Enoxaparin
Identification
- Summary
Enoxaparin is a low molecular weight heparin used for the prophylaxis of deep vein thrombosis and ischemic complications of unstable angina and non-Q-wave myocardial infarction.
- Brand Names
- Lovenox
- Generic Name
- Enoxaparin
- DrugBank Accession Number
- DB01225
- Background
Enoxaparin is a common low-molecular-weight heparin (LMWH) used in the prevention and management of various thromboembolic disorders. Initially approved by the FDA in 1993, it is administered by a subcutaneous or intravenous injection and marketed by several pharmaceutical companies.10 Enoxaparin markedly reduces the incidence of venous thromboembolism in hospitalized patients when compared to unfractionated heparin, without increasing the risk of serious bleeding.5,7
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Not Available
Pharmacology
- Indication
Enoxaparin is indicated for the prevention of ischemic complications in unstable angina and in non Q-wave myocardial infarction; it is indicated in conjunction with percutaneous intervention and/or other treatment for the management of acute ST elevation myocardial infarction. 10
Enoxaparin is also indicated in the prophylaxis of DVT in abdominal surgery, hip replacement, knee replacement, or medical patients with severely restricted mobility during acute illness. Additionally, enoxaparin is indicated for the inpatient treatment of DVT with or without pulmonary embolism and the treatment of outpatient DVT without pulmonary embolism.10
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- Associated Conditions
- Associated Therapies
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- Pharmacodynamics
This drug has an immediate onset of action.11 Enoxaparin increases Thrombin Time (TT) and activated partial thromboplastin time (aPTT), preventing and reducing thromboembolic complications such as DVT, pulmonary embolism, and ischemic cardiac complications.1 Administered at 1.5 mg/kg subcutaneously in a pharmacodynamic study, enoxaparin led to a higher ratio of anti-Factor Xa to anti-Factor IIa activity (mean ±SD, 14.0±3.1) (based on areas under anti-Factor activity versus time curves) when compared to that of heparin (mean ±SD, 1.22±0.13). Increases in the TT and aPTT were 1.8 times those of the control group.10 Enoxaparin at 1 mg/kg subcutaneously every 12 hours led to aPTT values of 45 seconds or less in most patients. Average aPTT prolongation time on Day 1 was approximately 16% higher than on Day 4 of enoxaparin therapy.10
Caution is advised during treatment with enoxaparin - the risk of hemorrhage and thrombocytopenia is increased. In pregnant women with prosthetic mechanic heart valves, the risk of thromboembolism is increased.10
- Mechanism of action
Enoxaparin binds to antithrombin III, a serine protease inhibitor, forming a complex that irreversibly inactivates factor Xa, which is frequently used to monitor anticoagulation in the clinical setting.8 Following factor Xa inactivation, enoxaparin is released and binds to other anti-thrombin molecules. Factor IIa (thrombin) is directly inhibited by enoxaparin, however with less potency than unfractionated heparin (UFH). 6 Due to the cascade of effects resulting from enoxaparin binding, thrombin is unable to convert fibrinogen to fibrin and form a clot, preventing thromboembolic events.
Target Actions Organism AAntithrombin-III potentiatorHumans ACoagulation factor X inhibitorHumans UProthrombin inhibitorHumans - Absorption
Mean absolute bioavailability of enoxaparin, after 1-2 mg/kg given subcutaneously is approximately 100% in healthy volunteers. The absorption of enoxaparin is proportional to the dose, demonstrating linear absorption. The average maximum plasma anti-Xa activity is reached 3 to 5 hours after a subcutaneous injection.9,12 A 30 mg IV bolus preceding an immediate 1 mg/kg SC every twice a day led to maximum anti-Factor Xa levels of 1.16 IU/mL. Steady-state is reached within 3-4 days9 of treatment with a Cmax of 1.2 IU/mL.12 The AUC under the thrombin generation curve was 305 +/- 48.8
- Volume of distribution
The volume of distribution of enoxaparin is approximately 4-5L, similar to normal blood volume.10,12
- Protein binding
Enoxaparin binds to antithrombin III.12 The percentage of plasma protein binding for enoxaparin is not readily available in the literature.
