Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H25N7O3 |
Molecular Weight | 471.5121 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cn1c2ccc(cc2nc1CNc3ccc(cc3)C(=N)N)C(=O)N(CCC(=O)O)c4ccccn4
InChI
InChIKey=YBSJFWOBGCMAKL-UHFFFAOYSA-N
InChI=1S/C25H25N7O3/c1-31-20-10-7-17(25(35)32(13-11-23(33)34)21-4-2-3-12-28-21)14-19(20)30-22(31)15-29-18-8-5-16(6-9-18)24(26)27/h2-10,12,14,29H,11,13,15H2,1H3,(H3,26,27)(H,33,34)
Molecular Formula | C25H25N7O3 |
Molecular Weight | 471.5121 |
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 |
---|---|---|
New issues in oral anticoagulants. | 2008 |
|
[Anaesthesia and thromboembolic disease]. | 2008 Nov |
|
Recently published papers: Novel therapies in chronic obstructive pulmonary disease, cardiac chemicals and intensive care outcomes. | 2009 |
|
[Dabigatran versus Warfarin in patients with atrial fibrillation. Results of the RE-LY study]. | 2009 |
|
A cost-effectiveness model comparing rivaroxaban and dabigatran etexilate with enoxaparin sodium as thromboprophylaxis after total hip and total knee replacement in the irish healthcare setting. | 2009 |
|
The prevention and treatment of venous thromboembolism with LMWHs and new anticoagulants. | 2009 |
|
Coadministration of dabigatran etexilate and atorvastatin: assessment of potential impact on pharmacokinetics and pharmacodynamics. | 2009 |
|
Recent developments in the use of oral anticoagulants. | 2009 Aug |
|
Clinical trials update from the European Society of Cardiology Meeting 2009: AAA, RELY, PROTECT, ACTIVE-I, European CRT survey, German pre-SCD II registry, and MADIT-CRT. | 2009 Dec |
|
[New oral anticoagulants. Consequences for perioperative coagulation diagnostics and therapy]. | 2009 Dec |
|
Oral direct thrombin inhibitor AZD0837 for the prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation: a randomized dose-guiding, safety, and tolerability study of four doses of AZD0837 vs. vitamin K antagonists. | 2009 Dec |
|
Dabigatran versus warfarin in the treatment of acute venous thromboembolism. | 2009 Dec 10 |
|
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 |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Dec 31 |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Dec 31 |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Dec 31 |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Dec 31 |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Dec 31 |
|
Dabigatran: new drug. Continue to use heparin, a better-known option. | 2009 Jun |
|
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 |
|
[Pharmacokinetics and pharmacodynamics of the new oral anticoagulants dabigatran and rivaroxaban]. | 2009 May-Jun |
|
[Dabigatran and rivaroxaban, new oral anticoagulants for the treatment of venous thromboembolism]. | 2009 May-Jun |
|
[The results of the RE-lY study promise more effective, safer and easier prevention of embolic complications in patients with non-valvular atrial fibrillation]. | 2009 Nov |
|
Direct inhibitors of coagulation proteins - the end of the heparin and low-molecular-weight heparin era for anticoagulant therapy? | 2009 Nov |
|
Dabigatran, a direct thrombin inhibitor, demonstrates antifibrotic effects on lung fibroblasts. | 2009 Nov |
|
The RE-LY study: Randomized Evaluation of Long-term anticoagulant therapY: dabigatran vs. warfarin. | 2009 Nov |
|
Adherence to a new oral anticoagulant treatment prescription: dabigatran etexilate. | 2009 Nov 3 |
|
Dabigatran etexilate in venous thromboembolism. | 2009 Oct |
|
Rivaroxaban for the prevention of venous thromboembolism: a single technology appraisal. | 2009 Oct |
|
[New developments in antithrombotic care]. | 2009 Sep |
|
[Dabigatran: clinical pharmacology]. | 2009 Sep |
|
[Perspectives in cardiology: evidence of efficacy in atrial fibrillation and hopes in acute coronary syndrome]. | 2009 Sep |
|
[Anticoagulants drugs direct trombin inhibitors]. | 2009 Sep |
|
Dabigatran versus warfarin in patients with atrial fibrillation. | 2009 Sep 17 |
|
Dabigatran: safer, more effective and easier to use than warfarin. | 2009 Sep-Oct |
|
Pharmacology, pharmacokinetics, and pharmacodynamics of dabigatran etexilate, an oral direct thrombin inhibitor. | 2009 Sep-Oct |
|
Dabigatran enhances clot susceptibility to fibrinolysis by mechanisms dependent on and independent of thrombin-activatable fibrinolysis inhibitor. | 2010 Apr |
|
[Dabigatran: a new therapeutic option for therapy and prophylaxis of thromboembolic diseases?]. | 2010 Feb |
|
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 potential benefits of low-molecular-weight heparins in cancer patients. | 2010 Jan 14 |
|
The new oral anticoagulants. | 2010 Jan 7 |
|
Does dabigatran improve stroke prevention in atrial fibrillation? A rebuttal. | 2010 Jun |
|
Thrombin-induced CCN2 expression as a target for anti-fibrotic therapy in scleroderma. | 2010 Jun |
|
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 |
|
New anticoagulants for prevention and treatment of venous thromboembolism. | 2010 May |
|
[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
Fri Jun 25 23:41:51 UTC 2021
by
admin
on
Fri Jun 25 23:41:51 UTC 2021
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Record UNII |
I0VM4M70GC
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Record Status |
Validated (UNII)
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Record Version |
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-
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NCI_THESAURUS |
C263
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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LOINC |
68980-2
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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LOINC |
74220-5
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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LIVERTOX |
255
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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Code System | Code | Type | Description | ||
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SUB25417
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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C554682
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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CHEMBL48361
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | |||
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C73224
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | |||
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216210
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | |||
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DABIGATRAN
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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1546356
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | RxNorm | ||
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211914-51-1
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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Dabigatran
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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M4064
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | Merck Index | ||
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211914-51-1
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | |||
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I0VM4M70GC
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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DB14726
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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8027
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY | |||
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8062
Created by
admin on Fri Jun 25 23:41:51 UTC 2021 , Edited by admin on Fri Jun 25 23:41:51 UTC 2021
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PRIMARY |
Related Record | Type | Details | ||
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR | |||
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INHIBITOR -> TARGET | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
REVERSIBLE
IC50
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Related Record | Type | Details | ||
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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 |
after i.v. infusion of 5 mg of 14C dabigatran in healthy volunteers
TRACE AMOUNT
PLASMA
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METABOLITE -> PARENT |
after i.v. infusion of 5 mg of 14C dabigatran in healthy volunteers
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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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
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
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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||
|
METABOLITE -> PARENT |
after p.o. administration of 200 mg of 14C dabigatran etexilate in healthy volunteers
FECAL
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||
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METABOLITE -> PARENT |
after i.v. infusion of 5 mg of 14C dabigatran in healthy volunteers
URINE
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METABOLITE -> PARENT |
after i.v. infusion of 5 mg of 14C dabigatran in healthy volunteers
FECAL
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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INTRAVENOUS ADMINISTRATION |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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