Identification

Name
Tinzaparin
Accession Number
DB06822
Type
Small Molecule
Groups
Approved
Description

Tinzaparin is a low molecular weight heparin (LMWH), produced by enzymatic depolymerization of unfractionated heparin from porcine intestinal mucosa. It is a heterogeneous mixture of with an average molecular weight between 5500 and 7500 daltons. Tinzaparin is composed of molecules with and without a special site for high affinity binding to antithrombin III (ATIII). This complex greatly accelerates the inhibition of factor Xa. It is an anticoagulant and considered an antithrombotic. Tinzaparin must be given either subcutaneously or parenterally. LMWHs are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.

Synonyms
  • Tinzaparin sodium
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
InnohepInjection, solution20000 [iU]/mLSubcutaneousLeo Pharma2010-07-012017-08-01Us
InnohepSolution20000 unitSubcutaneousLeo Pharma2011-09-13Not applicableCanada
InnohepSolution10000 unitSubcutaneousLeo Pharma2011-09-09Not applicableCanada
InnohepSolution12000 unitSubcutaneousLeo Pharma2014-09-30Not applicableCanada
InnohepSolution20000 unitSubcutaneousLeo Pharma1997-02-28Not applicableCanada
InnohepSolution20000 unitSubcutaneousLeo Pharma2011-09-16Not applicableCanada
InnohepSolution20000 unitSubcutaneousLeo Pharma1997-09-23Not applicableCanada
InnohepSolution10000 unitSubcutaneousLeo Pharma1995-12-31Not applicableCanada
InnohepSolution8000 unitSubcutaneousLeo Pharma2014-09-30Not applicableCanada
InnohepSolution10000 unitSubcutaneousLeo Pharma2011-12-10Not applicableCanada
Categories
UNII
7UQ7X4Y489
CAS number
9041-08-1
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Tinzaparin is used for the prevention of postoperative venous thromboembolism in patients undergoing orthopedic surgery and in patients undergoing general surgery who are at high risk of developing postoperative venous thromboembolism. It is also used for the treatment of deep vein thrombosis and/or pulmonary embolism. It is indicated for use in preventing clot formation in indwelling intravenous lines for hemodialysis.

Structured Indications
Pharmacodynamics

Tinzaparin, like other LMWHs, have a higher anti-Xa activity than anti-IIa activity. The anti-Xa activity of tinzaparin is 2.0 +/- 0.5 times greater than its to anti-IIa activity. Heparin exhibits approximately equal inhibitory activity against Xa and IIa. Tinzaparin is an anticoagulant that blocks the formation of thrombi. Like all LMWHs, tinzaparin only causes activated partial thromboplastin time (aPTT) prolongation at higher doses and routine monitoring is not recommended. However, anti-factor Xa levels may be monitored in some conditions such as pregnancy and renal dysfunction. Its use should be avoided in patients with a creatinine clearance less than 20 mL/min. In these patients, unfractionated heparin should be used. Tinzaparin can be used in patients who have a creatinine clearance between 20-30 mL/min, giving it the highest safety threshold for use in renal failure patients compared to all the LMWHs.

Mechanism of action

Tinzaparin binds to the plasma protein antithrombin III, forming a complex with then accelerates the inhibition of factor Xa. Its affinity for factor Xa is 2-4 times greater than that of unbound ATIII. The inactivation of factor Xa in turn will exponentially generation of thrombin (factor IIa) molecules, which is needed to activate fibrinogen to fibrin. The coagulation cascade is inhibited because fibrin cannot be formed in the presence of tinzaparin. Like all LMWH, it cannot be given intramuscularly due to increased risk of hematoma.

TargetActionsOrganism
AAntithrombin-III
potentiator
Human
UIntegrin alpha-4
inhibitor
Human
UStromal cell-derived factor 1
binder
Human
Absorption

Subcutaneous injection - about 90% when measured as anti-Xa activity versus 67% for anti-IIa activity.

Volume of distribution

Anti-Xa activity is 4 L. Anti-IIa activity is 10.9 L

Protein binding

Low protein binding compared to unfractionated heparin.

Metabolism

Sulfation and polymerization occurs in the liver.

Route of elimination

Linear elimination through kidneys

Half life

Anti-Xa activity is 82 minutes. Anti-IIa activity is 71 minutes.