- Metabolism
Enoxaparin is mainly metabolized by the liver via desulfation and/or depolymerization to lower and less potent molecular weight metabolites.10,12
- Route of elimination
Enoxaparin is mainly excreted by the kidneys.4 Renal clearance of active fragments represents about 10% of the administered dose and total renal excretion of active and non-active fragments 40% of the dose.12
- Half-life
The half-life of enoxaparin is about 4 hours after a single dose administered subcutaneously and about 7 hours after several doses.12 One source mentions a half-life ranging from 1 hour to 4.5 hours.9
- Clearance
The mean clearance of enoxaparin is 0.74 L/h after a 1.5 mg/kg intravenous infusion over 6 hours12; clearance of enoxaparin is significantly decreased in patients with severe renal impairment.2
- Adverse Effects
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data- Toxicity
The oral LD50 for enoxaparin in mice is >5000 mg/kg; the subcutaneous LD50 of enoxaparin in mice is >2500 mg/kg.13 Accidental overdose after the administration of enoxaparin may cause hemorrhage. Enoxaparin administered by injection is mainly neutralized by gradual intravenous injection of a 1% protamine sulfate solution. The dose of protamine sulfate should be equal to the dose of enoxaparin administered: 1 mg protamine sulfate for 1 mg enoxaparin, of enoxaparin was administered in the previous 8 hours. If a minimum of 12 hours has passed since the last enoxaparin dose, protamine may not be necessary; it is important to avoid an overdose with protamine, as fatal reactions may occur.10
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of bleeding can be increased when Abciximab is combined with Enoxaparin. Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Enoxaparin. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Enoxaparin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Enoxaparin. Acenocoumarol The risk or severity of bleeding can be increased when Enoxaparin is combined with Acenocoumarol. Acetylsalicylic acid Acetylsalicylic acid may increase the anticoagulant activities of Enoxaparin. Albutrepenonacog alfa The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Enoxaparin. Alclofenac The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Enoxaparin. Aldesleukin The risk or severity of bleeding can be increased when Enoxaparin is combined with Aldesleukin. Alemtuzumab The risk or severity of bleeding can be increased when Enoxaparin is combined with Alemtuzumab. 
Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more - Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- Product Ingredients
Ingredient UNII CAS InChI Key Enoxaparin sodium 8NZ41MIK1O 679809-58-6 Not applicable - Product Images
- International/Other Brands
- Clexane
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Inclunox Solution 40 mg / 0.4 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-05-04 Not applicable Canada 
Inclunox Solution 80 mg / 0.8 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-05-04 Not applicable Canada Inclunox Solution 30 mg / 0.3 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-06-21 Not applicable Canada Inclunox Solution 60 mg / 0.6 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-05-04 Not applicable Canada Inclunox Solution 100 mg / 1 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-05-04 Not applicable Canada Inclunox Hp Solution 150 mg / 1 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-05-04 Not applicable Canada Inclunox Hp Solution 120 mg / 0.8 mL Intravenous; Subcutaneous Sandoz Canada Incorporated 2021-05-04 Not applicable Canada Inhixa Injection, solution 40 mg/0.4mL Techdow Pharma Netherlands B.V. 2021-01-12 Not applicable EU 
Inhixa Injection, solution 40 mg/0.4mL Techdow Pharma Netherlands B.V. 2021-01-12 Not applicable EU Inhixa Injection, solution 60 mg/0.6mL Techdow Pharma Netherlands B.V. 2021-01-12 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Enoxaparin sodium Injection 120 mg/0.8mL Subcutaneous Winthrop U.S. 2011-10-03 Not applicable US 
Enoxaparin Sodium Injection 100 mg/1mL Subcutaneous Amphastar Pharmaceuticals, Inc. 2011-09-19 Not applicable US Enoxaparin Sodium Injection 100 mg/1mL Subcutaneous Amphastar Pharmaceuticals, Inc. 2011-09-19 Not applicable US Enoxaparin Sodium Injection 100 mg/1mL Subcutaneous Sandoz Inc 2010-07-23 Not applicable US Enoxaparin Sodium Injection 100 mg/1mL Subcutaneous NorthStar Rx LLC 2019-12-01 Not applicable US Enoxaparin Sodium Injection 80 mg/0.8mL Subcutaneous Apotex Corp. 2019-01-31 Not applicable US Enoxaparin Sodium Injection, solution 30 mg/0.3mL Intravenous; Subcutaneous Teva Parenteral Medicines, Inc. 2014-12-19 Not applicable US Enoxaparin Sodium Injection, solution 30 mg/0.3mL Intravenous; Subcutaneous Italfarmaco SpA 2021-04-01 Not applicable US Enoxaparin sodium Injection 80 mg/0.8mL Subcutaneous Winthrop U.S. 2011-10-03 Not applicable US Enoxaparin Sodium Injection 150 mg/1mL Subcutaneous Amphastar Pharmaceuticals, Inc. 2011-09-19 Not applicable US
Categories
- ATC Codes
- B01AB05 — Enoxaparin
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- E47C0NF7LV
- CAS number
- 9005-49-6
References
- Synthesis Reference
Jorgen I. Nielsen, "Process of using light absorption to control enzymatic depolymerization of heparin to produce low molecular weight heparin." U.S. Patent US5106734, issued May, 1981.
