60-0 10mg $74 2018-11-19 Buy
Cayman Chemical 23035 Bivalirudin ≥98% 128270-60-0 25mg $172 2018-11-19 Buy

Bivalirudin Chemical Properties,Uses,Production

Anticoagulants

Bivalirudin is a kind of synthetic novel anticoagulants. It is the direct, specific and reversible inhibitor of thrombin. It was developed by the Swiss Basset (Biogen) originally. Then it was transferred to the United States Medicines Company, and approved for marketing in the United States in 2000. Its anticoagulant ingredient is a kind of 20 peptides derived from hirudin. Bivalirudin can specifically bind with catalytic site and the anion binding site of whether thrombin that is in the blood circulation or thrombus-bound thrombin, thus directly inhibiting thrombin activity. And its role is characterized by short, reversible. Early clinical studies show that the anticoagulation treatment of bivalirudin is good. And the incidence of bleeding events is low. So its use is safer than traditional heparin therapy. It is mainly used for the prevention of angioplasty interventional treatment of ischemic complications of unstable angina pectoris before and after.
Bivalirudin has a inhibitory effect on soluble and thrombus-bound thrombin in vitro. That effect cannot be affected by products that are released by platelet, and it can extend plasma activated partial thromboplastin time, thrombin time and prothrombin time of normal human with a dose-dependent manner. It is suitable for percutaneous coronary intervention (PCI) unstable angina. In 2010, domestic PCI operation cases reached 300,000. The annual compound growth rate was over 30%. This showed that sales prospects of bivalirudin after the listing are considerable.
Clinically experiments prove that bivalirudin is more effective than the current mainstream unfractionated heparin/low molecular weight heparin and platelet glycoprotein receptor antagonist in applications around PCI. Especially the risk of bleeding has a significant reduction, and the use safety of anticoagulants is greatly improved:
1. It can significantly reduce the incidence of bleeding in elective PCI patients. The total clinical outcome risk fell 14%.
2. It does not cause antibody-mediated thrombocytopenia.
3. Reversibly bind with thrombin. Short half-life. Hard to develop ischemic and hemorrhagic complications.
4. It is not mainly excreted through the kidneys and can be safely used in patients with renal impairment.
The above information is edited by the chemicalbook of Duan Yalan.

Dosage

The first dose 0.75 mg/kg is injected intravenously. Then it is continuously injected intravenously with 1.75 mg/kg per hour by percutaneous coronary intervention. ACT should be monitored after first intravenous injection for 5 minutes. If necessary, 0.3mg/kg bivalirudin is injected again. After percutaneous coronary intervention treatment, it is continued to use for 4h. If necessary, 0.2 mg/kg bivalirudin per hour is continuously injected for 20h. When it is used, using 5mL water for injection to dissolve, and then using 50 mL normal saline to be diluted to 5mg/mL solution.

Adverse reactions and precautions

1. To guard against the occurrence of bleeding, including intracranial hemorrhage, thrombocytopenia. Intravenously injection should stop immediately when a sudden drop in blood pressure and blood volume.
2. Back pain, headaches, insomnia, anxiety, abdominal pain, diarrhea, nausea, vomiting, low blood pressure can be seen. When serious bivalirudin should be discontinued. Patients with renal dysfunction should reduce its dosage.
3. Patients allergic to bivalirudin and active bleeding should be banned. Women, infants, breast-feeding women should be careful to use this product.
4. Bivalirudin cannot bind with plasma proteins and red blood cells. When bivalirudin is used with heparin, warfarin, or thrombolytic drugs, it will increase the possibility of bleeding of patients. Once the excessive use, it should be discontinued. The product can be cleared by hemodialysis.