Clearance

Clearance is dose-dependant. The clearance of tinzaparin based on anti-Xa activity ranged from 1.14 to 2.04 L/hr

Toxicity

Osteoporosis with increasing duration of use, bleeding, alopecia, heparin induced thrombocytopenia (HIT). All of these adverse drug reactions occur less with LMWH compared to unfractionated heparin. Tinzaparin showed no toxic effects at doses up to 5 mg/kg in mice, rats, or dogs in standard acute, subacute, and chronic toxicity studies.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabTinzaparin may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolTinzaparin may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Tinzaparin.Approved, Vet Approved
AliskirenTinzaparin may increase the hyperkalemic activities of Aliskiren.Approved, Investigational
AloxiprinThe risk or severity of adverse effects can be increased when Aloxiprin is combined with Tinzaparin.Experimental
AlprostadilAlprostadil may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
AmilorideTinzaparin may increase the hyperkalemic activities of Amiloride.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Tinzaparin.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Tinzaparin.Approved
AncrodTinzaparin may increase the anticoagulant activities of Ancrod.Approved, Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Tinzaparin.Investigational
Antithrombin III humanTinzaparin may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanTinzaparin may increase the anticoagulant activities of Apixaban.Approved
AprotininThe therapeutic efficacy of Tinzaparin can be decreased when used in combination with Aprotinin.Approved, Investigational, Withdrawn
ArdeparinTinzaparin may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanTinzaparin may increase the anticoagulant activities of Argatroban.Approved, Investigational
AzelastineAzelastine may increase the anticoagulant activities of Tinzaparin.Approved
Azilsartan medoxomilTinzaparin may increase the hyperkalemic activities of Azilsartan medoxomil.Approved, Investigational
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Tinzaparin.Approved, Investigational
BecaplerminTinzaparin may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BeraprostBeraprost may increase the anticoagulant activities of Tinzaparin.Investigational
BivalirudinTinzaparin may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BuflomedilBuflomedil may increase the anticoagulant activities of Tinzaparin.Experimental
ButylphthalideButylphthalide may increase the anticoagulant activities of Tinzaparin.Investigational
CanagliflozinTinzaparin may increase the hyperkalemic activities of Canagliflozin.Approved
CandesartanTinzaparin may increase the hyperkalemic activities of Candesartan.Experimental
Candesartan cilexetilTinzaparin may increase the hyperkalemic activities of Candesartan cilexetil.Approved
CangrelorCangrelor may increase the anticoagulant activities of Tinzaparin.Approved
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Tinzaparin.Experimental, Investigational
CertoparinTinzaparin may increase the anticoagulant activities of Certoparin.Approved, Investigational
CilostazolCilostazol may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
Citric AcidTinzaparin may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Tinzaparin.Approved
CloricromenCloricromen may increase the anticoagulant activities of Tinzaparin.Experimental
Dabigatran etexilateTinzaparin may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinTinzaparin may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidTinzaparin may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanTinzaparin may increase the anticoagulant activities of Darexaban.Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
DersalazineThe risk or severity of adverse effects can be increased when Dersalazine is combined with Tinzaparin.Investigational
DesirudinTinzaparin may increase the anticoagulant activities of Desirudin.Approved
DextranTinzaparin may increase the anticoagulant activities of Dextran.Approved, Investigational, Vet Approved
DicoumarolTinzaparin may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Tinzaparin.Approved, Investigational
DipyridamoleDipyridamole may increase the anticoagulant activities of Tinzaparin.Approved
Edetic AcidTinzaparin may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanTinzaparin may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinTinzaparin may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
EplerenoneTinzaparin may increase the hyperkalemic activities of Eplerenone.Approved
EplivanserinEplivanserin may increase the anticoagulant activities of Tinzaparin.Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Tinzaparin.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Tinzaparin.Approved
EprosartanTinzaparin may increase the hyperkalemic activities of Eprosartan.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
Ethyl biscoumacetateTinzaparin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ferulic acidTinzaparin may increase the anticoagulant activities of Ferulic acid.Experimental
FimasartanTinzaparin may increase the hyperkalemic activities of Fimasartan.Approved, Investigational
FluindioneTinzaparin may increase the anticoagulant activities of Fluindione.Approved, Investigational
FondaparinuxTinzaparin may increase the anticoagulant activities of Fondaparinux.Approved, Investigational
Fondaparinux sodiumTinzaparin may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
ForasartanTinzaparin may increase the hyperkalemic activities of Forasartan.Experimental
GabexateTinzaparin may increase the anticoagulant activities of Gabexate.Investigational
GuacetisalThe risk or severity of adverse effects can be increased when Guacetisal is combined with Tinzaparin.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Tinzaparin.Experimental