US5106734- General References
- Iqbal Z, Cohen M: Enoxaparin: a pharmacologic and clinical review. Expert Opin Pharmacother. 2011 May;12(7):1157-70. doi: 10.1517/14656566.2011.570261. Epub 2011 Apr 7. [Article]
- Sanderink GJ, Guimart CG, Ozoux ML, Jariwala NU, Shukla UA, Boutouyrie BX: Pharmacokinetics and pharmacodynamics of the prophylactic dose of enoxaparin once daily over 4 days in patients with renal impairment. Thromb Res. 2002 Feb 1;105(3):225-31. doi: 10.1016/s0049-3848(02)00031-2. [Article]
- Azizi M, Veyssier-Belot C, Alhenc-Gelas M, Chatellier G, Billaud-Mesguish E, Fiessinger JN, Aiach M: Comparison of biological activities of two low molecular weight heparins in 10 healthy volunteers. Br J Clin Pharmacol. 1995 Dec;40(6):577-84. [Article]
- Bruno R, Baille P, Retout S, Vivier N, Veyrat-Follet C, Sanderink GJ, Becker R, Antman EM: Population pharmacokinetics and pharmacodynamics of enoxaparin in unstable angina and non-ST-segment elevation myocardial infarction. Br J Clin Pharmacol. 2003 Oct;56(4):407-14. doi: 10.1046/j.1365-2125.2003.01904.x. [Article]
- Laporte S, Liotier J, Bertoletti L, Kleber FX, Pineo GF, Chapelle C, Moulin N, Mismetti P: Individual patient data meta-analysis of enoxaparin vs. unfractionated heparin for venous thromboembolism prevention in medical patients. J Thromb Haemost. 2011 Mar;9(3):464-72. doi: 10.1111/j.1538-7836.2011.04182.x. [Article]
- Nutescu EA, Burnett A, Fanikos J, Spinler S, Wittkowsky A: Pharmacology of anticoagulants used in the treatment of venous thromboembolism. J Thromb Thrombolysis. 2016 Jan;41(1):15-31. doi: 10.1007/s11239-015-1314-3. [Article]
- Hofmann T: Clinical application of enoxaparin. Expert Rev Cardiovasc Ther. 2004 May;2(3):321-37. doi: 10.1586/14779072.2.3.321. [Article]
- Wei MY, Ward SM: The Anti-Factor Xa Range For Low Molecular Weight Heparin Thromboprophylaxis. Hematol Rep. 2015 Nov 23;7(4):5844. doi: 10.4081/hr.2015.5844. eCollection 2015 Nov 23. [Article]
- Dawes J: Comparison of the pharmacokinetics of enoxaparin (Clexane) and unfractionated heparin. Acta Chir Scand Suppl. 1990;556:68-74. [Article]
- FDA Approved Drug Products: Lovenox (enoxaparin sodium injection), for subcutaneous and intravenous use [Link]
- NIH StatPearls: Enoxaparin [Link]
- Medsafe NZ Datasheet: CLEXANE AND CLEXANE FORTE (enoxaparin sodium) for injection [Link]
- Pfizer: Enoxaparin sodium MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB14551
- KEGG Drug
- D07510
- PubChem Substance
- 46507450
- ChemSpider
- 751
- 67108
- ChEMBL
- CHEMBL1201685
- Therapeutic Targets Database
- DAP000616
- PharmGKB
- PA449463
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Enoxaparin_sodium
