Details
Stereochemistry | ACHIRAL |
Molecular Formula | C34H41N7O5 |
Molecular Weight | 627.7332 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCCCOC(=O)NC(=N)C1=CC=C(NCC2=NC3=C(C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=NC=CC=C4)N2C)C=C1
InChI
InChIKey=KSGXQBZTULBEEQ-UHFFFAOYSA-N
InChI=1S/C34H41N7O5/c1-4-6-7-10-21-46-34(44)39-32(35)24-12-15-26(16-13-24)37-23-30-38-27-22-25(14-17-28(27)40(30)3)33(43)41(20-18-31(42)45-5-2)29-11-8-9-19-36-29/h8-9,11-17,19,22,37H,4-7,10,18,20-21,23H2,1-3H3,(H2,35,39,44)
Molecular Formula | C34H41N7O5 |
Molecular Weight | 627.7332 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022512s007lbl.pdf
https://www.pradaxa.com/
Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022512s007lbl.pdf
https://www.pradaxa.com/
Dabigatran ethyl ester is a one of the intermediate, which is formed during metabolic reactions from dabigatran etexilate. Dabigatran ethyl ester forming under the action of intestinal carboxylesterase 2 (CES2) further is hydrolyzed by CES1 with formation of active drug, thrombin inhibitor, dabigatranand. Dabigatran ethyl ester is a much stronger inhibitor of ribosyldihydronicotinamide dehydrogenase, than dabigatran.
CNS Activity
Sources: http://cardiobrief.org/2010/11/07/re-ly-substudy-finds-dabigatran-effective-in-secondary-stroke-prevention/
Curator's Comment: Dabigatran doesn’t cross the blood-brain barrier.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2265 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24212379 |
|||
Target ID: CHEMBL204 |
1.2 nM [IC50] | ||
Target ID: CHEMBL3959 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | PRADAXA Approved UsePRADAXA is a direct thrombin inhibitor indicated:
To reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (1.1)
For the treatment of deep venous thrombosis (DVT) and pulmonary embolism (PE) in patients who have been treated with a parenteral anticoagulant for 5-10 days (1.2)
To reduce the risk of recurrence of DVT and PE in patients who have been previously treated (1.3)
For the prophylaxis of DVT and PE in patients who have undergone hip replacement surgery Launch Date1.28735995E12 |
|||
Primary | PRADAXA Approved UsePRADAXA is a direct thrombin inhibitor indicated:
To reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (1.1)
For the treatment of deep venous thrombosis (DVT) and pulmonary embolism (PE) in patients who have been treated with a parenteral anticoagulant for 5-10 days (1.2)
To reduce the risk of recurrence of DVT and PE in patients who have been previously treated (1.3)
For the prophylaxis of DVT and PE in patients who have undergone hip replacement surgery Launch Date1.28735995E12 |
|||
Preventing | PRADAXA Approved UsePRADAXA is a direct thrombin inhibitor indicated:
To reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (1.1)
For the treatment of deep venous thrombosis (DVT) and pulmonary embolism (PE) in patients who have been treated with a parenteral anticoagulant for 5-10 days (1.2)
To reduce the risk of recurrence of DVT and PE in patients who have been previously treated (1.3)
For the prophylaxis of DVT and PE in patients who have undergone hip replacement surgery Launch Date1.28735995E12 |
|||
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
348 ng/mL |
150 mg 2 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DABIGATRAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2232 ng × h/mL |
150 mg 2 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DABIGATRAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11.3 h |
150 mg 2 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DABIGATRAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
65% |
150 mg 2 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DABIGATRAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
400 mg 3 times / day single, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: single Dose: 400 mg, 3 times / day Sources: Page: p.301 |
healthy, 18–45 n = 8 Health Status: healthy Age Group: 18–45 Sex: M Population Size: 8 Sources: Page: p.301 |
|
400 mg single, oral Highest studied dose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.301 |
healthy, 18–45 n = 6 Health Status: healthy Age Group: 18–45 Sex: M Population Size: 6 Sources: Page: p.301 |
|
150 mg 6 times / day multiple, oral Recommended Dose: 150 mg, 6 times / day Route: oral Route: multiple Dose: 150 mg, 6 times / day Sources: Page: p.605 |
healthy, 18–45 n = 14 Health Status: healthy Age Group: 18–45 Sex: M+F Population Size: 14 Sources: Page: p.605 |
Disc. AE: C-reactive protein increased, Alanine aminotransferase increase... AEs leading to discontinuation/dose reduction: C-reactive protein increased (7.14%) Sources: Page: p.605Alanine aminotransferase increase (7.14%) Haematuria (7.14%) Epistaxis (7.14%) Haemorrhoidal haemorrhage (7.14%) |
150 mg 2 times / day multiple, oral Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.5 |
