The Metabolism and Disposition of the Oral Direct Thrombin Inhibitor, Dabigatran, in Humans

No abstract is available for this paper.

• Publication year

  2008

• Venue

  Drug Metabolism And Disposition

• Publication date

  2008-02-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/dmd.107.019083PMID 18006647
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Pharmacokinetics and Pharmacodynamics of the Direct Oral Thrombin Inhibitor Dabigatran in Healthy Elderly Subjects

  2008cited by this paper
• The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects.

  2007influential reference
• A new oral direct thrombin inhibitor, dabigatran etexilate, compared with enoxaparin for prevention of thromboembolic events following total hip or knee replacement: the BISTRO II randomized trial

  2005cited by this paper
• Pharmacokinetic Profile of the Oral Direct Thrombin Inhibitor Dabigatran Etexilate in Healthy Volunteers and Patients Undergoing Total Hip Replacement

  2005influential reference
• The pharmacology and management of the vitamin K antagonists: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy.

  2004cited by this paper
• Dose escalating safety study of a new oral direct thrombin inhibitor, dabigatran etexilate, in patients undergoing total hip replacement: BISTRO I

  2004cited by this paper
• Serine proteases as targets for antithrombotic therapy

  2003cited by this paper
• Characterization of in vitro biotransformation of new, orally active, direct thrombin inhibitor ximelagatran, an amidoxime and ester prodrug.

  2003cited by this paper
• Structure-based design of novel potent nonpeptide thrombin inhibitors.

  2002cited by this paper
• In Vitro Intestinal Permeability of Factor Xa Inhibitors: Influence of Chemical Structure on Passive Transport and Susceptibility to Efflux

  2001cited by this paper
• Inactivation studies of acetylcholinesterase with phenylmethylsulfonyl fluoride.

  2000cited by this paper
• Assessment of microsomal tolbutamide hydroxylation by a simple thin-layer chromatography radioactivity assay.

  1998cited by this paper
• Metabolic deesterification of tazarotene in human blood and rat and human liver microsomes.

  1997cited by this paper
• Mannitol therapy revisited (1940-1997).

  1997cited by this paper
• Catalytic role of cytochrome P4502B6 in the N-demethylation of S-mephenytoin.

  1996cited by this paper
• In vivo and in vitro measurement of CYP2C19 activity.

  1996cited by this paper
• Cytochrome P450 inhibitors. Evaluation of specificities in the in vitrometabolism of therapeutic agents by human liver microsomes.

  1995cited by this paper
• Validation of the (ω-l)-hydroxylation of lauric acid as an in vitro substrate probe for human liver CYP2E1

  1995cited by this paper
• Validation of the (omega-1)-hydroxylation of lauric acid as an in vitro substrate probe for human liver CYP2E1.

  1995cited by this paper
• Acyl glucuronides as chemically reactive intermediates

  1994cited by this paper
• Conjugation—Deconjugation Reactions in Drug Metabolism and Toxicity

  1994cited by this paper
• Lauric acid as a model substrate for the simultaneous determination of cytochrome P450 2E1 and 4A in hepatic microsomes.

  1994cited by this paper
• Bufuralol hydroxylation by cytochrome P450 2D6 and 1A2 enzymes in human liver microsomes.

  1994cited by this paper
• Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2.

  1993cited by this paper
• In vitro effects of various cholinesterase inhibitors on acetyl- and butyrylcholinesterase of healthy volunteers.

  1991cited by this paper
• Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism.

  1986cited by this paper

• UGT2B15 single nucleotide polymorphism reduces dabigatran acylglucuronide formation in humans

  2025cites this paper
• Idarucizumab more effectively reverses the anticoagulant effects of dabigatran acylglucuronide than dabigatran

  2025cites this paper
• Osmotic laxatives do not alter dabigatran plasma concentration in healthy volunteers – a randomized, controlled, cross-over trial

  2025cites this paper
• Future directions in drug-drug interaction evaluations: Industry perspective on the ICH M12 guidance.

  2025cites this paper
• Administration of decapsulated dabigatran via nasogastric tube: A case report.

  2025cites this paper
• Design, synthesis and anticoagulant activity evaluation of deuterium-labeled dabigatran etexilate and its intermediate derivatives

  2025cites this paper
• Novel role of serum albumin imidase activity in the formation of BI 761036 (M232), a major metabolite of iclepertin.

  2025cites this paper
• Tryptase-like proteases: A novel perspective for fibrosis.