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Acute Coronary Syndrome (ACS) / Myocardial Infarction / Myocardial Ischemia / Unstable Angina Pectoris 1 4 Completed Prevention Acute Coronary Syndrome (ACS) 1 4 Completed Prevention Acute Ischemic Stroke (AIS) 1 4 Completed Prevention Anticoagulants / BMI >30 kg/m2 / Thrombosis, Venous 1 4 Completed Prevention Antiphospholipid Syndrome / Recurrent Miscarriages 1 4 Completed Prevention Deep Vein Thrombosis / Pulmonary Embolism / Venous Thromboembolism Diseases 1 4 Completed Prevention Deteriorating renal function / Venous Thromboembolism 1 4 Completed Prevention Enoxaparin / Placental Insufficiency 1 4 Completed Prevention Fracture of Neck of Femur / Necrosis of Femoral Head / Osteoarthritis in the Hip Joint 1 4 Completed Prevention Inflammation 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Cardinal Health
- Lake Erie Medical and Surgical Supply
- Neuman Distributors Inc.
- Physicians Total Care Inc.
- Sanofi-Aventis Inc.
- Dosage Forms
Form Route Strength Solution Intravenous; Subcutaneous 100 mg Solution Intravenous; Subcutaneous 300 mg Injection, solution Parenteral 10.000 IE Injection, solution Parenteral 100 MG/1ML Injection, solution Parenteral 10000 IE/1ML Injection, solution Parenteral 20 MG/0.2ML Injection, solution Parenteral 2000 IE/0.2ML Injection, solution Parenteral 4.000 IE Solution Intra-arterial; Intravenous; Subcutaneous 40 mg Injection, solution Parenteral 4000 IE/0.4ML Injection, solution Parenteral 4000 I.E./0.4ML Injection, solution Parenteral 40 MG/0.4ML Injection, solution Parenteral 4000 IE Injection, solution Parenteral 6.000 IE Injection Subcutaneous Injection, solution Parenteral 6000 I.E./0.6ML Injection, solution Parenteral 60 MG/0.6ML Injection, solution Parenteral 6000 IE Injection, solution Parenteral 6000 IE/0.6ML Injection, solution Parenteral 60 MG Injection, solution Parenteral 8.000 IE Injection, solution Parenteral 8000 I.E./0.8ML Injection, solution Parenteral 80 MG/0.8ML Injection, solution Parenteral 8000 IE/0.8ML Injection, solution Parenteral 80 MG Solution Intra-arterial; Intravenous; Subcutaneous 80 mg Solution Subcutaneous 100 mg Solution Intra-arterial; Intravenous; Subcutaneous 20 mg Solution Intra-arterial; Intravenous; Subcutaneous 60 mg Injection, solution Intravenous; Parenteral Injection, solution Subcutaneous Solution Intra-arterial; Intravenous; Subcutaneous 100 mg Injection, solution Parenteral Injection, solution Parenteral 10000 IE Injection, solution Parenteral 2000 IE Injection, solution Parenteral 8000 IE Injection, solution 100 mg/1ml Injection Intravenous; Subcutaneous 300 mg/3mL Injection Subcutaneous 100 mg/1mL Injection Subcutaneous 120 mg/0.8mL Injection Subcutaneous 150 mg/1mL Injection Subcutaneous 30 mg/0.3mL Injection Subcutaneous 300 mg/3mL Injection Subcutaneous 40 mg/0.4mL Injection Subcutaneous 60 mg/0.6mL Injection Subcutaneous 80 mg/0.8mL Injection, solution Intravenous; Subcutaneous 100 mg/1mL Injection, solution Intravenous; Subcutaneous 120 mg/0.8mL Injection, solution Intravenous; Subcutaneous 150 mg/1mL Injection, solution Intravenous; Subcutaneous 30 mg/0.3mL Injection, solution Intravenous; Subcutaneous 40 mg/0.4mL Injection, solution