Dabigatran Etexilate (free base)
N-[2-[4-[N-(Hexyloxycarbonyl)amidino]phenylaminomethyl]-1-methyl-1H-benzimidazol-5-ylcarbonyl]-N-(2-pyridyl)-beta-alanine ethyl ester
CAS: 211915-06-9
Molecular Formula: C34H41N7O5
Dabigatran Etexilate (free base) - Names and Identifiers
Dabigatran Etexilate (free base) - Physico-chemical Properties
| Molecular Formula | C34H41N7O5 |
| Molar Mass | 627.73 |
| Density | 1.24±0.1 g/cm3(Predicted) |
| Melting Point | 128-129° |
| Boling Point | 827.9°C at 760 mmHg |
| Flash Point | 454.5°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Vapor Presure | 1.49E-27mmHg at 25°C |
| Appearance | Solid |
| Color | White to Pale Yellow |
| pKa | 9.88±0.46(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Stability | Hygroscopic |
| Refractive Index | 1.614 |
| In vitro study | Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) and thrombin-induced platelet aggregation (IC50: 10 nM) and has no inhibitory effect on other platelet stimulating agents. Dabigatran inhibits the generation of (PPP) thrombin in the plasma of depleted platelets with an IC50 of 0.56 μm as measured by the endogenous thrombin Index (ETP). In in vitro experiments, Dabigatran has a concentration-dependent anticoagulant effect on various species. In human PPP, the activated partial thromboplastin time (aPTT), prothrombin time (PT) were doubled at concentrations of 0.23,0.83 and 0.18 μm, respectively. And Ecarin clotting time (ECT).. |
| In vivo study | Dabigatran dose-dependently prolonged aPPT after intravenous administration in rats (0.3,1 and 3 mg/kg) and rhesus monkeys (0.15,0.3 and 0.6 mg/kg). Dabigatran etexilate (20 mg/kg, P. O.) produced less prolongation of the k value and less attenuation of the maximum increase in pigs than enoxaparin. Dabigatran(0.01-0.1 mg/kg) dose-dependently reduced thrombosis, with ED50 (50% effective dose) being 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibited thrombus formation in a dose-and time-dependent manner, with maximal inhibition occurring after 30 min of pretreatment, indicating a faster acting effect. |
Dabigatran Etexilate (free base) - Reference Information
| oral anticoagulant | everyone must know that warfarin is currently the main drug for preventing stroke and systemic embolism in patients with atrial fibrillation, and it is used in anticoagulant therapy for patients with atrial fibrillation. Warfarin has always been regarded as the gold standard for antithrombotic therapy in this field. However, in clinical practice, warfarin has been found to interact with many drugs and diet, such as quinolone and macrolide antibiotics, which often cannot guarantee that its dose is always maintained in the treatment window and increases the risk of bleeding. In order to ensure the safety of medication, it is necessary to routinely monitor the coagulation function and adjust the dosage. dabigatran etexilate is another new oral anticoagulant approved by the U.S. Food and Drug Administration after warfarin. It is a non-peptide thrombin inhibitor that specifically and selectively blocks thrombin (free or bound) The activity exerts the anticoagulant effect. It has the characteristics of oral administration, strong effect, no need for special drug monitoring, and less drug interaction. It is a major progress in the field of anticoagulant therapy and potentially fatal thrombosis prevention, and is a milestone. After oral administration and gastrointestinal absorption, it is converted into dabigatran with direct anticoagulant activity in the body. Through the fibrin-specific binding site bound to thrombin, fibrinogen is prevented from cleaving into fibrin, thereby blocking The final step of the clotting waterfall network and thrombosis. Dabugatran can also be dissociated from the fibrin-thrombin conjugate to play a reversible anticoagulant effect. At the 2009 annual meeting of the European Society of Cardiology, Boehringer Ingelheim, Germany, announced for the first time the largest clinical trial of atrial fibrillation outcomes to date-RE-LY (a new direct thrombin inhibitor dabigatran etexilate long-term anticoagulant therapy Randomized evaluation) research data. The results showed that compared with the well-controlled warfarin treatment group, dabigatran etexilate significantly reduced the risk of stroke and embolic diseases (including hemorrhagic stroke), significantly reduced the incidence of hemorrhage (including fatal hemorrhage and intracranial hemorrhage), and significantly reduced vascular mortality. The results also show that dabigatran etexilate provides an effective and stable anticoagulant effect without routine monitoring of coagulation function and dosage adjustment. |
