Identification

Name
Heparin
Accession Number
DB01109  (APRD00056)
Type
Small Molecule
Groups
Approved, Investigational
Description

Unfractionated heparin (UH) is a heterogenous preparation of anionic, sulfated glycosaminoglycan polymers with weights ranging from 3000 to 30,000 Da. It is a naturally occurring anticoagulant released from mast cells. It binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. UH is different from low molecular weight heparin (LMWH) in the following ways: the average molecular weight of LMWH is about 4.5 kDa whereas it is 15 kDa for UH; UH requires continuous infusions; activated partial prothrombin time (aPTT) monitoring is required when using UH; and UH has a higher risk of bleeding and higher risk of osteoporosis in long term use. Unfractionated heparin is more specific than LMWH for thrombin. Furthermore, the effects of UH can typically be reversed by using protamine sulfate.

Synonyms
  • Calciparine
  • Eparina
  • heparina
  • Heparinate
  • Heparinic acid
  • Liquaemin
  • Panheprin
  • Unfractionated heparin
External IDs
CY216
Product Ingredients
IngredientUNIICASInChI Key
Heparin calciumM4F288ZCTR37270-89-6Not applicable
Heparin sodiumZZ45AB24CANot AvailableNot applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Calcilean Inj 20000unit/0.8mlLiquid20000 unitSubcutaneousOrganon Teknika Canada Inc.1987-12-311997-08-11Canada
Calciparine Inj 20000iu/ampLiquid20000 unitSubcutaneousChoay Lab1974-12-311998-06-09Canada
Calciparine Inj 5000iuLiquid5000 unitSubcutaneousChoay Lab1977-12-311998-06-09Canada
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02Us
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-06-28Us
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02Us
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02Us
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02Us
Hep-LockSolution100 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-06-28Us
Hep-LockSolution10 [USP'U]/1mLIntravenousBaxter Laboratories1972-03-222010-02-02Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Heparin Lock FlushInjection, solution100 [USP'U]/1mLIntravenousHospira, Inc.1943-04-272011-07-01Us
Heparin Lock FlushInjection, solution10 [USP'U]/1mLIntravenousHospira, Inc.1943-04-272011-03-01Us
Heparin SodiumInjection, solution5000 [USP'U]/1mLIntravenous; SubcutaneousCardinal Health2010-07-06Not applicableUs
Heparin SodiumInjection1000 [USP'U]/1mLIntravenous; SubcutaneousSandoz2011-06-08Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/1mLIntravenous; SubcutaneousSagent Pharmaceuticals2010-07-06Not applicableUs
Heparin SodiumInjection, solution5000 [USP'U]/1mLIntravenous; SubcutaneousSafecor Health, LLC2014-09-30Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/1mLIntravenous; SubcutaneousHospira, Inc.2009-08-31Not applicableUs
Heparin SodiumInjection, solution10000 [USP'U]/1mLIntravenous; SubcutaneousCardinal Health2009-12-07Not applicableUs
Heparin SodiumInjection20000 [USP'U]/1mLIntravenous; SubcutaneousSagent Pharmaceuticals2010-07-06Not applicableUs
Heparin SodiumInjection, solution1000 [USP'U]/1mLIntravenous; SubcutaneousCardinal Health2009-08-31Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Heparin Sod and 0.9% Sod Chloride InjHeparin (2 unit) + Sodium Chloride (9 mg)SolutionIntravenousBaxter Laboratories1990-12-31Not applicableCanada
Heparin Sodium & 5% Dextrose Injection LiqHeparin sodium (10000 unit) + Dextrose, unspecified form (5 g)SolutionIntravenousBaxter Laboratories1992-12-312011-02-01Canada
Heparin Sodium & Dextrose 5% In Viaflex LiqHeparin sodium (5000 unit) + Dextrose, unspecified form (5 g)SolutionIntravenousBaxter Laboratories1991-12-312011-02-01Canada
Heparin Sodium 1000units In 0.9% Sodium Chloride Injection USPHeparin sodium (200 unit) + Citric Acid (37 mg) + Sodium Chloride (900 mg) + Sodium phosphate, dibasic (430 mg)SolutionIntravenousB. Braun Medical Inc.1996-09-10Not applicableCanada
Heparin Sodium 20000units In 5% Dextrose InjHeparin sodium (4000 unit) + Dextrose, unspecified form (5 g)SolutionIntravenousB. Braun Medical Inc.1996-09-10Not applicableCanada
Heparin Sodium 25000units In 5% Dextrose InjHeparin sodium (10000 unit) + Dextrose, unspecified form (5 g)SolutionIntravenousB. Braun Medical Inc.1996-09-10Not applicableCanada
Heparin Sodium and Dextrose 5% Inj USPHeparin sodium (4000 unit) + Dextrose, unspecified form (5 g)LiquidIntravenousBaxter Laboratories1991-12-312011-02-01Canada
Heparin Sodium In 5% Dextrose Injection, 25000unit/500mlHeparin sodium (5000 unit) + Citric Acid (93 mg) + Dextrose, unspecified form (5 g) + Sodium phosphate, dibasic (410 mg)SolutionIntravenousB. Braun Medical Inc.1993-12-31Not applicableCanada
Heparin Sodium in DextroseHeparin sodium (4000 [USP'U]/100mL) + D-glucose monohydrate (5 g/100mL)InjectionIntravenousB. Braun Medical Inc.1992-07-20Not applicableUs
Heparin Sodium in DextroseHeparin sodium (10000 [USP'U]/100mL) + D-glucose monohydrate (5 g/100mL)InjectionIntravenousB. Braun Medical Inc.1992-07-20Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Heparin Lock FlushHeparin sodium (10 [USP'U]/1mL)Injection, solutionIntravenousAPP Pharmaceuticals, Inc.2009-08-29Not applicableUs
Heparin Lock FlushHeparin sodium (100 [USP'U]/1mL)Injection, solutionIntravenousAPP Pharmaceuticals, Inc.2009-08-12Not applicableUs
Heparin SodiumHeparin sodium (1 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2011-02-22Not applicableUs
Heparin SodiumHeparin sodium (100 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-05-09Not applicableUs
Heparin SodiumHeparin sodium (30 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2013-11-22Not applicableUs
Heparin SodiumHeparin sodium (50 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-08-09Not applicableUs
Heparin SodiumHeparin sodium (50 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-12-21Not applicableUs
Heparin SodiumHeparin sodium (4 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-11-13Not applicableUs
Heparin SodiumHeparin sodium (0.5 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-03-22Not applicableUs
Heparin SodiumHeparin sodium (10 [USP'U]/1mL)Injection, solutionIntravenousCantrell Drug Company2012-10-26Not applicableUs
International/Other Brands
Calcilean / Calciparine / Hep-lock / Hepalean / Heparin LEO / Liquaemin / Liquemin / Multiparin / Novoheparin
Categories
UNII
T2410KM04A
CAS number
9005-49-6
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Unfractionated heparin is indicated for prophylaxis and treatment of venous thrombosis and its extension, prevention of post-operative deep venous thrombosis and pulmonary embolism and prevention of clotting in arterial and cardiac surgery. In cardiology, it is used to prevent embolisms in patients with atrial fibrillation and as an adjunct antithrombin therapy in patients with unstable angina and/or non-Q wave myocardial infarctions (i.e. non-ST elevated acute coronary artery syndrome) who are on platelet glycoprotein (IIb/IIIa) receptor inhibitors. Additionally, it is used to prevent clotting during dialysis and surgical procedures, maintain the patency of intravenous injection devices and prevent in vitro coagulation of blood transfusions and in blood samples drawn for laboratory values.

