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Identification
NameTinzaparin
Accession NumberDB06822
TypeSmall Molecule
GroupsApproved
DescriptionTinzaparin 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.
Structure
Thumb
Synonyms
Tinzaparin sodium
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
InnohepSolution20000 unitSubcutaneousLeo Pharma Inc2011-09-16Not applicableCanada
InnohepInjection, solution20000 [iU]/mLSubcutaneousLEO Pharma Inc.2010-07-01Not applicableUs
InnohepSolution16000 unitSubcutaneousLeo Pharma Inc2014-09-30Not applicableCanada
InnohepSolution20000 unitSubcutaneousLeo Pharma Inc1997-09-23Not applicableCanada
InnohepSolution20000 unitSubcutaneousLeo Pharma Inc2011-09-13Not applicableCanada
InnohepSolution10000 unitSubcutaneousLeo Pharma Inc2011-09-09Not applicableCanada
InnohepSolution8000 unitSubcutaneousLeo Pharma Inc2014-09-30Not applicableCanada
InnohepSolution10000 unitSubcutaneousLeo Pharma Inc2011-12-10Not applicableCanada
InnohepSolution12000 unitSubcutaneousLeo Pharma Inc2014-09-30Not applicableCanada
InnohepSolution10000 unitSubcutaneousLeo Pharma Inc1997-07-31Not applicableCanada
Innohep - 20000anti-XA Iu/mlLiquid20000 unitSubcutaneousLeo Pharma Inc1997-02-28Not applicableCanada
Innohep Disp.syr.-11700 Anti-XA Iu/mlLiquid11700 unitSubcutaneousLeo Pharma Inc1995-12-311998-08-05Canada
Innohep Multi-dose Vial- 10000 Anti-XA Iu/mlLiquid10000 unitSubcutaneousLeo Pharma Inc1995-12-31Not applicableCanada
Logiparin Liq Sc 10000 Fxaiu/mlLiquid10000 unitSubcutaneousNovo Nordisk Canada Inc1994-12-311997-08-14Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIINot Available
CAS number9041-08-1
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationTinzaparin 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
PharmacodynamicsTinzaparin, 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 actionTinzaparin 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Antithrombin-IIIProteinyes
potentiator
HumanP01008 details
Integrin alpha-4Proteinunknown
inhibitor
HumanP13612 details
Stromal cell-derived factor 1Proteinunknown
binder
HumanP48061 details
Related Articles
AbsorptionSubcutaneous 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 bindingLow protein binding compared to unfractionated heparin.
Metabolism

Sulfation and polymerization occurs in the liver.

Route of eliminationLinear elimination through kidneys
Half lifeAnti-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