unhealthy n = 6059 Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Population Size: 6059 Sources: Page: p.5 |
Disc. AE: Bleeding, Gastrointestinal disorder NOS... AEs leading to discontinuation/dose reduction: Bleeding Sources: Page: p.5Gastrointestinal disorder NOS |
150 mg 2 times / day multiple, oral Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.6 |
unhealthy n = 6059 Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Population Size: 6059 Sources: Page: p.6 |
Disc. AE: Bleeding... AEs leading to discontinuation/dose reduction: Bleeding (grade 5, 0.07%) Sources: Page: p.6 |
150 mg 2 times / day multiple, oral (max) Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Sources: Page: p.1 |
Disc. AE: Spinal epidural hematoma, Bleeding... AEs leading to discontinuation/dose reduction: Spinal epidural hematoma Sources: Page: p.1Bleeding (grade 3-5) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Alanine aminotransferase increase | 7.14% Disc. AE |
150 mg 6 times / day multiple, oral Recommended Dose: 150 mg, 6 times / day Route: oral Route: multiple Dose: 150 mg, 6 times / day Sources: Page: p.605 |
healthy, 18–45 n = 14 Health Status: healthy Age Group: 18–45 Sex: M+F Population Size: 14 Sources: Page: p.605 |
C-reactive protein increased | 7.14% Disc. AE |
150 mg 6 times / day multiple, oral Recommended Dose: 150 mg, 6 times / day Route: oral Route: multiple Dose: 150 mg, 6 times / day Sources: Page: p.605 |
healthy, 18–45 n = 14 Health Status: healthy Age Group: 18–45 Sex: M+F Population Size: 14 Sources: Page: p.605 |
Epistaxis | 7.14% Disc. AE |
150 mg 6 times / day multiple, oral Recommended Dose: 150 mg, 6 times / day Route: oral Route: multiple Dose: 150 mg, 6 times / day Sources: Page: p.605 |
healthy, 18–45 n = 14 Health Status: healthy Age Group: 18–45 Sex: M+F Population Size: 14 Sources: Page: p.605 |
Haematuria | 7.14% Disc. AE |
150 mg 6 times / day multiple, oral Recommended Dose: 150 mg, 6 times / day Route: oral Route: multiple Dose: 150 mg, 6 times / day Sources: Page: p.605 |
healthy, 18–45 n = 14 Health Status: healthy Age Group: 18–45 Sex: M+F Population Size: 14 Sources: Page: p.605 |
Haemorrhoidal haemorrhage | 7.14% Disc. AE |
150 mg 6 times / day multiple, oral Recommended Dose: 150 mg, 6 times / day Route: oral Route: multiple Dose: 150 mg, 6 times / day Sources: Page: p.605 |
healthy, 18–45 n = 14 Health Status: healthy Age Group: 18–45 Sex: M+F Population Size: 14 Sources: Page: p.605 |
Bleeding | Disc. AE | 150 mg 2 times / day multiple, oral Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.5 |
unhealthy n = 6059 Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Population Size: 6059 Sources: Page: p.5 |
Gastrointestinal disorder NOS | Disc. AE | 150 mg 2 times / day multiple, oral Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.5 |
unhealthy n = 6059 Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Population Size: 6059 Sources: Page: p.5 |
Bleeding | grade 5, 0.07% Disc. AE |
150 mg 2 times / day multiple, oral Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.6 |
unhealthy n = 6059 Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Population Size: 6059 Sources: Page: p.6 |
Spinal epidural hematoma | Disc. AE | 150 mg 2 times / day multiple, oral (max) Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Sources: Page: p.1 |
Bleeding | grade 3-5 Disc. AE |
150 mg 2 times / day multiple, oral (max) Recommended Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Non-valvular atrial fibrillation|deep venous thrombosis|pulmonary embolism Sources: Page: p.1 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: 68-69, (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no [IC50 >100 uM] | |||
Page: (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 110 |
no | |||
Page: (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 110 |
no | |||
Page: (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 110 |
no | |||
Page: 54-56, 56-57, (PMDA_A100_1 Japanese) 34, (PMDA_I100-_ Japanese) 68 |
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: (PMDA_A100_1 Japanese) 32, (PMDA_I100-_ Japanese) 33 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
no | |||
Page: (ClinPharm) 13, (PMDA_A100_1 Japanese) 32, 40-41, (PMDA_I100_1 Japanese) 33 |
no | no (co-administration study) Comment: Coadministration of Atorvastatin (CYP3A4 & P-gp inhibitor, 400 mg QD x 4 days) with Dabigatran metexilate mesylate (150 mg BID x 3 days and 150 mg QD on Day 4) decreased total Dabigatran AUCtau,ss by 58% and Cmax,ss by 50%., Coadministration of Clarithromycin (CYP3A4 & P-gp inhibitor, 500 mg BID x 5 days & 500 mg QD on Day 6) with Dabigatran metexilate mesylate (150 mg QD on Day 6) increased total Dabigatran AUCinf by 19% and Cmax by 15%., Coadministration of Rifampicin (CYP3A4 & P-gp inducer, 600 mg QD x 7 days in the night) with Dabigatran metexilate mesylate (150 mg QD on Day 8 morning) decreased total Dabigatran AUCinf by 67% and Cmax by 66%., Coadministration of Ketoconazole (CYP3A4 & P-gp inhibitor, 400mg QD ) with Dabigatran metexilate mesylate (150 mg QD) increased total Dabigatran AUCinf by 138% and Cmax by 135%. Page: (ClinPharm) 13, (PMDA_A100_1 Japanese) 32, 40-41, (PMDA_I100_1 Japanese) 33 |