Associated Conditions
Associated Therapies
Pharmacodynamics

Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from 3000 to 30,000 daltons. Heparin is obtained from liver, lung, mast cells, and other cells of vertebrates. Heparin is a well-known and commonly used anticoagulant which has antithrombotic properties. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Small amounts of heparin in combination with antithrombin III, a heparin cofactor,) can inhibit thrombosis by inactivating Factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor. Heparin prolongs several coagulation tests. Of all the coagulation tests, activated partial prothrombin time (aPTT) is the most clinically important value.

Mechanism of action

Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa. This process occurs at a slow rate. Administered heparin binds reversibly to ATIII and leads to almost instantaneous inactivation of factors IIa and Xa The heparin-ATIII complex can also inactivate factors IX, XI, XII and plasmin. The mechanism of action of heparin is ATIII-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Heparin is not a thrombolytic or fibrinolytic. It prevents progression of existing clots by inhibiting further clotting. The lysis of existing clots relies on endogenous thrombolytics.

TargetActionsOrganism
AAntithrombin-III
potentiator
Human
ACoagulation factor X
inhibitor
Human
UP-selectin
inhibitor
Human
UFibroblast growth factor receptor 4Not AvailableHuman
UFibroblast growth factor 4Not AvailableHuman
UFibroblast growth factor 19Not AvailableHuman
UFibroblast growth factor receptor 1Not AvailableHuman
UFibroblast growth factor 1Not AvailableHuman
UFibroblast growth factor receptor 2Not AvailableHuman
UFibroblast growth factor 2Not AvailableHuman
UPlatelet factor 4Not AvailableHuman
UHepatocyte growth factorNot AvailableHuman
Absorption

Heparin must be given parenterally as it is not absorbed through the gastrointestinal mucosa. It is usually given by iv infusion or deep sc injection. The onset of action is immediate after iv injection but can be delayed 20 to 60 minutes following sc injection.

Plasma heparin concentrations may be increased and activated partial thromboplastin times (aPTTs) may be more prolonged in geriatric adults (older than 60 years of age) compared with younger adults.

Volume of distribution

40-70 mL/min (approximately the same as blood volume) Although heparin does not distribute into adipose tissues, clinicians should use actual body weight in obese patients to account for extra vasculature.

Protein binding

Very high, mostly to low-density lipoproteins. It is also extensively bound by globulins and fibrinogens.

Metabolism

Liver and the reticulo-endothelial system are the sites of biotransformation. The metabolic fate of heparin is not well understood.

Route of elimination

The drug appears to be removed mainly by the reticuloendothelial system. A small fraction of unchanged heparin also appears to be excreted in urine. Heparin cannot be eliminated by hemodialysis.

Half life

1.5 hours.

The plasma half-life of heparin increases from about 60 minutes with a 100 unit/kg dose to about 150 minutes with a 400 unit/kg dose.

Clearance

Adult Clearance = 0.43 ml/kg/min 25-28 weeks gestation = 1.49 ml/kg/min

Toxicity

In mouse, the median lethal dose is greater than 5000 mg/kg. Another side effect is heparin-induced thrombocytopenia (HIT syndrome). Platelet counts usually do not fall until between days 5 and 12 of heparin therapy. HIT is caused by an immunological reaction that makes platelets form clots within the blood vessels, thereby using up coagulation factors. It can progress to thrombotic complications such as arterial thrombosis, gangrene, stroke, myocardial infarction and disseminated intravascular coagulation. Symptoms of overdose may show excessive prolongation of aPTT or by bleeding, which may be internal or external, major or minor. Therapeutic doses of heparin give for at least 4 months have been associated with osteoporosis and spontaneous vertebral fractures. Osteoporosis may be reversible once heparin is discontinued. Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity in neonates. Toxicity appears to have resulted from administration of large amounts (i.e., about 100–400 mg/kg daily) of benzyl alcohol in these neonates. Its use is principally associated with the use of bacteriostatic 0.9% sodium chloride intravascular flush or endotracheal tube lavage solutions.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Fc Epsilon Receptor I Signaling in Mast CellsSignaling
Heparin Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(1,2,6,7-3H)TestosteroneThe therapeutic efficacy of Heparin can be increased when used in combination with (1,2,6,7-3H)Testosterone.
(R)-warfarinThe risk or severity of bleeding can be increased when Heparin is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of bleeding can be increased when Heparin is combined with (S)-Warfarin.
1-TestosteroneThe therapeutic efficacy of Heparin can be increased when used in combination with 1-Testosterone.
18-methyl-19-nortestosteroneThe therapeutic efficacy of Heparin can be increased when used in combination with 18-methyl-19-nortestosterone.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when Heparin is combined with 4-hydroxycoumarin.
4-HydroxytestosteroneThe therapeutic efficacy of Heparin can be increased when used in combination with 4-Hydroxytestosterone.
5beta-dihydrotestosteroneThe therapeutic efficacy of Heparin can be increased when used in combination with 5beta-dihydrotestosterone.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Heparin.
AcebutololThe risk or severity of hyperkalemia can be increased when Heparin is combined with Acebutolol.
Food Interactions
  • Adequate calcium intake is recommended, needs increased with long term use, supplement recommended.
  • Many herbs with anticoagulant properties (e.g. ginger, garlic, ginseng, green tea, evening primrose) may increase the risk of bleeding in patients on anticoagulant therapy such as heparin

References

Synthesis Reference

Fernando Fussi, Gianfranco Fedeli, "Oligo-heteropolysaccharides having a heparin-like activity method for their preparation and pharmaceutical compositions based thereon." U.S. Patent US4757057, issued June, 1952.