  2025cites this paper
• Effect of vepdegestrant, a PROTAC oestrogen receptor degrader, on dabigatran and rosuvastatin pharmacokinetics in healthy participants

  2025cites this paper
• Gastric stress events impact the bioavailability of a poorly soluble weak base dabigatran from pellet-filled capsules: An outcome from pharmacokinetic simulations based on biorelevant dissolution testing, machine learning, and a novel timewise first-order dissolution model.

  2025cites this paper
• Safety and optimal use of direct oral anticoagulant therapy.

  2025cites this paper
• Translation of a physiologically-based pharmacokinetic model for dabigatran etexilate to the design of a safety and efficacy study in post-partum women.

  2025cites this paper
• Eudragit S100-coated liposomes: a pH-responsive strategy to overcome dabigatran etexilate's oral bioavailability challenge.

  2025cites this paper
• Pharmacokinetic drug-drug interactions of direct oral anticoagulants

  2025cites this paper
• Variability in intestinal drug metabolizing enzymes and transporters in Crohn's disease and potential impact on oral drug absorption

  2025cites this paper
• Machine Learning Models With Prognostic Implications for Predicting Gastrointestinal Bleeding After Coronary Artery Bypass Grafting and Guiding Personalized Medicine: Multicenter Cohort Study

  2025cites this paper
• Assessing the relative contribution of CYP3A-and P-gp-mediated pathways to the overall disposition and drug-drug interaction of dabigatran etexilate using a comprehensive mechanistic physiological-based pharmacokinetic model

  2024cites this paper
• Being precise with anticoagulation to reduce adverse drug reactions: are we there yet?

  2024cites this paper
• Risk factors for postgastric endoscopic submucosal dissection bleeding in direct oral anticoagulant users

  2024cites this paper
• Comparative Cardioprotective Effectiveness: NOACs vs. Nattokinase—Bridging Basic Research to Clinical Findings

  2024influential citation
• The pharmacokinetics of dabigatran in a rat model of hyperlipidaemia induced by poloxamer 407

  2024influential citation
• The level is in the details: Why differences between direct‐acting oral anticoagulants should be considered in the treatment of patients with epilepsy

  2024cites this paper
• Pharmacology of spinal interventions: review of agents used in spine pain procedures

  2024cites this paper
• S974 A Closer Look into Gastrointestinal Bleeding in Heart Failure Patients

  2024cites this paper
• Uncovering the Role of Direct Oral Anticoagulants in Stroke Prevention for Atrial Fibrillation: A Review of the Literature

  2024influential citation
• Direct oral anticoagulants in cirrhosis: Rationale and current evidence

  2024cites this paper
• The Use of DOACs in Pediatrics: Current Therapeutic and Prophylactic Indications, Cardiac Indications, and Real-World Evidence—A Review

  2024cites this paper
• Synthesis of deuterium labeled dabigatran etexilate

  2024cites this paper
• Intestinal P‐gp activity is reduced in postmenopausal women under breast cancer therapy

  2024cites this paper
• [The multidirectional effects of thrombin and the possibility of their control in neurology].

  2024cites this paper
• Dabigatran pharmacokinetic-pharmacodynamic in sheep: Informing dose for anticoagulation during cardiopulmonary bypass

  2024cites this paper
• Lymphatic uptake of a highly lipophilic protease inhibitor prodrug from a lipid-based formulation is limited by instability in the intestine.

  2024cites this paper
• Evaluation of Drug–Drug Interactions Between Clarithromycin and Direct Oral Anticoagulants Using Physiologically Based Pharmacokinetic Models

  2024cites this paper
• Practical guidance for direct oral anticoagulant use in the treatment of venous thromboembolism in primary and metastatic brain tumor patients

  2024cites this paper
• A rapid and sensitive analytical methodology for the simultaneous biomonitoring of two direct oral anticoagulant drugs and their major metabolites in thromboembolic disordered patients samples for clinical evaluations.

  2024cites this paper
• Special Section on Perspective on Drug Metabolism and Disposition, Part I — Minireview Human Absorption, Distribution, Metabolism, and Excretion Studies: Origins, Innovations, and Importance S

  2023cites this paper
• Gastroprotective therapy in patients with atrial fibrillation receiving anticoagulant therapy: A review

  2023cites this paper
• Implications of potential clinically relevant interactions between COVID‐19 vaccines and concomitant medications

  2023cites this paper
• Direct oral anticoagulant drugs for the management of venous thromboembolism.