Intravenous; Subcutaneous 60 mg/0.6mL Injection, solution Intravenous; Subcutaneous 80 mg/0.8mL Solution 100 mg/1ml Solution Subcutaneous Solution Intravenous; Subcutaneous 20 mg Solution Hemodialysis; Intravenous; Subcutaneous 80 mg Solution Subcutaneous 20 mg Solution Subcutaneous 60 mg Solution Intravenous; Subcutaneous 40 mg Solution Subcutaneous 80 mg Solution Hemodialysis; Intravenous; Subcutaneous 60 mg Solution Intravenous; Subcutaneous 60 mg Solution Intravenous; Subcutaneous 80 mg Injection, solution Parenteral 10000 IU Injection, solution Parenteral 2000 IU Injection, solution Parenteral 4000 IU Injection, solution Parenteral 6000 IU Injection, solution Parenteral 8000 IU Solution Intravenous; Subcutaneous 100 mg / 1 mL Solution Intravenous; Subcutaneous 150 mg / 1 mL Injection, solution 1000 mg/10mL Injection, solution 120 mg/0.8mL Injection, solution 150 mg/1mL Injection, solution 20 mg/0.2mL Injection, solution 300 mg/3mL Injection, solution 40 mg/0.4mL Injection, solution 500 mg/5mL Injection, solution 60 mg/0.6mL Injection, solution 80 mg/0.8mL Injection, solution Epidural; Intravenous bolus; Subcutaneous Injection, solution Extracorporeal; Parenteral Injection, solution Parenteral; Subcutaneous Injection, solution Parenteral 100 mg/ml Injection, solution Parenteral 100 MG Injection, solution Parenteral 40 MG Injection Injection Intravenous; Subcutaneous 100 mg/1mL Injection Intravenous; Subcutaneous 120 mg/0.8mL Injection Intravenous; Subcutaneous 30 mg/0.3mL Injection Intravenous; Subcutaneous 40 mg/0.4mL Injection Intravenous; Subcutaneous 60 mg/0.6mL Injection Intravenous; Subcutaneous 80 mg/0.8mL Solution Subcutaneous 100 mg / mL Solution Subcutaneous 30 mg / 0.3 mL Solution Subcutaneous 40 mg / 0.4 mL Solution Subcutaneous 60 mg / 0.6 mL Solution Subcutaneous 80 mg / 0.8 mL Injection, solution Injection, solution Parenteral 10000 IU/mL Injection, solution Parenteral 100 MG/1.0ML Injection, solution Parenteral 2000 IU/0.2mL Injection, solution Parenteral 20 MG Injection, solution Parenteral 4000 IU/0.4mL Injection, solution Parenteral 6000 IU/0.6mL Injection, solution Parenteral 8000 IU/0.8mL Solution Subcutaneous 120 mg / 0.8 mL Solution Subcutaneous 150 mg / mL Solution Subcutaneous 90 mg / 0.6 mL Solution Intravenous; Subcutaneous 100 mg / mL Solution Intravenous; Subcutaneous 20 mg / 0.2 mL Solution Intravenous; Subcutaneous 30 mg / 0.3 mL Solution Intravenous; Subcutaneous 40 mg / 0.4 mL Solution Intravenous; Subcutaneous 60 mg / 0.6 mL Solution Intravenous; Subcutaneous 80 mg / 0.8 mL Solution Intravenous; Subcutaneous 120 mg / 0.8 mL Solution Intravenous; Subcutaneous 150 mg / mL Solution Subcutaneous 40 mg Solution Subcutaneous Solution Intravenous; Subcutaneous 300 mg / 3 mL Injection, solution Intraluminal; Intravenous; Subcutaneous - Prices