US4757057
General References
  1. Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16. [PubMed:10549711]
  2. Ferro DR, Provasoli A, Ragazzi M, Casu B, Torri G, Bossennec V, Perly B, Sinay P, Petitou M, Choay J: Conformer populations of L-iduronic acid residues in glycosaminoglycan sequences. Carbohydr Res. 1990 Jan 15;195(2):157-67. [PubMed:2331699]
  3. Mulloy B, Forster MJ, Jones C, Davies DB: N.m.r. and molecular-modelling studies of the solution conformation of heparin. Biochem J. 1993 Aug 1;293 ( Pt 3):849-58. [PubMed:8352752]
  4. Hirsh J, Raschke R: Heparin and low-molecular-weight heparin: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest. 2004 Sep;126(3 Suppl):188S-203S. [PubMed:15383472]
  5. Petitou M, Herault JP, Bernat A, Driguez PA, Duchaussoy P, Lormeau JC, Herbert JM: Synthesis of thrombin-inhibiting heparin mimetics without side effects. Nature. 1999 Apr 1;398(6726):417-22. [PubMed:10201371]
  6. Spruill WJ, Wade WE, Huckaby WG, Leslie RB: Achievement of anticoagulation by using a weight-based heparin dosing protocol for obese and nonobese patients. Am J Health Syst Pharm. 2001 Nov 15;58(22):2143-6. [PubMed:11760916]
  7. McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8. [PubMed:7254945]
  8. Authors unspecified: Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983 Sep;72(3):356-8. [PubMed:6889041]
  9. Authors unspecified: Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982 Aug;12(2):10-1. [PubMed:7188569]
  10. Authors unspecified: Neonatal deaths associated with use of benzyl alcohol--United States. MMWR Morb Mortal Wkly Rep. 1982 Jun 11;31(22):290-1. [PubMed:6810084]
External Links
KEGG Compound
C00374
PubChem Substance
46507594
ChEBI
28304
ChEMBL
CHEMBL1909300
Therapeutic Targets Database
DAP000189
PharmGKB
PA449855
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Heparin
ATC Codes
S01XA14 — HeparinC05BA03 — HeparinC05BA53 — Heparin, combinationsB01AB51 — Heparin, combinationsB01AB01 — Heparin
AHFS Codes
  • 20:12.04.16 — Heparins
  • 92:00.00 — Miscellaneous Therapeutic Agents
FDA label
Download (198 KB)
MSDS
Download (72.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceAltered Heparin Response / Cardiopulmonary Bypass1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedPreventionExtracorporeal Membrane Oxygenation Complication1
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentOral Mucositis1
1CompletedTreatmentSystemic Embolism / Thrombophlebitis1
1Not Yet RecruitingTreatmentExtracorporeal Membrane Oxygenation Complication1
1Not Yet RecruitingTreatmentRenal Failure1
1RecruitingTreatmentType1 Diabetes Mellitus1
1Unknown StatusTreatmentEnd-Stage Renal Disease (ESRD) / Hemodialysis Catheter-Associated Infection1
1Unknown StatusTreatmentHealthy Volunteers3
1, 2CompletedOtherHealthy Volunteers1
1, 2CompletedTreatmentAntithrombotic1
1, 2RecruitingPreventionThoracic Surgery / Thromboprophylaxis1
1, 2TerminatedPreventionBloodstream Infection Due to Central Venous Catheter / Bloodstream Infection Due to Hickman Catheter / Catheter-related Bloodstream Infection (CRBSI) Nos / Catheter-related Bloodstream Infection Due to Central Venous Catheter1
1, 2TerminatedTreatmentMultiple Myeloma (MM) / Plasma Cell Neoplasms1
2CompletedBasic ScienceMalignant Lymphomas / Multiple Myeloma (MM)1
2CompletedPreventionCoronary Artery Disease / Percutaneous Coronary Intervention (PCI)1
2CompletedPreventionNonvalvular Atrial Fibrillation1
2CompletedTreatmentAcute Coronary Syndromes (ACS)1
2CompletedTreatmentAngioplasty, Transluminal, Percutaneous Coronary1
2CompletedTreatmentCoronary Artery Disease1
2CompletedTreatmentCoronary Artery Disease / Unstable Angina (UA)1
2CompletedTreatmentCoronary Heart Disease (CHD)1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
2CompletedTreatmentHeart Catheterization1
2CompletedTreatmentShock, Cardiogenic1
2CompletedTreatmentShock, Septic1
2Not Yet RecruitingPreventionCentral Venous Catheter Associated Bloodstream Infection / Central Venous Catheter Thrombosis1
2Not Yet RecruitingPreventionLower Urinary Tract Symptoms (LUTS) / Postoperative Urinary Tract Infection1
2Not Yet RecruitingTreatmentCerebral Venous Thrombosis1
2RecruitingTreatmentAcute Circulatory Failure / Shock, Septic1
2RecruitingTreatmentAneurysmal Subarachnoid Hemorrhage / Heparin-induced Thrombocytopenia Type II / Intracranial Aneurysms / Neurobehavioral Manifestations / Vasospasm, Intracranial1
2RecruitingTreatmentBladder Pain Syndrome / Interstitial Cystitis1
2TerminatedTreatmentAcute Chest Syndrome / Sickle Cell Disorders1
2Unknown StatusPreventionEmbolic Stroke1
2WithdrawnTreatmentCoronary Heart Disease (CHD) / Myocardial Infarction1
2WithdrawnTreatmentDiabetes, Diabetes Mellitus Type 11
2WithdrawnTreatmentSepsis1
2, 3CompletedPreventionDeep Vein Thrombosis (DVT)1
2, 3CompletedPreventionDeep Venous Thrombosis1
2, 3CompletedTreatmentInfertilities1
2, 3TerminatedTreatmentSinus Thrombosis, Intracranial1
2, 3Unknown StatusPreventionDeep Vein Thrombosis (DVT) / Pulmonary Embolism (PE)1
2, 3WithdrawnTreatmentMinor burns1
3CompletedNot AvailableCardiovascular Disease (CVD) / Thrombosis, Venous / Venous Thromboembolism (VTE)1
3CompletedPreventionCritical Illness / Deep Venous Thrombosis1
3CompletedPreventionDiagnostic Coronary Angiography1
3CompletedPreventionHaemorrhage1
3CompletedPreventionRecurrent Miscarriages / Recurrent Pregnancy Losses1
3CompletedPreventionRenal Dialysis1
3CompletedPreventionSystemic Embolism1
