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Th1001 details
Primary information
ID10001
Therapeutic IDTh1001
Protein NameLepirudin
Sequence>Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ
Molecular Weight6979
Chemical FormulaC287H440N80O111S6
Isoelectric Point3.7
Hydrophobicity-0.777
Melting point65
Half-lifeApproximately 1.3 hours
DescriptionLepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.
Indication/DiseaseFor the treatment of heparin-induced thrombocytopenia.
PharmacodynamicsLepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Mechanism of ActionLepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
ToxicityIn case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
MetabolismLepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%)
AbsorptionBioavailability is 100% following injection.
12.2 L [Healthy young subjects (n = 18, age 18-60 years)]
Clearance164 ml/min [Healthy 18-60 yrs]
CategoriesAmino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors
Patents NumberCA1339104
Date of Issue29-Jul-1997
Date of Expiry29-Jul-2014
Drug InteractionGinkgo biloba = may increase bleed risk.
TargetProthrombin
Brand NameRefludan
CompanyBerlex Labs
Brand DescriptionBerlex Labs
Prescribed Forheparin-induced thrombocytopenia (HIT) and associated thromboembolic disease
Chemical Name[Leu1, Thr2]-63-desulfohirudin
FormulationEach vial of REFLUDAN contains 50 mg lepirudin. Other ingre-dients are 40 mg mannitol and sodium hydroxide for adjust-ment of pH to approximately 7
Physical Appearance Sterile, white, freeze-dried powder
Route of AdministrationIntravenous infusion
Recommended DosageRecommended dose is 0.4 mg/kg body weight (up to 110kg) slowly intravenously (eg, over 15 to 20seconds) as a bolus dose, and can be followed by 0.15 mg/kg body weight (up to 110kg)/hour as a continuous Intravenous infusion for 2 to 10 days or longer if CL.
ContraindicationHypersensitivity
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA


Primary information
ID10002
Therapeutic IDTh1001
Protein NameLepirudin
Sequence>Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ
Molecular Weight6979
Chemical FormulaC287H440N80O111S6
Isoelectric Point3.7
Hydrophobicity-0.777
Melting point65
Half-lifeApproximately 1.3 hours
DescriptionLepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.
Indication/DiseaseFor the treatment of heparin-induced thrombocytopenia.
PharmacodynamicsLepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Mechanism of ActionLepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
ToxicityIn case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
MetabolismLepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%)
AbsorptionBioavailability is 100% following injection.
18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)]
Clearance139 ml/min [Healthy 65-80 yrs]
CategoriesAmino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors
Patents NumberUS5180668
Date of Issue19-Jan-1993
Date of Expiry6-Mar-2012
Drug InteractionTreprostinil = increases the risk of bleeding when combined with Lepirudin.
TargetNA
Brand NameNA
CompanyBayer Healthcare
Brand DescriptionBayer Healthcare
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA


Primary information
ID10003
Therapeutic IDTh1001
Protein NameLepirudin
Sequence>Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ
Molecular Weight6979
Chemical FormulaC287H440N80O111S6
Isoelectric Point3.7
Hydrophobicity-0.777
Melting point65
Half-lifeApproximately 1.3 hours
DescriptionLepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.
Indication/DiseaseFor the treatment of heparin-induced thrombocytopenia.
PharmacodynamicsLepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Mechanism of ActionLepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
ToxicityIn case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
MetabolismLepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%)
AbsorptionBioavailability is 100% following injection.
18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)]
Clearance61 ml/min [renal impaired]
CategoriesAmino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetNA
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA


Primary information
ID10004
Therapeutic IDTh1001
Protein NameLepirudin
Sequence>Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ
Molecular Weight6979
Chemical FormulaC287H440N80O111S6
Isoelectric Point3.7
Hydrophobicity-0.777
Melting point65
Half-lifeApproximately 1.3 hours
DescriptionLepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.
Indication/DiseaseFor the treatment of heparin-induced thrombocytopenia.
PharmacodynamicsLepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Mechanism of ActionLepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
ToxicityIn case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
MetabolismLepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%)
AbsorptionBioavailability is 100% following injection.
32.1 L [HIT patients (n = 73)]
Clearance114 ml/min [HIT (Heparin-induced thrombocytopenia)]
CategoriesAmino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetNA
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1NA
Useful Link 2NA
RemarksNA