||
Page: 54-55, 56-57, (ClinPharm) 12, 13, 33-36, (PMDA_A100_1 Japanese) 33, 39, 40-41, (PMDA_I100_1 Japanese) 66, (PMDA_K103_1 Japanese) 152-156 |
no | no (co-administration study) Comment: Caco-2 cells, Efflux ratio = 1.09 (3 mcM), 0.95 (300 mcM); MDR1-LLC-PK1 cells, Efflux ratio = 1.35 (10 mcM); Coadministration of Amiodarone (P-gp & CYP2C9 inhibitor, 600 mg QD on Day 4) with Dabigatran metexilate mesylate (150 mg BID x 3 days and 150 mg QD on Day 4) increased total Dabigatran AUCtau,ss by 58% and Cmax by 50%., Coadministration of Verapamil (P-gp inhibitor, 120 mg single or multiple doses, or 240 mg single dose) with Dabigatran metexilate mesylate (150 mg single dose) increased total Dabigatran AUCinf by 39~143% and Cmax by 12~179%., Coadministration of Quinidine (200 mg every 2 hr x 5 on Day 3 (3 hr after the first Dabigatran dose), P-gp inhibitor) with Dabigatran metexilate mesylate (150 mg BID x 3 days (2nd dose on Day 3 was administrated 1 hr after the final Quinidine dose) increased total Dabigatran AUCtau,ss by 53% and Cmax,ss by 56%., Coadministration of Ketoconazole (CYP3A4 & P-gp inhibitor, 400mg QD ) with Dabigatran metexilate mesylate (150 mg QD) increased total Dabigatran AUCinf by 138% and Cmax by 135%., Coadministration of Atorvastatin (CYP3A4 & P-gp inhibitor, 400 mg QD x 4 days) with Dabigatran metexilate mesylate (150 mg BID x 3 days and 150 mg QD on Day 4) decreased total Dabigatran AUCtau,ss by 58% and Cmax,ss by 50%., Coadministration of Clarithromycin (CYP3A4 & P-gp inhibitor, 500 mg BID x 5 days & 500 mg QD on Day 6) with Dabigatran metexilate mesylate (150 mg QD on Day 6) increased total Dabigatran AUCinf by 19% and Cmax by 15%., Coadministration of Rifampicin (CYP3A4 & P-gp inducer, 600 mg QD x 7 days in the night) with Dabigatran metexilate mesylate (150 mg QD on Day 8 morning) decreased total Dabigatran AUCinf by 67% and Cmax by 66%. Page: 54-55, 56-57, (ClinPharm) 12, 13, 33-36, (PMDA_A100_1 Japanese) 33, 39, 40-41, (PMDA_I100_1 Japanese) 66, (PMDA_K103_1 Japanese) 152-156 |
||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
yes [Km 371.4 uM] | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
yes [Km 511.7 uM] | |||
Page: 70-71, (PMDA_A100_1 Japanese) 33, (PMDA_I100-_ Japanese) 101 |
yes [Km 987.3 uM] |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
[Haemostasis and antithrombotic drugs: pharmacology and novel therapeutic approaches]. | 2006 May |
|
Effects of the direct thrombin inhibitor dabigatran on ex vivo coagulation time in orthopaedic surgery patients: a population model analysis. | 2006 Nov |
|
Investigational treatments of venous thromboembolism. | 2007 Apr |
|
Antithrombotic and anticoagulant effects of the direct thrombin inhibitor dabigatran, and its oral prodrug, dabigatran etexilate, in a rabbit model of venous thrombosis. | 2007 Jun |
|
Emergence of new oral antithrombotics: a critical appraisal of their clinical potential. | 2008 |
|
New issues in oral anticoagulants. | 2008 |
|
Dabigatran etexilate. | 2008 |
|
[New anticoagulants]. | 2008 Feb |
|
Update on atrial fibrillation: part I. | 2008 Feb |
|
New oral anticoagulants in atrial fibrillation. | 2008 Jan |
|
New developments in anticoagulation for atrial fibrillation. | 2008 Sep |
|
The prevention and treatment of venous thromboembolism with LMWHs and new anticoagulants. | 2009 |
|
Use of anticoagulants in elderly patients: practical recommendations. | 2009 |
|
[New anticoagulants for secondary haemostasis--anti IIa inhibitors]. | 2009 Aug |
|
Use of emerging oral anticoagulants in clinical practice: translating results from clinical trials to orthopedic and general surgical patient populations. | 2009 Aug |
|
Recent developments in the use of oral anticoagulants. | 2009 Aug |
|
Favorable therapeutic index of the direct factor Xa inhibitors, apixaban and rivaroxaban, compared with the thrombin inhibitor dabigatran in rabbits. | 2009 Aug |
|
Enhancement of pig embryonic implants in factor VIII KO mice: a novel role for the coagulation cascade in organ size control. | 2009 Dec 21 |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Dec 31 |
|
Oral thrombin inhibitor dabigatran etexilate vs North American enoxaparin regimen for prevention of venous thromboembolism after knee arthroplasty surgery. | 2009 Jan |
|
New anticoagulants: focus on venous thromboembolism. | 2009 Jul |
|
The prevention of hospital-acquired venous thromboembolism in the United Kingdom. | 2009 Mar |
|