  2023cites this paper
• Effects of Simvastatin on Pharmacokinetics and Anticoagulant Effects of Dabigatran in Healthy Subjects

  2023cites this paper
• Preclinical Study on a Novel Fluoroderivative of Dabigatran Etexilate in Animal Models

  2023cites this paper
• Advance of New Oral Anticoagulants in the Treatment of Portal Vein Thrombosis in Cir-rhosis

  2023cites this paper
• Physiologically-based pharmacokinetic modeling to predict drug-drug interactions of dabigatran etexilate and rivaroxaban in the Chinese older adults

  2023cites this paper
• Features of the use of oral anticoagulants in clinical practice: focus on gastrointestinal complications

  2023cites this paper
• ダビガトラン過量服薬に対するイダルシズマブの静脈内投与：血漿中ダビガトラン濃度と血液凝固能の関連性(Intravenous idarucizumab for dabigatran overdose: association between plasma dabigatran concentration and coagulation profile)

  2023cites this paper
• Liver injury from direct oral anticoagulants

  2023cites this paper
• The Potentially Significant Role of CYP3A-Mediated Oxidative Metabolism of Dabigatran Etexilate and Its Intermediate Metabolites in Drug-Drug Interaction Assessments Using Microdose Dabigatran Etexilate

  2023influential citation
• Idarucizumab for Emergency Reversal of the Anticoagulant Effects of Dabigatran: Final Results of a Japanese Postmarketing Surveillance Study

  2023cites this paper
• Synthesis of Novel Arginine Building Blocks with Increased Lipophilicity Compatible with Solid-Phase Peptide Synthesis

  2023cites this paper
• Effect of direct oral anticoagulant dabigatran on early bone healing: An experimental study in rats

  2023cites this paper
• Direct Thrombin Inhibitor Dabigatran Compromises Pulmonary Endothelial Integrity in a Murine Model of Breast Cancer Metastasis to the Lungs; the Role of Platelets and Inflammation-Associated Haemostasis

  2022cites this paper
• A three-step stacking capillary electrophoresis of field-amplified sample injection, sweeping, and micellar collapse for determination of dabigatran and its active metabolite in human plasma

  2022cites this paper
• The impact of advanced age on anticoagulant therapy for acute venous thromboembolism

  2022cites this paper
• Peculiarities of dabigatran pharmacogenetics: literature review

  2022cites this paper
• Therapeutic Strategies for Disseminated Intravascular Coagulation Associated with Aortic Aneurysm

  2022cites this paper
• Use of Non-Vitamin K Dependent Oral Anticoagulant in Ischemic Stroke

  2022cites this paper
• In vivo Anticoagulant Activity of Immediate Release Tablets of Dabigatran Etexilate Mesylate Cocrystals

  2022cites this paper
• Direct Oral Anticoagulants: An Updated Systematic Review of Their Clinical Pharmacology and Clinical Effectiveness and Safety in Patients With Nonvalvular Atrial Fibrillation

  2022cites this paper
• [Dabigatran Reversal: A Practical Approach].

  2022cites this paper
• Direct oral anticoagulants in pediatric venous thromboembolism: Review of approved products rivaroxaban and dabigatran

  2022cites this paper
• Influence of ABCB1, CYP3A5 and CYP3A4 gene polymorphisms on prothrombin time and the residual equilibrium concentration of rivaroxaban in patients with non-valvular atrial fibrillation in real clinical practice

  2022cites this paper
• Gut microbiota and cardiac arrhythmia: a pharmacokinetic scope

  2022cites this paper
• Impact of anticoagulants on the clinical outcomes of colonic diverticular bleeding comparing warfarin and direct oral anticoagulants

  2022cites this paper
• Carboxylesterase-2 plays a critical role in dabigatran etexilate active metabolite formation.

  2022cites this paper
• In Vitro Antithrombotic, Hematological Toxicity, and Inhibitor Studies of Protocatechuic, Isovanillic, and p-Hydroxybenzoic Acids from Maclura tricuspidata (Carr.) Bur

  2022cites this paper
• Inhibition of Radix Scutellariae flavones on carboxylesterase mediated activations of prodrugs.

  2022cites this paper
• Cutaneous Ulcer Caused by Apixaban Treatment Is Resolved after Replacement with Dabigatran

  2022cites this paper
• Pharmakologische Eigenschaften mit Praxisrelevanz

  2022cites this paper
• Development and Validation of UPLC-MS/MS Method for Quantifying of Free and Total Dabigatran in Human Plasma: An Application for a Bioequivalence Study.

