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Th1009 details
Primary information
ID1055
ThPP IDTh1009
Therapeutic Peptide/Protein NameAlteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight59042.3
Chemical FormulaC2569H3928N746O781S40
Isoelectric Point7.61
Hydrophobicity-0.516
Melting Point (℃)60
Half LifeN.A.
DescriptionGlycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells.
Indication/DiseaseTo manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli
PharmacodynamicsAlteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin, thus limited conversion of plasminogen takes place in the absence of fibrin.
Mechanism of ActionAlteplase on binding to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain cleaves (domain) the Arg/Val bond in plasminogen to form plasmin which in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesThrombolytic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionGinkgo biloba.Additive anticoagulant/antiplatelet effects may increase bleeding risk. Concomitant therapy should be avoided.
TargetPlasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1
Information of corresponding available drug in the market
Brand NameActivase
CompanyGenentech Inc
Brand DiscriptionActivase is a tissue plasminogen activator produced by recombinant DNA technology. It is a sterile, purified glycoprotein of 527 amino acids, synthesized using the complementary DNA (cDNA) for natural human tissue-type plasminogen activator obtained from
Prescribed forTo treat blood clots in the lungs and improve heart function and survival followed by a heart attack. Activase may also be used to improve recovery and reduce disability in certain patients who have suffered from a stroke.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceSterile, white to off-white, lyophilized powder
Route of AdministrationIntravenous
Recommended DosageThe recommended dose is not to exceed 100 mg. Patients weighing > 67 kg are recommended a dose of 100 mg as a 15 mg intravenous bolus, followed by 50 mg infused over the next 30 minutes, and then 35 mg infused over the next 60 minutes.
ContraindicationAllergic
Side EffectsRash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue.
Useful Linkhttp://www.drugs.com/cdi/activase.html
PubMed ID15650539
3-D StructureTh1009 (View) or (Download)
Primary information
ID1056
ThPP IDTh1009
Therapeutic Peptide/Protein NameAlteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight59042.3
Chemical FormulaC2569H3928N746O781S40
Isoelectric Point7.61
Hydrophobicity-0.516
Melting Point (℃)60
Half LifeN.A.
DescriptionGlycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells.
Indication/DiseaseTo manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli
PharmacodynamicsAlteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin, thus limited conversion of plasminogen takes place in the absence of fibrin.
Mechanism of ActionAlteplase on binding to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain cleaves (domain) the Arg/Val bond in plasminogen to form plasmin which in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesThrombolytic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionIV nitroglycerin may decrease the effect of alteplase.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationHave active internal bleeding, history of stroke, recent brain or spinal surgery (within 3 months), a growth in the brain, abnormal formation of blood vessels.
Side EffectsBlack or bloody stools; bloody vomit; change in color of your fingers or toes; changes in vision; chills; coughing up blood; decreased amount of urine produced; difficulty breathing or sudden shortness of breath; difficulty swallowing.
Useful Linkhttp://www.rxlist.com/activase-drug.htm
PubMed ID15650539
3-D StructureTh1009 (View) or (Download)
Primary information
ID1057
ThPP IDTh1009
Therapeutic Peptide/Protein NameAlteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight59042.3
Chemical FormulaC2569H3928N746O781S40
Isoelectric Point7.61
Hydrophobicity-0.516
Melting Point (℃)60
Half LifeN.A.
DescriptionGlycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells.
Indication/DiseaseTo manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli
PharmacodynamicsAlteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin, thus limited conversion of plasminogen takes place in the absence of fibrin.
Mechanism of ActionAlteplase on binding to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain cleaves (domain) the Arg/Val bond in plasminogen to form plasmin which in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesThrombolytic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionTiclopidine.Increased bleeding risk. Monitor for signs of bleeding.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationCertain type of bulging blood vessel (aneurysm), have a heart attack or blood clot in the lung and you also have had recent brain or spinal injury
Side EffectsNumbness in arm or leg; one-sided weakness; pain, redness, or swelling at the injection site; purple skin color; rectal bleeding; seizures; severe bleeding; severe muscle aches or pain; severe stomach pain; sharp or crushing chest pain; speech problems
Useful Linkhttp://www.drugs.com/drug-interactions/alteplase,activase-index.html?filter=1
PubMed ID15650539
3-D StructureTh1009 (View) or (Download)
Primary information
ID1058
ThPP IDTh1009
Therapeutic Peptide/Protein NameAlteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight59042.3
Chemical FormulaC2569H3928N746O781S40
Isoelectric Point7.61
Hydrophobicity-0.516
Melting Point (℃)60
Half LifeN.A.
DescriptionGlycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells.
Indication/DiseaseTo manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli
PharmacodynamicsAlteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin, thus limited conversion of plasminogen takes place in the absence of fibrin.
Mechanism of ActionAlteplase on binding to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain cleaves (domain) the Arg/Val bond in plasminogen to form plasmin which in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesThrombolytic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationHistory of bleeding problems, or severe uncontrolled high blood pressure.
Side EffectsSudden arm or leg pain; sudden dizziness, fainting, severe headache, or vomiting; unusual or easy bleeding or bruising.
Useful LinkN.A.
PubMed ID15650539
3-D StructureTh1009 (View) or (Download)