ToxicityOsteoporosis 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 organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabTinzaparin may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolTinzaparin may increase the anticoagulant activities of Acenocoumarol.Approved
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
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.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, Withdrawn
ArdeparinTinzaparin may increase the anticoagulant activities of Ardeparin.Approved, 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
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
BenazeprilTinzaparin may increase the hyperkalemic activities of Benazepril.Approved, Investigational
BeraprostBeraprost may increase the anticoagulant activities of Tinzaparin.Investigational
BivalirudinTinzaparin may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
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.Approved
CandoxatrilTinzaparin may increase the hyperkalemic activities of Candoxatril.Experimental
CangrelorCangrelor may increase the anticoagulant activities of Tinzaparin.Approved
CaptoprilTinzaparin may increase the hyperkalemic activities of Captopril.Approved
CertoparinTinzaparin may increase the anticoagulant activities of Certoparin.Approved
CilazaprilTinzaparin may increase the hyperkalemic activities of Cilazapril.Approved
CilostazolCilostazol may increase the anticoagulant activities of Tinzaparin.Approved
Citric AcidTinzaparin may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Tinzaparin.Approved, Nutraceutical
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
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, Vet Approved
Dextran 40Tinzaparin may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Tinzaparin may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Tinzaparin may increase the anticoagulant activities of Dextran 75.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
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
EnalaprilTinzaparin may increase the hyperkalemic activities of Enalapril.Approved, Vet Approved
EnalaprilatTinzaparin may increase the hyperkalemic activities of Enalaprilat.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
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
FluindioneTinzaparin may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxTinzaparin may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumTinzaparin may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
ForasartanTinzaparin may increase the hyperkalemic activities of Forasartan.Experimental
FosinoprilTinzaparin may increase the hyperkalemic activities of Fosinopril.Approved
GabexateTinzaparin may increase the anticoagulant activities of Gabexate.Investigational
HeparinTinzaparin may increase the anticoagulant activities of Heparin.Approved, Investigational
HirulogTinzaparin may increase the anticoagulant activities of Hirulog.Experimental
IbudilastIbudilast may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Tinzaparin.Approved, Nutraceutical
idraparinuxTinzaparin may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Tinzaparin.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
ImidaprilTinzaparin may increase the hyperkalemic activities of Imidapril.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
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Tinzaparin.Approved
LisinoprilTinzaparin may increase the hyperkalemic activities of Lisinopril.Approved, Investigational
LosartanTinzaparin may increase the hyperkalemic activities of Losartan.Approved
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Tinzaparin.Approved
MilrinoneMilrinone may increase the anticoagulant activities of Tinzaparin.Approved
MoexiprilTinzaparin may increase the hyperkalemic activities of Moexipril.Approved
NadroparinTinzaparin may increase the anticoagulant activities of Nadroparin.Approved
NafamostatTinzaparin may increase the anticoagulant activities of Nafamostat.Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Tinzaparin.Investigational
NCX 4016The risk or severity of adverse effects can be increased when NCX 4016 is combined with Tinzaparin.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Tinzaparin.Approved, 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
OmapatrilatTinzaparin may increase the hyperkalemic activities of Omapatrilat.Investigational
OtamixabanTinzaparin may increase the anticoagulant activities of Otamixaban.Investigational
PaliferminThe serum concentration of Palifermin can be increased when it is combined with Tinzaparin.Approved
Pentosan PolysulfateTinzaparin may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Tinzaparin.Approved, Investigational
PerindoprilTinzaparin may increase the hyperkalemic activities of Perindopril.Approved
PhenindioneTinzaparin may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonTinzaparin may increase the anticoagulant activities of Phenprocoumon.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Tinzaparin.Approved
Protein CTinzaparin may increase the anticoagulant activities of Protein C.Approved
ProtocatechualdehydeTinzaparin may increase the anticoagulant activities of Protocatechualdehyde.Approved
QuinaprilTinzaparin may increase the hyperkalemic activities of Quinapril.Approved, Investigational
RamatrobanRamatroban may increase the anticoagulant activities of Tinzaparin.Investigational
RamiprilTinzaparin may increase the hyperkalemic activities of Ramipril.Approved
RescinnamineTinzaparin may increase the hyperkalemic activities of Rescinnamine.Approved
ResveratrolResveratrol may increase the anticoagulant activities of Tinzaparin.Experimental, Investigational
ReviparinTinzaparin may increase the anticoagulant activities of Reviparin.Approved
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, Vet Approved
SaprisartanTinzaparin may increase the hyperkalemic activities of Saprisartan.Experimental
SaralasinTinzaparin may increase the hyperkalemic activities of Saralasin.Investigational
SCH-530348SCH-530348 may increase the anticoagulant activities of Tinzaparin.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Tinzaparin.Approved, Vet Approved
SpiraprilTinzaparin may increase the hyperkalemic activities of Spirapril.Approved
SpironolactoneTinzaparin may increase the hyperkalemic activities of Spironolactone.Approved
SRT501SRT501 may increase the anticoagulant activities of Tinzaparin.Investigational
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Tinzaparin.Approved
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
TemocaprilTinzaparin may increase the hyperkalemic activities of Temocapril.Experimental, Investigational
TesmilifeneTesmilifene may increase the anticoagulant activities of Tinzaparin.Investigational
TiclopidineTiclopidine may increase the anticoagulant activities of Tinzaparin.Approved
TirofibanTirofiban may increase the anticoagulant activities of Tinzaparin.Approved
TrandolaprilTinzaparin may increase the hyperkalemic activities of Trandolapril.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
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
Ym150Tinzaparin may increase the anticoagulant activities of Ym150.Investigational
Food Interactions
  • Herbs with anticoagulant/antiplatelet properties (ginger, gingko, garlic) may increase the risk of bleeding.
References
Synthesis ReferenceNot Available
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
ATC CodesB01AB10
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous20000 [iU]/mL
SolutionSubcutaneous10000 unit
SolutionSubcutaneous12000 unit
SolutionSubcutaneous16000 unit
SolutionSubcutaneous20000 unit
SolutionSubcutaneous8000 unit
LiquidSubcutaneous20000 unit
LiquidSubcutaneous11700 unit
LiquidSubcutaneous10000 unit
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot 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 activity is greatly enhanced in the presence of heparin.
Gene Name:
SERPINC1
Uniprot ID:
P01008
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 also receptors for VCAM1. Integrin alpha-4/beta-1 recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha-4/beta-7 is also a receptor for MADCAM1. It recognizes the sequence L-D-T in MADCAM1. On act...
Gene Name:
ITGA4
Uniprot ID:
P13612
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
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 the exacerbation of neurodegeneration in Alzheimer disease. Cleaves aggrecan at the '392-Glu-|-Ala-393' site.
Gene Name:
ADAMTS4
Uniprot ID:
O75173
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 ]
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Drug created on September 14, 2010 10:21 / Updated on August 17, 2016 12:24