Rivaroxaban -- an oral, direct Factor Xa inhibitor: lessons from a broad clinical study programme. | 2009 May |
|
Direct inhibitors of coagulation proteins - the end of the heparin and low-molecular-weight heparin era for anticoagulant therapy? | 2009 Nov |
|
Adherence to a new oral anticoagulant treatment prescription: dabigatran etexilate. | 2009 Nov 3 |
|
Dabigatran etexilate in venous thromboembolism. | 2009 Oct |
|
[New developments in antithrombotic care]. | 2009 Sep |
|
Dabigatran enhances clot susceptibility to fibrinolysis by mechanisms dependent on and independent of thrombin-activatable fibrinolysis inhibitor. | 2010 Apr |
|
Replacing aspirin and warfarin for secondary stroke prevention: is it worth the costs? | 2010 Feb |
|
New oral anticoagulants: a practical guide for clinicians. | 2010 Feb |
|
The new oral anticoagulants. | 2010 Jan 7 |
|
Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. | 2010 Mar |
|
Insights from the dabigatran versus warfarin in patients with atrial fibrillation (RE-LY) trial. | 2010 Mar |
|
[Oral prevention of thromboembolism with rivaroxaban and dabigatran: are the newly approved drugs innovations in orthopaedic and trauma surgery? ]. | 2010 Sep |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/dabigatran.html
Usual Adult Dose for Deep Vein Thrombosis - Prophylaxis
Recommended doses: 150 mg orally twice a day
Usual Adult Dose for Prevention of Thromboembolism in Atrial Fibrillation
Recommended doses: 150 mg orally twice a day
Usual Adult Dose for Deep Vein Thrombosis/Pulmonary Embolism Prophylaxis Following Hip Replacement Surgery
110 mg orally 1 to 4 hours after surgery and after hemostasis has been achieved, then 220 mg orally once a day for 28 to 35 days
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24497951
Dabigatran at higher concentrations (500 and 1000 nM) potently inhibited thrombus formation. In platelet-poor plasma, dabigatran at 250 and 500 nM efficiently prolonged the lag time (LT) and moderately reduce peak height (PH) of TG.
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:56:08 UTC 2023
by
admin
on
Wed Jul 05 23:56:08 UTC 2023
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Record UNII |
2E18WX195X
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C263
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WHO-VATC |
QB01AE07
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WHO-ATC |
B01AE07
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70743
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2E18WX195X
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DB06695
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213023
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SUB20521
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211915-06-9
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M4064
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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100000089553
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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1037042
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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776
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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CHEMBL539697
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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UU-126
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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DTXSID4057681
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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8028
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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C87480
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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70746
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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6379
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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2E18WX195X
Created by
admin on Wed Jul 05 23:56:08 UTC 2023 , Edited by admin on Wed Jul 05 23:56:08 UTC 2023
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PRODRUG |
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
FECAL
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METABOLITE ACTIVE -> PARENT |
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
FECAL
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
TRACE AMOUNT
PLASMA; URINE
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
FECAL
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
TRACE AMOUNT
URINE
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METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
TRACE AMOUNT
PLASMA
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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