3CompletedPreventionThromboembolism1
3CompletedPreventionThrombosis, Venous1
3CompletedPreventionVenous Thromboembolism (VTE)2
3CompletedTreatmentAcute Coronary Syndromes (ACS)2
3CompletedTreatmentAcute Deep Vein Thrombosis / Thrombosis, Venous1
3CompletedTreatmentAcute Myocardial Infarction (AMI)1
3CompletedTreatmentAcute Pulmonary Thromboembolism / Pulmonary Embolism (PE)1
3CompletedTreatmentAcute Respiratory Distress Syndrome (ARDS) / Severe Acute Respiratory Syndrome1
3CompletedTreatmentAngina Pectoris / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Infarction / Myocardial Ischemia1
3CompletedTreatmentAngioplasty, Transluminal, Percutaneous Coronary2
3CompletedTreatmentCardiovascular Disease (CVD) / Coronary Artery Bypass Graft Surgery Patients1
3CompletedTreatmentCarotid Artery Dissection / Cervical Artery Dissection / Strokes / Vertebral Artery Dissection1
3CompletedTreatmentCoronary Artery Bypass Graft Surgery Patients / Surgery, Cardiac1
3CompletedTreatmentDeep Vein Thrombosis (DVT)2
3CompletedTreatmentDeep Vein Thrombosis (DVT) / Pulmonary Embolism (PE)1
3CompletedTreatmentDeep Venous Thrombosis1
3CompletedTreatmentMyocardial Infarction2
3CompletedTreatmentPatients With Acute Renal Insufficiency1
3CompletedTreatmentPersistent Nonvalvular Atrial Fibrillation1
3CompletedTreatmentPostoperative Hemorrhages1
3CompletedTreatmentPrimary PCI - STEMI1
3CompletedTreatmentPulmonary Embolism (PE)1
3CompletedTreatmentSevere Sepsis With Septic Shock / Severe Sepsis Without Septic Shock1
3CompletedTreatmentSubmassive Pulmonary Embolism1
3CompletedTreatmentThrombosis, Venous1
3Not Yet RecruitingTreatmentDisseminated Intravascular Coagulation (DIC) / Sepsis1
3Not Yet RecruitingTreatmentIntrauterine Growth Restriction1
3RecruitingPreventionAdenocarcinoma of the Colon1
3RecruitingPreventionAnticoagulant Drugs / Cardiac Diseases1
3RecruitingPreventionCatheter-Related Infections / Chronic Renal Failure (CRF)1
3RecruitingTreatmentAcute Myocardial Infarction (AMI)1
3RecruitingTreatmentDeep Vein Thrombosis (DVT) / Pulmonary Embolism (PE) / Venous Thromboembolism (VTE)1
3RecruitingTreatmentImpaired Renal Function1
3SuspendedPreventionMalignant Female Reproductive System Neoplasm1
3TerminatedPreventionAplastic Anaemia (AA) / Childhood Cancers / Metabolic Disorders1
3TerminatedTreatmentAcute Myocardial Infarction (AMI)1
3TerminatedTreatmentBurn Injuries / Inhalation Injury1
3TerminatedTreatmentFibrinolysis / Hemodilution / Retinal Artery Occlusions / Strokes / Visual Acuity1
3TerminatedTreatmentPercutaneous Coronary Intervention1
3TerminatedTreatmentRetinal Vein Occlusions(RVO)1
3Unknown StatusPreventionChronic Renal Failure (CRF)1
3Unknown StatusPreventionEnd Stage Renal Disease (ESRD)1
3Unknown StatusPreventionFrom Surgery in the Two Study Groups / Prophylaxis Given for 8±2 Days After Planned Laparoscopic / Safety of Extended 4-week Heparin Prophylaxis Compared to / Surgery for Colorectal Cancer / The Clinical Benefit Will be Evaluated as the Difference in / The Incidence of VTE or VTE-related Death Occurring Within 30 Days / The Primary Study Objective is to Assess the Efficacy and1
3Unknown StatusTreatmentTo Investigate the Effects of Low Dose Aspirin and Low Molecular Weight Heparin in IVF Out Come1
3WithdrawnTreatmentHeparin1
3WithdrawnTreatmentRecent Obstructive Portal Vein Thrombosis / Thrombosis Portal Vein1
4Active Not RecruitingPreventionCatheter-Related Infections1
4CompletedNot AvailableRenal Insufficiency, Acute1
4CompletedNot AvailableVenous Thromboembolism (VTE)1
4CompletedDiagnosticInsulin Resistance Syndrome X / Pancreatic Beta Cell Function1
4CompletedDiagnosticMesenteric vascular insufficiency1
4CompletedPreventionAnticoagulation / Cardiopulmonary Bypass / Surgery, Cardiac1
4CompletedPreventionArteriovenous Fistulas1
4CompletedPreventionCatheter Related Infections1
4CompletedPreventionChronic Renal Failure (CRF)1
4CompletedPreventionCirculation, Extracorporeal / Surgery, Cardiac1
4CompletedPreventionDeep Vein Thrombosis (DVT) / Osteoarthritis (OA)1
4CompletedTreatmentAcute Coronary Syndromes (ACS)2
4CompletedTreatmentAcute Myocardial Infarction (AMI) / Percutaneous Coronary Intervention1
4CompletedTreatmentAcute Renal Failure (ARF)1
4CompletedTreatmentBruises1
4CompletedTreatmentCVD1
4CompletedTreatmentCoronary Artery Disease3
4CompletedTreatmentCoronary Heart Disease (CHD) / Myocardial Infarction1
4CompletedTreatmentDeep Vein Thrombosis (DVT)1
4CompletedTreatmentHeart Disease, Ischemic1
4CompletedTreatmentHypercoagulability / Pregnancy1
4CompletedTreatmentNon ST Segment Elevation Myocardial Infarction (NSTEMI) / ST Segment Elevation Myocardial Infarction (STEMI)1
4CompletedTreatmentPulmonary Embolism (PE) / Thromboembolism / Thrombotic events / Vascular Diseases1
4CompletedTreatmentST Elevation Acute Myocardial Infarction1
4CompletedTreatmentSepsis1
4CompletedTreatmentSelective coronary arteriography1
4Not Yet RecruitingDiagnosticHaemorrhage / Heparin / Heparin overdose1
4Not Yet RecruitingTreatmentCoronary Heart Disease (CHD)1
4Not Yet RecruitingTreatmentST Elevation Myocardial Infarction (STEMI)1
4RecruitingPreventionDeep Venous Thrombosis / Lymphocele After Surgical Procedure / Prostate Cancer / Pulmonary Embolism (PE) / Venous Thromboembolism (VTE)1
4RecruitingSupportive CareHaemorrhage / Myocardial Infarction / Strokes / Venous Thromboembolism (VTE)1
4RecruitingTreatmentAcute Kidney Injury (AKI)1