HeparinTinzaparin may increase the anticoagulant activities of Heparin.Approved, Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Tinzaparin.Investigational
IbudilastIbudilast may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Tinzaparin.Approved, Investigational, Nutraceutical
IdraparinuxTinzaparin may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Tinzaparin.Approved, Investigational, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Tinzaparin.Investigational
IloprostIloprost may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
IndobufenIndobufen may increase the anticoagulant activities of Tinzaparin.Investigational
IrbesartanTinzaparin may increase the hyperkalemic activities of Irbesartan.Approved, Investigational
KetanserinKetanserin may increase the anticoagulant activities of Tinzaparin.Investigational
LepirudinTinzaparin may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanTinzaparin may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Tinzaparin.Approved, Investigational
LinsidomineLinsidomine may increase the anticoagulant activities of Tinzaparin.Experimental
LosartanTinzaparin may increase the hyperkalemic activities of Losartan.Approved
MelagatranTinzaparin may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Tinzaparin.Approved
Methyl salicylateThe risk or severity of adverse effects can be increased when Methyl salicylate is combined with Tinzaparin.Approved, Vet Approved
MilrinoneMilrinone may increase the anticoagulant activities of Tinzaparin.Approved
NadroparinTinzaparin may increase the anticoagulant activities of Nadroparin.Approved, Investigational
NafamostatTinzaparin may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Tinzaparin.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Tinzaparin.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Tinzaparin.Investigational
OlmesartanTinzaparin may increase the hyperkalemic activities of Olmesartan.Approved, Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Tinzaparin.Approved
OtamixabanTinzaparin may increase the anticoagulant activities of Otamixaban.Investigational
PaliferminThe serum concentration of Palifermin can be increased when it is combined with Tinzaparin.Approved
Pentaerythritol TetranitrateTinzaparin may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
Pentosan PolysulfateTinzaparin may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
PhenindioneTinzaparin may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonTinzaparin may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
Phenyl aminosalicylateThe risk or severity of adverse effects can be increased when Phenyl aminosalicylate is combined with Tinzaparin.Approved
PicotamidePicotamide may increase the anticoagulant activities of Tinzaparin.Experimental
PrasugrelPrasugrel may increase the anticoagulant activities of Tinzaparin.Approved
Protein CTinzaparin may increase the anticoagulant activities of Protein C.Approved
Protein S humanTinzaparin may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeTinzaparin may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Tinzaparin.Investigational
RelcovaptanRelcovaptan may increase the anticoagulant activities of Tinzaparin.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Tinzaparin.Approved, Experimental, Investigational
ReviparinTinzaparin may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelRidogrel may increase the anticoagulant activities of Tinzaparin.Approved
RivaroxabanTinzaparin may increase the anticoagulant activities of Rivaroxaban.Approved
SacubitrilTinzaparin may increase the hyperkalemic activities of Sacubitril.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Tinzaparin.Approved, Investigational, Vet Approved
SaprisartanTinzaparin may increase the hyperkalemic activities of Saprisartan.Experimental
SaralasinTinzaparin may increase the hyperkalemic activities of Saralasin.Investigational
SarpogrelateSarpogrelate may increase the anticoagulant activities of Tinzaparin.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Tinzaparin.Approved, Vet Approved
SpironolactoneTinzaparin may increase the hyperkalemic activities of Spironolactone.Approved
SRT501SRT501 may increase the anticoagulant activities of Tinzaparin.Investigational
SulodexideTinzaparin may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TasosartanTinzaparin may increase the hyperkalemic activities of Tasosartan.Approved
TelmisartanTinzaparin may increase the hyperkalemic activities of Telmisartan.Approved, Investigational
TesmilifeneTesmilifene may increase the anticoagulant activities of Tinzaparin.Investigational
TicagrelorTicagrelor may increase the anticoagulant activities of Tinzaparin.Approved
TiclopidineTiclopidine may increase the anticoagulant activities of Tinzaparin.Approved
TirofibanTirofiban may increase the anticoagulant activities of Tinzaparin.Approved
TranilastTranilast may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Tinzaparin.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Tinzaparin is combined with Treprostinil.Approved, Investigational
TriamtereneTinzaparin may increase the hyperkalemic activities of Triamterene.Approved
TriflusalTriflusal may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Tinzaparin.Approved
TroxerutinTinzaparin may increase the anticoagulant activities of Troxerutin.Investigational
ValsartanTinzaparin may increase the hyperkalemic activities of Valsartan.Approved, Investigational
VorapaxarVorapaxar may increase the anticoagulant activities of Tinzaparin.Approved
WarfarinTinzaparin may increase the anticoagulant activities of Warfarin.Approved
XimelagatranTinzaparin may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food Interactions
  • Herbs with anticoagulant/antiplatelet properties (ginger, gingko, garlic) may increase the risk of bleeding.