Clinical evaluation

In order to prove the efficacy and safety of bivalirudin in the treatment of patients with acute coronary syndrome (ACS), the researchers designed the ACUITY clinical research.
ACUITY clinical trial was to compare the efficacy and safety of bivalirudin with traditional heparin platelet glycoprotein Ⅱb/Ⅲa inhibitor therapy in high-risk ACS patients. ACUITY results published in a recent issue of the "New England Journal of Medicine" showed that the efficacy of bivalirudin alone is same with traditional anticoagulant drugs. While preventing ischemic events, it can significantly reduce bleeding.
ACUITY trial chooses 13,819 patients from 17 countries with high-risk non-ST segment elevation acute coronary syndrome. Patients were randomly divided into three group: unfractionated heparin or low molecular weight heparin and glycoprotein Ⅱb/Ⅲa inhibitor combination group, bivalirudin and glycoprotein Ⅱb/Ⅲa inhibitor combination group and bivalirudin alone group. The primary endpoint is ischemic composite endpoint occurred in 30 days (death, myocardial infarction or unplanned revascularization due to ischemia), major bleeding events and overall clinical outcomes (the sum of ischemic or serious bleeding events). The results showed that compared with heparin and glycoprotein Ⅱb/Ⅲa inhibitor combination group, the incidence of ischemic events in bivalirudin alone group did not significantly increase (7.8% vs 7.3%;. P = 0.32 ). Bleeding risk decreased 47% (3.0% vs. 5.7%; P <0.001), and the overall clinical outcomes were also improved significantly (10.1% vs.11.7%; P = 0.015). Using bivalirudin alone is not inferior to the combination of heparin and glycoprotein Ⅲb/Ⅲa inhibito. In addition, the combinations of bivalirudin and glycoprotein Ⅱb/Ⅲa inhibitor are also not inferior to heparin and glycoprotein Ⅱb/Ⅲa inhibitors, but no advantage at all.
Stone, the study leader in Columbia University Medical Center Stone, believes that " for high-risk ACS patients with early intervention therapy, bivalirudin is a suitable alternative to heparin or enoxaparin when used with glycoprotein Ⅱb/Ⅲa inhibitors. Compared with the combinations of heparin and glycoprotein Ⅱb/Ⅲa inhibitors or the combinations of bivalirudin and glycoprotein Ⅱb/Ⅲa inhibitor, bivalirudin treatment can make patients to have a more significant net clinical benefit. And event-free survival in 30 days can be improved. "

Uses

Alternative medicine as ordinary heparin and platelet glycoprotein IIb/IIIa antagonists.

Description

Bivalirudin was launched in New Zealand as an anticoagulant for i.v. treatment of patients with unstable angina undergoing percutaneous transluminal coronary angioplasty. Bivalirubin is a synthetic 20 amino acid peptide rationally modeled on hirudin (residues 53- 64), the most potent and specific naturally-occuring known inhibitor of thrombin, the enzyme that plays a key role in hemostasis and blood clot formation. This peptide is a direct thrombin inhibitor that maintains the unique bivalent binding properties of hirudin to the catalytic site and to the fibrin-recognition exosite of the enzyme, so acting directly on thrombin with high affinity and specificity. In vitro studies demonstrated that alpha- and zeta-thrombins, both with the higher fibrinogen-procoagulant activities, were inhibited. In rats receiving high doses of bivalirudin, the platelet deposition in carotide was reduced by 63% compared to controls. The results of clinical studies, conducted only in patients receiving concomitant aspirin, suggested that the use of bivalirudin was more efficacious and more predictable than unfractionated heparin, with fewer bleeding complications. Despite some unresolved developmental issues, the attractive properties of this novel agent could make it a useful alternative to heparin in a variety of coagulation disorders.

Originator

Biogen (US)

Uses

Anticoagulant; antithrombotic.

Definition

ChEBI: A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva o the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.

brand name

Angiomax (Medicinova).

Bivalirudin Preparation Products And Raw materials

Raw materials

Preparation Products


Bivalirudin Suppliers

Global( 179)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22043 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Rixing Chemical CO.,LTD
13237129059
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ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 16534 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 1664 55
SUZHOU TIANMA PHARMA GROUP TIANJI BIO-PHARMACEUTICAL CO., LTD.
18315825527
kevin@tianmapharma.com CHINA 19 58
Chengdu Biopurify Phytochemicals Ltd.
18080483897
maggie@biopurify.com CHINA 2238 58
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 24118 58
Hubei Jusheng Technology Co.,Ltd.
86-188-71490254
peter@hubeijusheng.com CHINA 20229 58

View Lastest Price from Bivalirudin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-07-24 Bivalirudin
128270-60-0
US $50.00 / G 10KG 99% 10kg career henan chemical co

128270-60-0(Bivalirudin)Related Search:


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  • Bivalirudin, TFA
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  • BITTERMELONP.E
  • Human Bivalirudin
  • Bivalirudin Acetate
  • Bivalirudin BG 8967, Hirulog, Hirulog I
  • BG 8967, Hirulog, Hirulog I
  • Bivalirudin(Bivalirudin Trifluoroacetate)
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  • Bivalirudin trifluoroacetate salt
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  • Hirulog trifluoroacetate salt
  • Bivalirudin Trifluoacetate
  • Bivalirudinum
  • API
  • proteins
  • 128270-60-0
  • C98H138N24O33
  • Peptide
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