4RecruitingTreatmentAcute Kidney Injury (AKI) / Acute Renal Failure (ARF) / Heart Failure, Unspecified1
4RecruitingTreatmentAnticoagulants / Extracorporeal Membrane Oxygenation Complication / Pediatric ALL1
4RecruitingTreatmentCoronary Artery Disease1
4RecruitingTreatmentEndstage Renal Disease1
4RecruitingTreatmentIschaemic Heart Diseases1
4RecruitingTreatmentRecurrent Pregnancy Losses1
4RecruitingTreatmentThrombophilia With Recurrent Pregnancy Loss1
4SuspendedPreventionTraumatic Brain Injury (TBI) / Venous Thromboembolism (VTE)1
4TerminatedNot AvailableMalignancies / Venous Thromboembolism (VTE)1
4TerminatedPreventionVenous Thromboembolism (VTE)1
4TerminatedTreatmentAortic Stenosis, Non-rheumatic1
4TerminatedTreatmentCoronary Artery Disease1
4TerminatedTreatmentMyocardial Infarction / Unstable Angina (UA)1
4Unknown StatusPreventionBypass Complications / Obesity, Morbid / Thromboembolism1
4Unknown StatusPreventionHemorrhage / Respiration, Artificial1
4Unknown StatusTreatmentAbortions spontaneous / Pregnancy1
4Unknown StatusTreatmentAcute Ischemic Stroke (AIS)1
4Unknown StatusTreatmentAcute Kidney Injury (AKI) / Hemodialysis Treatment1
4Unknown StatusTreatmentCoronary Artery Disease1
4Unknown StatusTreatmentMyocardial Infarction1
4WithdrawnPreventionDiabetes Mellitus (DM) / Hemodialysis Treatment1
Not AvailableActive Not RecruitingNot AvailableDeep Venous Thrombosis, Protection Against / Renal Insufficiency,Chronic1
Not AvailableActive Not RecruitingNot AvailableLipoprotein Lipase Deficiency1
Not AvailableCompletedNot AvailableCerebral Artery Anuerysm / Neoplasms, Brain / Spinal Stenosis1
Not AvailableCompletedNot AvailableMalignant Lymphomas / Thromboembolism / Unspecified Adult Solid Tumor, Protocol Specific1
Not AvailableCompletedNot AvailableThrombosis, Venous1
Not AvailableCompletedNot AvailableThrombotic events1
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Leptin Resistance1
Not AvailableCompletedPreventionCicatrix1
Not AvailableCompletedPreventionDeep Vein Thrombosis (DVT) / Malignancies / Pulmonary Embolism (PE)1
Not AvailableCompletedPreventionDouble Lumen Infection / Hemodialysis Treatment1
Not AvailableCompletedPreventionPrimary Brain Tumors1
Not AvailableCompletedPreventionThrombosis, Venous1
Not AvailableCompletedPreventionThrombotic events1
Not AvailableCompletedSupportive CareMultiple Myeloma (MM)1
Not AvailableCompletedSupportive CareOff Pump Coronary Artery Bypass Surgery1
Not AvailableCompletedTreatmentAngioedema1
Not AvailableCompletedTreatmentCoronary Artery Bypass Graft Surgery Patients1
Not AvailableCompletedTreatmentFatty Acids, Nonesterified / Glomerular Filtration Rate (GFR) / Renal Circulation / Renal Plasma Flow1
Not AvailableCompletedTreatmentGlucocorticoid Metabolism / Hyperandrogenism1
Not AvailableCompletedTreatmentPeripheral Revascularisation1
Not AvailableCompletedTreatmentThrombotic events1
Not AvailableEnrolling by InvitationNot AvailableBMI >30 kg/m2 / Insulin Resistance1
Not AvailableEnrolling by InvitationTreatmentAcute DVT of Lower Extremity1
Not AvailableNo Longer AvailableNot AvailableDiabetes, Diabetes Mellitus Type 11
Not AvailableNot Yet RecruitingTreatmentCatheter Thrombosis / Hemodialysis Catheter Infection1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Pressure (Hypertension) / High Cholesterol / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain NOS / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombotic events / Toxic effect of hydrocyanic acid and cyanides / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingNot AvailableEmbolism and Thrombosis of the Radial Artery1
Not AvailableRecruitingNot AvailableHemostatic Disorders1
Not AvailableRecruitingNot AvailableIntra Operative Bleeding, Blood Salvage1
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Hyperinsulinemia / Hypogonadotropic Hypogonadotropism / Infertilities1
Not AvailableRecruitingBasic ScienceCarnitine Palmitoyltransferase II Deficiency, Myopathic / Long-Chain 3-Hydroxyacyl-CoA Dehydrogenase Deficiency / Medium-chain Acyl-CoA Dehydrogenase Deficiency / Normal Volunteers / Trifunctional Protein Deficiency / Very Long-chain Acyl-CoA Dehydrogenase Deficiency1
Not AvailableRecruitingSupportive CareAcute Respiratory Failure / Extracorporeal Membrane Oxygenation Complication / Haemorrhage1
Not AvailableRecruitingTreatmentArteriovenous Malformations / Cerebral Aneurysms1
Not AvailableRecruitingTreatmentBMI >30 kg/m2 / Cardiopulmonary Bypass1
Not AvailableRecruitingTreatmentChronic Stable Angina Pectoris / Refractory Angina1
Not AvailableRecruitingTreatmentSecond Degree Burns1
Not AvailableTerminatedNot AvailableInflammatory Reaction / Nutrition / Peritoneal dialysis therapy1
Not AvailableTerminatedDiagnosticCoagulation, Blood / Compression Devices, Intermittent Pneumatic / Postoperative Complications / Thrombelastography1
Not AvailableTerminatedTreatmentPulmonary Embolism (PE) / Thrombosis, Venous1
Not AvailableUnknown StatusTreatmentAnginal Pain / BMI >30 kg/m2 / Nonvalvular Atrial Fibrillation / Obesity, Morbid / Thoracic Pain / Venous Thromboembolism (VTE)1
Not AvailableUnknown StatusTreatmentShock, Septic1
Not AvailableWithdrawnPreventionAnticoagulants / Infants, Premature / Thrombotic events1
Not AvailableWithdrawnPreventionCarotid Artery Injury / Vertebral Artery Injury1
Not AvailableWithdrawnPreventionLower Extremity Deep Venous Thrombosis1
Not AvailableWithdrawnSupportive CareMalignancies1