Unit description Cost Unit Lovenox 300 mg/3ml Solution 3ml Vial 281.47USD vial Lovenox 150 mg/ml Solution 1ml Syringe 140.94USD syringe Lovenox 100 mg/ml Solution 1ml Syringe 93.93USD syringe Lovenox 80 mg/0.8ml Solution 0.8ml Syringe 75.14USD syringe Lovenox 60 mg/0.6ml Solution 0.6ml Syringe 56.36USD syringe Lovenox 40 mg/0.4ml Solution 0.4ml Syringe 37.53USD syringe Lovenox Hp (0.8Ml/1Ml Syringe) 150 mg/ml Syringe 34.63USD syringe Lovenox 30 mg/0.3ml Solution 0.3ml Syringe 28.15USD syringe Lovenox (0.4 - 1 Ml Syringe) 100 mg/ml Syringe 23.09USD syringe Lovenox 100 mg/ml 23.09USD syringe Lovenox (0.3 Ml Syringe) 30 mg/syr Syringe 6.97USD syringe DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5389618 No 1995-02-14 2012-02-14 US CA2045433 No 2002-07-30 2011-06-25 Canada
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 50 g/L https://imgcdn.mckesson.com/CumulusWeb/Click_and_learn/SDS_SANOFI_LOVENOX.pdf logP -1.7 https://hmdb.ca/metabolites/HMDB0014551 logS -2 https://hmdb.ca/metabolites/HMDB0014551 pKa -2.8 https://hmdb.ca/metabolites/HMDB0014551 - Predicted Properties
- Not Available
- Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.9215 Blood Brain Barrier - 0.8366 Caco-2 permeable - 0.6496 P-glycoprotein substrate Non-substrate 0.698 P-glycoprotein inhibitor I Non-inhibitor 0.5818 P-glycoprotein inhibitor II Non-inhibitor 0.9771 Renal organic cation transporter Non-inhibitor 0.9454 CYP450 2C9 substrate Non-substrate 0.6694 CYP450 2D6 substrate Non-substrate 0.8196 CYP450 3A4 substrate Non-substrate 0.5842 CYP450 1A2 substrate Non-inhibitor 0.8157 CYP450 2C9 inhibitor Non-inhibitor 0.771 CYP450 2D6 inhibitor Non-inhibitor 0.8869 CYP450 2C19 inhibitor Non-inhibitor 0.7655 CYP450 3A4 inhibitor Non-inhibitor 0.9194 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9232 Ames test Non AMES toxic 0.5957 Carcinogenicity Non-carcinogens 0.694 Biodegradation Not ready biodegradable 0.851 Rat acute toxicity 2.3846 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9589 hERG inhibition (predictor II) Non-inhibitor 0.7157
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory a...
- Gene Name
- SERPINC1
- Uniprot ID
- P01008
- Uniprot Name
- Antithrombin-III
- Molecular Weight
- 52601.935 Da
References
- Peng K, Wang C, Pang BS, Yang YH: [Effects of thrombolysis and anticoagulation on the functions of vascular endothelial cells and coagulation and fibrinolysis in patients with pulmonary thromboembolism]. Zhonghua Jie He He Hu Xi Za Zhi. 2005 Sep;28(9):596-9. [Article]
- Lee S, Gibson CM: Enoxaparin in acute coronary syndromes. Expert Rev Cardiovasc Ther. 2007 May;5(3):387-99. [Article]
- Bisio A, Vecchietti D, Citterio L, Guerrini M, Raman R, Bertini S, Eisele G, Naggi A, Sasisekharan R, Torri G: Structural features of low-molecular-weight heparins affecting their affinity to antithrombin. Thromb Haemost. 2009 Nov;102(5):865-73. doi: 10.1160/TH09-02-0081. [Article]
- NIH StatPearls: Enoxaparin [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- The effects of enoxaparin on factor X occur due to downstream effects after binding to antithrombin III.