  2022cites this paper
• verapam-PECULIARITIES OF DABIGATRAN PHARMACOGENETICS: LITERATURE REVIEW

  2022cites this paper
• Grundlagen des perioperativen Umgangs mit direkten oralen Antikoagulanzien

  2022cites this paper
• SLC4A4, FRAS1, and SULT1A1 Genetic Variations Associated With Dabigatran Metabolism in a Healthy Chinese Population

  2022influential citation
• Neuropharmacology in the Intensive Care Unit.

  2022cites this paper
• Novel inhibitors of breast cancer resistance protein (BCRP, ABCG2) among marketed drugs.

  2022cites this paper
• Physiologically‐based pharmacokinetics modeling to investigate formulation factors influencing the generic substitution of dabigatran etexilate

  2021influential citation
• Relationship between the degree of renal dysfunction and the safety and efficacy outcomes in patients with atrial fibrillation receiving direct oral anticoagulants

  2021cites this paper
• The pleiotropic effects of antithrombotic drugs in the metabolic-cardiovascular-neurodegenerative disease continuum: impact beyond reduced clotting.

  2021cites this paper
• 2021 European Heart Rhythm Association Practical Guide on the Use of Non-Vitamin K Antagonist Oral Anticoagulants in Patients with Atrial Fibrillation.

  2021cites this paper
• Comparison of the efficacy of rivaroxaban and dabigatran etexilate in preventing venous thrombosis after arthroplasty

  2021cites this paper
• Pharmacogenetics of Direct Oral Anticoagulants: A Systematic Review

  2021cites this paper
• Biopharmaceutics considerations for direct oral anticoagulants

  2021cites this paper
• Laboratory Monitoring of Direct Oral Anticoagulants (DOACs)

  2021cites this paper
• Next Asra guidelines anticoagulation neuraxial anesthesia 2010 asra guidelines on neuraxial anesthesia and anticoagulation. Asra guidelines for neuraxial anesthesia and anticoagulation

  2021cites this paper
• Direct oral anticoagulants are associated with potentially bleeding lesions in suspected mid-gastrointestinal bleeding

  2021cites this paper
• Управление факторами риска желудочно-кишечных кровотечений на фоне антикоагулянтной терапии

  2021cites this paper
• Determination of Dabigatran Concentration in Human Plasma and Breast Milk

  2021cites this paper
• Physiologically‐based pharmacokinetic modeling to evaluate in vitro‐to‐in vivo extrapolation for intestinal P‐glycoprotein inhibition

  2021cites this paper
• Postoperative Bleeding Complications in Patients on Novel Oral Anticoagulants and Vitamin K Antagonist Following an Invasive Dental Procedure - A Review of Literature

  2021cites this paper
• Strategies for the prevention and treatment of bleeding in patients treated with dabigatran: an update

  2021cites this paper
• Mass spectrometry-based targeted proteomics method for the quantification of clinically relevant drug metabolizing enzymes in human specimens.

  2021cites this paper
• Pharmacokinetics and Pharmacodynamics of DOAC

  2021cites this paper
• Association Between Use of Pharmacokinetic‐Interacting Drugs and Effectiveness and Safety of Direct Acting Oral Anticoagulants: Nested Case‐Control Study

  2021cites this paper
• Risk of Major Bleeding and Thromboembolism in Asian Atrial Fibrillation Patients Using Non-vitamin K Oral Anticoagulants Versus Warfarin

  2021cites this paper
• Reduced physiologically-based pharmacokinetic model of dabigatran etexilate-dabigatran and its application for prediction of intestinal P-gp-mediated drug-drug interactions.

  2021cites this paper
• Direct Oral Anticoagulants: From Randomized Clinical Trials to Real-World Clinical Practice

  2021cites this paper
• Alternatives for Vitamin K Antagonists as Thromboprophylaxis for Mechanical Heart Valves and Mechanical Circulatory Support Devices: A Systematic Review

  2021cites this paper
• Risk of major bleeding and thromboembolism in Asian patients with nonvalvular atrial fibrillation using direct oral anticoagulants versus warfarin

  2021cites this paper
• Review Article: Gastrointestinal Bleeding Risk with Direct Oral Anticoagulants

  2021cites this paper
• Direct Oral Anticoagulants in Patients with Atrial Fibrillation and Renal Dysfunction

  2021cites this paper
• Comparative Analysis of Compliance between Rivaroxaban with Heparin & Warfarin in the Management of Deep Vein Thrombosis Tertiary Care Hospital Larkana

  2021cites this paper