Not AvailableWithdrawnTreatmentAnaphylactic-type reactions1
Not AvailableWithdrawnTreatmentVenous Thromboembolism (VTE)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amerisource Health Services Corp.
  • Amsino Medical Usa
  • APP Pharmaceuticals
  • B. Braun Melsungen AG
  • Baxter International Inc.
  • Becton Dickinson
  • Bioiberica Sa
  • Cardinal Health
  • Eisai Inc.
  • General Injectables and Vaccines Inc.
  • Hospira Inc.
  • Mason Distributors
  • Medefil Inc.
  • Medical Techniques LLC
  • Neuman Distributors Inc.
  • Pfizer Inc.
  • Pharmacia Inc.
  • Sagent Pharmaceuticals
  • Sandhills Packaging Inc.
  • Spectrum Pharmaceuticals
  • Tyco Healthcare Group LP
  • Vetter Pharma Fertigung GmbH and Co. KG
Dosage forms
FormRouteStrength
LiquidSubcutaneous20000 unit
LiquidSubcutaneous5000 unit
SolutionIntravenous10 [USP'U]/1mL
SolutionIntravenous100 [USP'U]/1mL
SolutionIntravenous; Subcutaneous25000 unit
SolutionIntravenous10 unit
SolutionIntravenous100 unit
Injection, solutionIntravenous100 1/1mL
LiquidIrrigation100 unit
LiquidIntravenous; Subcutaneous10000 unit
LiquidIntravenous; Subcutaneous1000 unit
LiquidIntravenous; Subcutaneous25000 unit
Injection, solutionIntravenous10 [USP'U]/1mL
Injection, solutionIntravenous100 [USP'U]/1mL
SolutionIntraperitoneal10 unit
SolutionIntravenous; Irrigation10 unit
SolutionIntravenous; Irrigation100 unit
SolutionIntravenous
InjectionIntravenous; Subcutaneous1000
InjectionIntravenous; Subcutaneous1000 [USP'U]/1mL
InjectionIntravenous; Subcutaneous10000
InjectionIntravenous; Subcutaneous10000 [USP'U]/1mL
InjectionIntravenous; Subcutaneous20000 [USP'U]/1mL
InjectionIntravenous; Subcutaneous5000 [USP'U]/1mL
Injection, solutionIntravenous0.5 [USP'U]/1mL
Injection, solutionIntravenous1 [USP'U]/1mL
Injection, solutionIntravenous10000 [USP'U]/100mL
Injection, solutionIntravenous2 [USP'U]/1mL
Injection, solutionIntravenous200 [USP'U]/100mL
Injection, solutionIntravenous30 [USP'U]/1mL
Injection, solutionIntravenous4 [USP'U]/1mL
Injection, solutionIntravenous40 [USP'U]/1mL
Injection, solutionIntravenous4000 [USP'U]/100mL
Injection, solutionIntravenous5 [USP'U]/1mL
Injection, solutionIntravenous50 [USP'U]/1mL
Injection, solutionIntravenous5000 [USP'U]/100mL
Injection, solutionIntravenous; Subcutaneous1000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous1000
Injection, solutionIntravenous; Subcutaneous10000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous10000
Injection, solutionIntravenous; Subcutaneous20000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous5000 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous5000
Injection, solutionIntravenous; Subcutaneous5000 [USP'U]/0.5mL
Injection, solution, concentrateIntravenous10000 [USP'U]/5mL
Injection, solution, concentrateIntravenous12500
Injection, solution, concentrateIntravenous20000
Injection, solution, concentrateIntravenous25000 [USP'U]/10mL
SolutionIntravenous40 unit
SolutionIntravenous50 unit
LiquidIntravenous
SolutionIntravenous2 unit
InjectionIntravenous
InjectionIntravenous200 [USP'U]/100mL
SolutionIntravenous; Subcutaneous5000 unit
SolutionSubcutaneous5000 unit
SolutionIntravenous; Subcutaneous10000 unit
SolutionIntravenous; Subcutaneous1000 unit
Prices
Unit descriptionCostUnit
Heparin sod 1000000 unit powder1318.63USD each
Heparin sod 100000 unit powder256.73USD each
Heparin Sodium (Porcine) 1000 unit/ml Solution 10ml Vial188.99USD vial
Heparin sod 25000 unit powder58.8USD each
Heparin Sodium (Porcine) 10000 unit/ml Solution 5ml Vial29.99USD vial
Heparin Sodium (Porcine) 10000 unit/ml vial10.37USD vial
Hep-lock flush 100 unit/ml kit10.08USD kit
Hep-lock flush 10 unit/ml kit8.91USD kit
Heparin Leo 25000 unit/ml8.42USD ml
Heparin sod 1000 unit/ml vial7.92USD ml
Heparin sod 5000 unit/ml syringe3.08USD ml
Heparin iv flush 100 unit/ml2.71USD ml
Hepalean 10000 unit/ml2.32USD ml
Heparin Leo 10000 unit/ml2.03USD ml
Heparin lock flush 10 unit/ml1.21USD ml
Heparin lock flush 100 unit/ml1.13USD ml
Hep-lock u-p 10 unit/ml vial0.98USD ml
Hepalean 1000 unit/ml0.98USD ml
Hep-lock u-p 100 unit/ml vial0.96USD ml
Heparin Leo 1000 unit/ml0.43USD ml
Heparin Leo 100 unit/ml Lock Flush0.36USD ml
Heparin Lock Flush 100 unit/ml Lock Flush0.3USD ml
Heparin Lock Flush 10 unit/ml Lock Flush0.29USD ml
Heparin iv flush 1 unit/ml syr0.19USD ml
Heparin iv flush 2 unit/ml syr0.19USD ml
Heparin lock 100 unit/ml vial0.13USD ml
Heparin lock 10 unit/ml vial0.1USD ml
Heparin-1/2ns 25000 unit/2500.03USD ml
Heparin-1/2ns 12500 unit/2500.02USD ml
Heparin-ns 2000 unit/1000 ml0.01USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP-13.2Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
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
  1. Mirow N, Zimmermann B, Maleszka A, Knobl H, Tenderich G, Koerfer R, Herberg FW: Plasma protein binding properties to immobilized heparin and heparin-albumin conjugate. Artif Organs. 2007 Jun;31(6):466-71. [PubMed:17537059]
  2. Sun W, Bandmann H, Schrader T: A fluorescent polymeric heparin sensor. Chemistry. 2007;13(27):7701-7. [PubMed:17600786]
  3. Pappalardo F, Franco A, Crescenzi G, De Simone F, Torracca L, Zangrillo A: Anticoagulation management in patients undergoing open heart surgery by activated clotting time and whole blood heparin concentration. Perfusion. 2006 Dec;21(5):285-90. [PubMed:17201083]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  5. Chuang YJ, Swanson R, Raja SM, Olson ST: Heparin enhances the specificity of antithrombin for thrombin and factor Xa independent of the reactive center loop sequence. Evidence for an exosite determinant of factor Xa specificity in heparin-activated antithrombin. J Biol Chem. 2001 May 4;276(18):14961-71. Epub 2001 Feb 7. [PubMed:11278930]