- General Function
- Serine-type endopeptidase activity
- Specific Function
- Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
- Gene Name
- F10
- Uniprot ID
- P00742
- Uniprot Name
- Coagulation factor X
- Molecular Weight
- 54731.255 Da
References
- Graff J, Picard-Willems B, Harder S: Monitoring effects of direct FXa-inhibitors with a new one-step prothrombinase-induced clotting time (PiCT) assay: comparative in vitro investigation with heparin, enoxaparin, fondaparinux and DX 9065a. Int J Clin Pharmacol Ther. 2007 Apr;45(4):237-43. [Article]
- Berges A, Laporte S, Epinat M, Zufferey P, Alamartine E, Tranchand B, Decousus H, Mismetti P: Anti-factor Xa activity of enoxaparin administered at prophylactic dosage to patients over 75 years old. Br J Clin Pharmacol. 2007 Oct;64(4):428-38. Epub 2007 May 17. [Article]
- Sanchez-Pena P, Hulot JS, Urien S, Ankri A, Collet JP, Choussat R, Lechat P, Montalescot G: Anti-factor Xa kinetics after intravenous enoxaparin in patients undergoing percutaneous coronary intervention: a population model analysis. Br J Clin Pharmacol. 2005 Oct;60(4):364-73. [Article]
- Dalmora SL, Junior LB, Schmidt CA, Vaccari SF, Oliveira PR, Codevilla CF: Validation of the anti-factor Xa assay for the potency assessment of enoxaparin in pharmaceutical formulations. J AOAC Int. 2004 Nov-Dec;87(6):1305-8. [Article]
- Paige JT, Gouda BP, Gaitor-Stampley V, Scalia PG, Klainer TE, Raum WJ, Martin LF: No correlation between anti-factor Xa levels, low-molecular-weight heparin, and bleeding after gastric bypass. Surg Obes Relat Dis. 2007 Jul-Aug;3(4):469-75. Epub 2007 Jun 12. [Article]
- NIH StatPearls: Enoxaparin [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Thrombospondin receptor activity
- Specific Function
- Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostas...
- Gene Name
- F2
- Uniprot ID
- P00734
- Uniprot Name
- Prothrombin
- Molecular Weight
- 70036.295 Da
References
- Nutescu EA, Burnett A, Fanikos J, Spinler S, Wittkowsky A: Pharmacology of anticoagulants used in the treatment of venous thromboembolism. J Thromb Thrombolysis. 2016 Jan;41(1):15-31. doi: 10.1007/s11239-015-1314-3. [Article]
- Gikakis N, Rao AK, Miyamoto S, Gorman JH 3rd, Khan MM, Anderson HL, Hack CE, Sun L, Niewiarowski S, Colman RW, Edmunds LH Jr: Enoxaparin suppresses thrombin formation and activity during cardiopulmonary bypass in baboons. J Thorac Cardiovasc Surg. 1998 Dec;116(6):1043-51. doi: 10.1016/s0022-5223(98)70057-1. [Article]
- FDA Approved Drug Products: Lovenox (enoxaparin sodium injection), for subcutaneous and intravenous use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other
- Curator comments
- In vitro studies demonstrate that enoxaparin leads to the liberation of myeloperoxidase from the vascular wall, increasing plasma myeloperoxidase levels.
- General Function
- Peroxidase activity
- Specific Function
- Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
- Gene Name
- MPO
- Uniprot ID
- P05164
- Uniprot Name
- Myeloperoxidase
- Molecular Weight
- 83867.71 Da
References
- Rudolph TK, Rudolph V, Witte A, Klinke A, Szoecs K, Lau D, Heitzer T, Meinertz T, Baldus S: Liberation of vessel adherent myeloperoxidase by enoxaparin improves endothelial function. Int J Cardiol. 2010 Apr 1;140(1):42-7. doi: 10.1016/j.ijcard.2008.10.035. Epub 2008 Dec 2. [Article]
- Baldus S, Eiserich JP, Mani A, Castro L, Figueroa M, Chumley P, Ma W, Tousson A, White CR, Bullard DC, Brennan ML, Lusis AJ, Moore KP, Freeman BA: Endothelial transcytosis of myeloperoxidase confers specificity to vascular ECM proteins as targets of tyrosine nitration. J Clin Invest. 2001 Dec;108(12):1759-70. doi: 10.1172/JCI12617. [Article]
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Drug created on June 13, 2005 13:24 / Updated on July 23, 2021 16:03