References

General References
  1. Friedel HA, Balfour JA: Tinzaparin. A review of its pharmacology and clinical potential in the prevention and treatment of thromboembolic disorders. Drugs. 1994 Oct;48(4):638-60. [PubMed:7528134]
  2. Simonneau G, Sors H, Charbonnier B, Page Y, Laaban JP, Azarian R, Laurent M, Hirsch JL, Ferrari E, Bosson JL, Mottier D, Beau B: A comparison of low-molecular-weight heparin with unfractionated heparin for acute pulmonary embolism. The THESEE Study Group. Tinzaparine ou Heparine Standard: Evaluations dans l'Embolie Pulmonaire. N Engl J Med. 1997 Sep 4;337(10):663-9. [PubMed:9278462]
  3. Planes A, Samama MM, Lensing AW, Buller HR, Barre J, Vochelle N, Beau B: Prevention of deep vein thrombosis after hip replacement--comparison between two low-molecular heparins, tinzaparin and enoxaparin. Thromb Haemost. 1999 Jan;81(1):22-5. [PubMed:10348714]
  4. Cheer SM, Dunn CJ, Foster R: Tinzaparin sodium: a review of its pharmacology and clinical use in the prophylaxis and treatment of thromboembolic disease. Drugs. 2004;64(13):1479-502. [PubMed:15212562]
  5. Hoy SM, Scott LJ, Plosker GL: Tinzaparin sodium: a review of its use in the prevention and treatment of deep vein thrombosis and pulmonary embolism, and in the prevention of clotting in the extracorporeal circuit during haemodialysis. Drugs. 2010 Jul 9;70(10):1319-47. doi: 10.2165/11203710-000000000-00000. [PubMed:20568836]
  6. Hedner U: Development of tinzaparin: a heparinase-digested low-molecular-weight heparin. Semin Thromb Hemost. 2000;26 Suppl 1:23-9. [PubMed:11011803]
  7. Pautas E, Siguret V, d'Urso M, Laurent M, Gaussem P, Fevrier M, Durand-Gasselin B: [Monitoring of tinzaparin in a ten day treatment dose in elderly patients]. Rev Med Interne. 2001 Feb;22(2):120-6. [PubMed:11234669]
  8. Pineo GF, Hull RD: Tinzaparin in the treatment of venous thromboembolism. Expert Opin Pharmacother. 2003 Dec;4(12):2355-62. [PubMed:14640933]
  9. Fossler MJ, Barrett JS, Hainer JW, Riddle JG, Ostergaard P, van der Elst E, Sprogel P: Pharmacodynamics of intravenous and subcutaneous tinzaparin and heparin in healthy volunteers. Am J Health Syst Pharm. 2001 Sep 1;58(17):1614-21. [PubMed:11556655]
  10. Cambus JP, Saivin S, Heilmann JJ, Caplain H, Boneu B, Houin G: The pharmacodynamics of tinzaparin in healthy volunteers. Br J Haematol. 2002 Mar;116(3):649-52. [PubMed:11849226]
External Links
KEGG Drug
D06398
PubChem Substance
347910373
Wikipedia
Tinzaparin
ATC Codes
B01AB10 — Tinzaparin
AHFS Codes
  • 20:12.04.16 — Heparins