  6. Petitou M, Herault JP, Bernat A, Driguez PA, Duchaussoy P, Lormeau JC, Herbert JM: Synthesis of thrombin-inhibiting heparin mimetics without side effects. Nature. 1999 Apr 1;398(6726):417-22. [PubMed:10201371]
  7. Schedin-Weiss S, Richard B, Olson ST: Kinetic evidence that allosteric activation of antithrombin by heparin is mediated by two sequential conformational changes. Arch Biochem Biophys. 2010 Dec 15;504(2):169-76. doi: 10.1016/j.abb.2010.08.021. Epub 2010 Sep 15. [PubMed:20816747]
  8. Gettins PG, Olson ST: Activation of antithrombin as a factor IXa and Xa inhibitor involves mitigation of repression rather than positive enhancement. FEBS Lett. 2009 Nov 3;583(21):3397-400. doi: 10.1016/j.febslet.2009.10.005. Epub 2009 Oct 9. [PubMed:19818773]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
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
  1. Ignjatovic V, Summerhayes R, Gan A, Than J, Chan A, Cochrane A, Bennett M, Horton S, Shann F, Lane G, Ross-Smith M, Monagle P: Monitoring Unfractionated Heparin (UFH) therapy: which Anti-Factor Xa assay is appropriate? Thromb Res. 2007;120(3):347-51. Epub 2006 Nov 21. [PubMed:17118432]
  2. Patey SJ, Edwards EA, Yates EA, Turnbull JE: Heparin derivatives as inhibitors of BACE-1, the Alzheimer's beta-secretase, with reduced activity against factor Xa and other proteases. J Med Chem. 2006 Oct 5;49(20):6129-32. [PubMed:17004727]
  3. Rezaie AR: Heparin-binding exosite of factor Xa. Trends Cardiovasc Med. 2000 Nov;10(8):333-8. [PubMed:11369259]
  4. Rosenberg RD: Role of heparin and heparinlike molecules in thrombosis and atherosclerosis. Fed Proc. 1985 Feb;44(2):404-9. [PubMed:3155697]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sialic acid binding
Specific Function
Ca(2+)-dependent receptor for myeloid cells that binds to carbohydrates on neutrophils and monocytes. Mediates the interaction of activated endothelial cells or platelets with leukocytes. The ligan...
Gene Name
SELP
Uniprot ID
P16109
Uniprot Name
P-selectin
Molecular Weight
90833.105 Da
References
  1. Simonis D, Fritzsche J, Alban S, Bendas G: Kinetic analysis of heparin and glucan sulfates binding to P-selectin and its impact on the general understanding of selectin inhibition. Biochemistry. 2007 May 22;46(20):6156-64. Epub 2007 Apr 26. [PubMed:17458940]
  2. Maugeri N, Di Fabio G, Barbanti M, de Gaetano G, Donati MB, Cerletti C: Parnaparin, a low-molecular-weight heparin, prevents P-selectin-dependent formation of platelet-leukocyte aggregates in human whole blood. Thromb Haemost. 2007 Jun;97(6):965-73. [PubMed:17549299]
  3. Simonis D, Christ K, Alban S, Bendas G: Affinity and kinetics of different heparins binding to P- and L-selectin. Semin Thromb Hemost. 2007 Jul;33(5):534-9. [PubMed:17629851]
  4. Asberg AE, Videm V: Inhibition of platelet receptors involved in neutrophil-platelet interaction in model cardiopulmonary bypass. Artif Organs. 2007 Aug;31(8):617-26. [PubMed:17651117]
  5. Gao Y, Li N, Fei R, Chen Z, Zheng S, Zeng X: P-Selectin-mediated acute inflammation can be blocked by chemically modified heparin, RO-heparin. Mol Cells. 2005 Jun 30;19(3):350-5. [PubMed:15995351]
  6. Koenig A, Norgard-Sumnicht K, Linhardt R, Varki A: Differential interactions of heparin and heparan sulfate glycosaminoglycans with the selectins. Implications for the use of unfractionated and low molecular weight heparins as therapeutic agents. J Clin Invest. 1998 Feb 15;101(4):877-89. [PubMed:9466983]
  7. Nelson RM, Cecconi O, Roberts WG, Aruffo A, Linhardt RJ, Bevilacqua MP: Heparin oligosaccharides bind L- and P-selectin and inhibit acute inflammation. Blood. 1993 Dec 1;82(11):3253-8. [PubMed:7694675]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation o...
Gene Name
FGFR4
Uniprot ID
P22455
Uniprot Name
Fibroblast growth factor receptor 4
Molecular Weight
87953.535 Da
References
  1. Loo BM, Kreuger J, Jalkanen M, Lindahl U, Salmivirta M: Binding of heparin/heparan sulfate to fibroblast growth factor receptor 4. J Biol Chem. 2001 May 18;276(20):16868-76. Epub 2001 Feb 21. [PubMed:11278860]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Heparin binding
Specific Function
Plays an important role in the regulation of embryonic development, cell proliferation, and cell differentiation. Required for normal limb and cardiac valve development during embryogenesis.
Gene Name
FGF4
Uniprot ID
P08620
Uniprot Name
Fibroblast growth factor 4
Molecular Weight
22047.355 Da
References
  1. Bellosta P, Iwahori A, Plotnikov AN, Eliseenkova AV, Basilico C, Mohammadi M: Identification of receptor and heparin binding sites in fibroblast growth factor 4 by structure-based mutagenesis. Mol Cell Biol. 2001 Sep;21(17):5946-57. [PubMed:11486033]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Fibroblast growth factor receptor binding
Specific Function
Involved in the suppression of bile acid biosynthesis through down-regulation of CYP7A1 expression, following positive regulation of the JNK and ERK1/2 cascades. Stimulates glucose uptake in adipoc...
Gene Name
FGF19
Uniprot ID
O95750
Uniprot Name
Fibroblast growth factor 19
Molecular Weight
24002.345 Da
References