| clinical application and risk assessment | in April 2008, EMA first approved the indication of dabigatetexilate as thrombosis prevention after hip and knee arthroplasty. in April 2008, dabigatran etexilate was first listed in Germany and Britain, and then approved to be listed in more than 40 countries and widely used in primary prevention of deep vein thrombosis in patients after elective total hip/knee arthroplasty. In October 2010, the FDA of the US Food and Drug Administration officially approved the sale of dabigatran etexilate for the prevention of stroke caused by atrial fibrillation (AF). AF is one of the most common arrhythmia, with an incidence rate of 1% in all age groups and 10% in people over 80 years old. It is found in almost all organic heart diseases, and can also occur in non-organic heart diseases. The medical community generally believes that there are great market opportunities and broad prospects for the prevention of stroke caused by atrial fibrillation (AF). on November 2, 2012, FDA released information indicating that new information has been evaluated for the possible risk of serious bleeding using anticoagulants (blood thinner) dabigatran etexilate (Pradaxa) and warfarin. This risk assessment uses FDA Sentinel Action (Sentinel Initiative) Mini-Sentinel Monitoring System's medical insurance compensation and management data. The results of this evaluation showed that the bleeding rate associated with the new use of dabigatran etexilate was not higher than that associated with the new use of warfarin, which is consistent with the large-scale clinical trials (RE-LY trials) on which the approval of dabigatran etexilate was based. FDA's safety investigation on this issue is still ongoing and is continuing to evaluate data from multiple sources. in March 2013, the latest review published by the U.S. food and drug administration (FDA) in the new england journal of medicine pointed out that after the small-scale sentinel assessment conducted in November 2012, FDA, as the drug regulatory department, did not change its target for taibiquan.®(Dabidatetexilate) recommendations made. FDA pointed out that it has not observed any relationship with the recent use of Taibiquan.®The incidence of related bleeding events is higher than that associated with the recent use of warfarin, which is RE-LY to the core study.®The results observed in are consistent. In May 2013, the new oral anticoagulant Taibiquan produced by Boehringer Ingelheim Company in Germany®China has been issued by the State Food and Drug Administration of China's import drug registration certificate, will soon be listed in China. |
| pharmacological effects | dabidogatran etexilate is the most advanced new generation of oral anticoagulant direct thrombin inhibitors (DTIs), aiming at the urgent clinical needs of prevention and treatment of acute and chronic thromboembolic diseases. Direct thrombin inhibitors play a strong anticoagulant effect by specifically blocking the activity of thrombin (free type and binding type). Thrombin is a central enzyme in the process of thrombosis. Unlike vitamin K antagonists that act on different coagulation factors, dabigatran etexilate can provide effective, predictable, and stable anticoagulant effects, and at the same time, there is less drug interaction, no drug food interaction, and no Routine coagulation function monitoring or dose adjustment. The clinical use experience of dabicatran etexilate has surpassed all other new oral anticoagulants. The drug has been used for various registered indications in more than 80 countries worldwide for more than 1.4 million patient years. |