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentAntiphospholipid Syndrome in Pregnancy / Pregnancy Loss1
1, 2Unknown StatusTreatmentRenal Cancers1
2CompletedBasic ScienceMalignant Lymphomas / Multiple Myeloma (MM)1
2CompletedTreatmentStroke, Ischemic1
2Not Yet RecruitingTreatmentCerebral Venous Thrombosis1
2TerminatedPreventionCancers / Venous Thromboembolism1
2TerminatedSupportive CareCancers / Deep Vein Thrombosis (DVT) / Pulmonary Embolism (PE) / Thrombosis / Venous Thromboembolism1
2, 3CompletedPreventionDeep Vein Thrombosis (DVT)1
2, 3CompletedPreventionHemodialysis-dependent patients / Thromboembolism1
3CompletedTreatmentDeep Venous Thrombosis1
3CompletedTreatmentVenous Thromboembolism1
3Not Yet RecruitingPreventionNeoplasms, Lung / Venous Thromboembolism1
3RecruitingPreventionAdenocarcinoma of the Colon1
3RecruitingTreatmentAcute Chest Syndrome / Anemias / Low-Molecular-Weight Heparin / Sickle Cell1
3RecruitingTreatmentDeep Vein Thrombosis (DVT) / Pulmonary Embolism (PE) / Venous Thromboembolism1
3TerminatedTreatmentNeoplasms / Venous Thromboembolism1
4CompletedNot AvailableVenous Thromboembolism1
4CompletedPreventionKidney Failure,Chronic1
4CompletedTreatmentAcute Pulmonary Embolism1
4CompletedTreatmentDeep Vein Thrombosis (DVT)1
4CompletedTreatmentIntrauterine Growth Retardation1
4CompletedTreatmentThromboembolism / Thrombosis / Thrombosis, Venous2
4CompletedTreatmentVenous Thromboembolism1
4RecruitingPreventionDeep Venous Thrombosis / Pulmonary Embolism (PE)1
4WithdrawnPreventionDiabetes Mellitus (DM) / Hemodialysis-dependent patients1
Not AvailableActive Not RecruitingNot AvailableDeep Venous Thrombosis, Protection Against / Renal Insufficiency,Chronic1
Not AvailableCompletedPreventionCancers / Deep Vein Thrombosis (DVT) / Pulmonary Embolism (PE)1
Not AvailableCompletedPreventionPrimary Brain Tumors1
Not AvailableRecruitingNot AvailableUnsuspected Pulmonary Embolism1
Not AvailableTerminatedNot AvailableInflammatory Reaction / Nutrition / Peritoneal dialysis therapy1
Not AvailableTerminatedTreatmentPulmonary Embolism (PE) / Thrombosis, Venous1
Not AvailableUnknown StatusNot AvailableHaemorrhage / Venous Thromboembolism1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous20000 [iU]/mL
SolutionSubcutaneous10000 unit
SolutionSubcutaneous12000 unit
SolutionSubcutaneous16000 unit
SolutionSubcutaneous20000 unit
SolutionSubcutaneous8000 unit
LiquidSubcutaneous11700 unit
LiquidSubcutaneous10000 unit
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not 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. 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. [PubMed:19888521]
  2. Florian-Kujawski M, Hoppensteadt D, Maddineni J, Ziegler H, Fareed J: Differential regulation of thrombin activatable fibrinolytic inhibitor by low molecular weight heparins. Pharmacologic implications. Int Angiol. 2004 Dec;23(4):346-54. [PubMed:15767980]
  3. Morris TA, Jacobson A, Marsh JJ, Lane JR: Pharmacokinetics of UH and LMWH are similar with respect to antithrombin activity. Thromb Res. 2005;115(1-2):45-51. [PubMed:15567452]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Integrins alpha-4/beta-1 (VLA-4) and alpha-4/beta-7 are receptors for fibronectin. They recognize one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. They are...
Gene Name
ITGA4
Uniprot ID
P13612
Uniprot Name
Integrin alpha-4
Molecular Weight
114898.745 Da
References
  1. Schlesinger M, Simonis D, Schmitz P, Fritzsche J, Bendas G: Binding between heparin and the integrin VLA-4. Thromb Haemost. 2009 Nov;102(5):816-22. doi: 10.1160/TH09-01-0061. [PubMed:19888514]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Not Available
Gene Name
CXCL12
Uniprot ID
P48061
Uniprot Name
Stromal cell-derived factor 1
Molecular Weight
10665.75 Da
References
  1. Koo CY, Sen YP, Bay BH, Yip GW: Targeting heparan sulfate proteoglycans in breast cancer treatment. Recent Pat Anticancer Drug Discov. 2008 Nov;3(3):151-8. [PubMed:18991783]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Cleaves aggrecan, a cartilage proteoglycan, and may be involved in its turnover. May play an important role in the destruction of aggrecan in arthritic diseases. Could also be a critical factor in ...
Gene Name
ADAMTS4
Uniprot ID
O75173
Uniprot Name
A disintegrin and metalloproteinase with thrombospondin motifs 4
Molecular Weight
90196.02 Da
References
  1. Mousa SA: Effect of low molecular weight heparin and different heparin molecular weight fractions on the activity of the matrix-degrading enzyme aggrecanase: structure-function relationship. J Cell Biochem. 2005 May 1;95(1):95-8. [PubMed:15723278]

Drug created on September 14, 2010 10:21 / Updated on April 23, 2018 23:11