  1. Harmer NJ, Pellegrini L, Chirgadze D, Fernandez-Recio J, Blundell TL: The crystal structure of fibroblast growth factor (FGF) 19 reveals novel features of the FGF family and offers a structural basis for its unusual receptor affinity. Biochemistry. 2004 Jan 27;43(3):629-40. [PubMed:14730967]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation ...
Gene Name
FGFR1
Uniprot ID
P11362
Uniprot Name
Fibroblast growth factor receptor 1
Molecular Weight
91866.935 Da
References
  1. Ibrahimi OA, Zhang F, Hrstka SC, Mohammadi M, Linhardt RJ: Kinetic model for FGF, FGFR, and proteoglycan signal transduction complex assembly. Biochemistry. 2004 Apr 27;43(16):4724-30. [PubMed:15096041]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
S100 protein binding
Specific Function
Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
Gene Name
FGF1
Uniprot ID
P05230
Uniprot Name
Fibroblast growth factor 1
Molecular Weight
17459.58 Da
References
  1. Robinson CJ, Harmer NJ, Goodger SJ, Blundell TL, Gallagher JT: Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes. J Biol Chem. 2005 Dec 23;280(51):42274-82. Epub 2005 Oct 11. [PubMed:16219767]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosi...
Gene Name
FGFR2
Uniprot ID
P21802
Uniprot Name
Fibroblast growth factor receptor 2
Molecular Weight
92024.29 Da
References
  1. Robinson CJ, Harmer NJ, Goodger SJ, Blundell TL, Gallagher JT: Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes. J Biol Chem. 2005 Dec 23;280(51):42274-82. Epub 2005 Oct 11. [PubMed:16219767]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Ligand-dependent nuclear receptor transcription coactivator activity
Specific Function
Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
Gene Name
FGF2
Uniprot ID
P09038
Uniprot Name
Fibroblast growth factor 2
Molecular Weight
30769.715 Da
References
  1. Rose K, Kriha D, Pallast S, Junker V, Klumpp S, Krieglstein J: Basic fibroblast growth factor: lysine 134 is essential for its neuroprotective activity. Neurochem Int. 2007 Jul;51(1):25-31. Epub 2007 Apr 19. [PubMed:17524524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Heparin binding
Specific Function
Released during platelet aggregation. Neutralizes the anticoagulant effect of heparin because it binds more strongly to heparin than to the chondroitin-4-sulfate chains of the carrier molecule. Che...
Gene Name
PF4
Uniprot ID
P02776
Uniprot Name
Platelet factor 4
Molecular Weight
10844.78 Da
References
  1. Greinacher A, Althaus K, Krauel K, Selleng S: Heparin-induced thrombocytopenia. Hamostaseologie. 2010 Jan;30(1):17-8, 20-8. [PubMed:20162249]
  2. Visentin GP, Ford SE, Scott JP, Aster RH: Antibodies from patients with heparin-induced thrombocytopenia/thrombosis are specific for platelet factor 4 complexed with heparin or bound to endothelial cells. J Clin Invest. 1994 Jan;93(1):81-8. [PubMed:8282825]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Potent mitogen for mature parenchymal hepatocyte cells, seems to be a hepatotrophic factor, and acts as a growth factor for a broad spectrum of tissues and cell types. Activating ligand for the rec...
Gene Name
HGF
Uniprot ID
P14210
Uniprot Name
Hepatocyte growth factor
Molecular Weight
83133.115 Da
References
  1. Sakata H, Stahl SJ, Taylor WG, Rosenberg JM, Sakaguchi K, Wingfield PT, Rubin JS: Heparin binding and oligomerization of hepatocyte growth factor/scatter factor isoforms. Heparan sulfate glycosaminoglycan requirement for Met binding and signaling. J Biol Chem. 1997 Apr 4;272(14):9457-63. [PubMed:9083085]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Syndecan binding
Specific Function
Endoglycosidase that cleaves heparan sulfate proteoglycans (HSPGs) into heparan sulfate side chains and core proteoglycans. Participates in extracellular matrix (ECM) degradation and remodeling. Se...
Gene Name
HPSE
Uniprot ID
Q9Y251
Uniprot Name
Heparanase
Molecular Weight
61148.17 Da
References
  1. Wang B, Jia J, Zhang X, Zcharia E, Vlodavsky I, Pejler G, Li JP: Heparanase affects secretory granule homeostasis of murine mast cells through degrading heparin. J Allergy Clin Immunol. 2011 Dec;128(6):1310-1317.e8. doi: 10.1016/j.jaci.2011.04.011. Epub 2011 May 14. [PubMed:21575986]
  2. Nadir Y, Brenner B: Heparanase procoagulant effects and inhibition by heparins. Thromb Res. 2010 Apr;125 Suppl 2:S72-6. doi: 10.1016/S0049-3848(10)70018-9. [PubMed:20434010]
  3. Levy-Adam F, Feld S, Suss-Toby E, Vlodavsky I, Ilan N: Heparanase facilitates cell adhesion and spreading by clustering of cell surface heparan sulfate proteoglycans. PLoS One. 2008 Jun 11;3(6):e2319. doi: 10.1371/journal.pone.0002319. [PubMed:18545691]
  4. Vlodavsky I, Ilan N, Naggi A, Casu B: Heparanase: structure, biological functions, and inhibition by heparin-derived mimetics of heparan sulfate. Curr Pharm Des. 2007;13(20):2057-73. [PubMed:17627539]
  5. Katz BZ, Muhl L, Zwang E, Ilan N, Herishanu Y, Deutsch V, Naparstek E, Vlodavsky I, Preissner KT: Heparanase modulates heparinoids anticoagulant activities via non-enzymatic mechanisms. Thromb Haemost. 2007 Dec;98(6):1193-9. [PubMed:18064313]
  6. Nasser NJ, Sarig G, Brenner B, Nevo E, Goldshmidt O, Zcharia E, Li JP, Vlodavsky I: Heparanase neutralizes the anticoagulation properties of heparin and low-molecular-weight heparin. J Thromb Haemost. 2006 Mar;4(3):560-5. [PubMed:16460439]

Drug created on June 13, 2005 07:24 / Updated on November 17, 2018 07:16