| safety | since renal impairment is a risk factor for bleeding in dabigatran etexilate, all patients should evaluate renal function before starting treatment to rule out severe renal impairment; during treatment, if there is suspected clinical situation of renal dysfunction, renal function should be reviewed routinely; elderly patients (>75 years old) or patients with moderate renal impairment, renal function should be reviewed at least once a year; dabigatran etexilate should not be used for hemodynamically obvious rheumatic heart valve disease (especially Mitral valve stenosis) patients and patients with artificial heart valves. Dabigatran etexilate Bleeding Risk and Renal Function Assessment: The content of the product monograph has been updated based on reports of severe bleeding events after the listing of dabigatran etexilate and the use of elderly patients and patients at high risk of bleeding or patients with renal impairment. The current updated content includes that it is recommended to evaluate renal function in patients who are considering or have been treated with dabigatran etexilate. The specific content is as follows: Before starting treatment with dabigatran etexilate, all patients must calculate Creatinine clearance rate (CrCl) to evaluate renal function to rule out severe renal function damage (ie CrCl<30 ml/min); during dabigatran etexilate treatment, if there is a clinical suspicion of rapid decline or rapid deterioration of renal function (such as hypovolemia, dehydration, and simultaneous use of certain drugs), renal function should be reviewed. These clinical conditions may lead to increased exposure to dabigatran etexilate; elderly (>75 years old) patients or patients with moderate renal impairment (CrCl30 -50 ml/min) should evaluate renal function by calculating creatinine clearance at least once a year. Advice to medical professionals: dabigatran etexilate is contraindicated in patients with severe renal impairment (CrCl<30 ml/min); patients at high risk of bleeding should not use dabigatran etexilate; clinical monitoring of patients, Pay attention to whether there is bleeding or anemia; if severe bleeding occurs, dabigatran etexilate should be discontinued and the bleeding site should be identified. Recommendations for patients with heart valve disease: The safety and efficacy of dabigatran etexilate has not been studied in patients with hemodynamically significant rheumatic heart valve disease (especially mitral stenosis) or patients with artificial heart valves. There is no data to support the adequate anticoagulant effect of dabigatran etexilate in patients fitted with prosthetic heart valves, with or without atrial fibrillation, so dabigatran etexilate is not suitable for patients with hemodynamically significant rheumatic heart valve disease manifestations or patients with prosthetic heart valves. |
| biological activity | Dabigatran Etexilate (BIBR-1048) is a dabigatran prodrug, dabigatran an effective, non-peptide small molecule compound, which can specifically and reversibly inhibit free and blood clot-bound thrombin. |
| Target | Value |
| Use | Dabidogatran etexilate is a new type of synthetic direct thrombin inhibitor, a dabigatran prodrug, and a non-peptide thrombin inhibitor. After oral administration and gastrointestinal absorption, it is converted into dabigatran with direct anticoagulant activity in vivo. dabigatran the fibrin-specific binding site bound to thrombin prevents fibrinogen from cleaving into fibrin, thus blocking the final step of the clotting waterfall network and thrombosis. dabigatran can be dissociated from fibrin-thrombin conjugate and exert reversible anticoagulant effect |
Last Update：2024-04-10 22:29:15
Supplier List
Spot supply
Product Name: Dabigatran Etexilate Visit Supplier Webpage Request for quotationCAS: 211915-06-9
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: N-[2-[4-[N-(Hexyloxycarbonyl)amidino]phenylaminomethyl]-1-methyl-1H-benzimidazol-5-ylcarbonyl]-N-(2-pyridyl)-beta-alanine ethyl ester Request for quotation
CAS: 211915-06-9
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 211915-06-9
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Multiple SpecificationsSpot supply
Product Name: Dabigatran etexilate Visit Supplier Webpage Request for quotationCAS: 211915-06-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Dabigatran Etexilate Visit Supplier Webpage Request for quotationCAS: 211915-06-9
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: N-[2-[4-[N-(Hexyloxycarbonyl)amidino]phenylaminomethyl]-1-methyl-1H-benzimidazol-5-ylcarbonyl]-N-(2-pyridyl)-beta-alanine ethyl ester Request for quotation
CAS: 211915-06-9
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
CAS: 211915-06-9
Tel: 0086-551-65418684
Email: sales@tnjchem.com
info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Multiple SpecificationsSpot supply
Product Name: Dabigatran etexilate Visit Supplier Webpage Request for quotationCAS: 211915-06-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History