Detailed description page of ThPDB2
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Th1009 details |
| Primary information | |
|---|---|
| ID | 10055 |
| Therapeutic ID | Th1009 |
| Protein Name | Alteplase |
| Sequence | >Th1009_Alteplase SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP |
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting point | 60 |
| Half-life | NA |
| Description | Glycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells. |
| Indication/Disease | To manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli |
| Pharmacodynamics | Alteplase 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 Action | Alteplase 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. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| NA | |
| Clearance | NA |
| Categories | Agents causing angioedema, Amino Acids, Peptides, and Proteins, Anticoagulants, Blood and Blood Forming Organs, Blood Proteins, Cardiovascular Agents, Endopeptidases, Enzymes, Enzymes and Coenzymes, Fibrin Modulating Agents, Fibrinolytic Agents, Hematologic Agents, Hydrolases, Ophthalmologicals, Peptide Hydrolases, Plasminogen Activators, Proteins, Sensory Organs, Serine Endopeptidases, Serine Proteases, Tissue Plasminogen Activator, Tissue Plasminogen Activator, antagonists & inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Ginkgo biloba.Additive anticoagulant/antiplatelet effects may increase bleeding risk. Concomitant therapy should be avoided. |
| Target | Plasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1 |
| Brand Name | Activase |
| Company | Genentech Inc |
| Brand Description | Genentech Inc |
| Prescribed For | To 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 Name | NA |
| Formulation | NA |
| Physical Appearance | Sterile, white to off-white, lyophilized powder |
| Route of Administration | Intravenous |
| Recommended Dosage | The 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. |
| Contraindication | Allergic |
| Side Effects | Rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10056 |
| Therapeutic ID | Th1009 |
| Protein Name | Alteplase |
| Sequence | >Th1009_Alteplase SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP |
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting point | 60 |
| Half-life | NA |
| Description | Glycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells. |
| Indication/Disease | To manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli |
| Pharmacodynamics | Alteplase 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 Action | Alteplase 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. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| NA | |
| Clearance | NA |
| Categories | Agents causing angioedema, Amino Acids, Peptides, and Proteins, Anticoagulants, Blood and Blood Forming Organs, Blood Proteins, Cardiovascular Agents, Endopeptidases, Enzymes, Enzymes and Coenzymes, Fibrin Modulating Agents, Fibrinolytic Agents, Hematologic Agents, Hydrolases, Ophthalmologicals, Peptide Hydrolases, Plasminogen Activators, Proteins, Sensory Organs, Serine Endopeptidases, Serine Proteases, Tissue Plasminogen Activator, Tissue Plasminogen Activator, antagonists & inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | IV nitroglycerin may decrease the effect of alteplase. |
| Target | NA |
| Brand Name | Cathflo |
| Company | Hoffmann La Roche |
| Brand Description | Hoffmann La Roche |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | Have 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 Effects | Black 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 Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10057 |
| Therapeutic ID | Th1009 |
| Protein Name | Alteplase |
| Sequence | >Th1009_Alteplase SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP |
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting point | 60 |
| Half-life | NA |
| Description | Glycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells. |
| Indication/Disease | To manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli |
| Pharmacodynamics | Alteplase 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 Action | Alteplase 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. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| NA | |
| Clearance | NA |
| Categories | Agents causing angioedema, Amino Acids, Peptides, and Proteins, Anticoagulants, Blood and Blood Forming Organs, Blood Proteins, Cardiovascular Agents, Endopeptidases, Enzymes, Enzymes and Coenzymes, Fibrin Modulating Agents, Fibrinolytic Agents, Hematologic Agents, Hydrolases, Ophthalmologicals, Peptide Hydrolases, Plasminogen Activators, Proteins, Sensory Organs, Serine Endopeptidases, Serine Proteases, Tissue Plasminogen Activator, Tissue Plasminogen Activator, antagonists & inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Ticlopidine.Increased bleeding risk. Monitor for signs of bleeding. |
| Target | NA |
| Brand Name | Cathflo Activase |
| Company | Genentech, Inc |
| Brand Description | Genentech, Inc |
| Prescribed For | Used to treat the symptoms of Acute Myocardial Infarction, Pulmonary Embolism, Acute Ischemic Stroke, and Central Venous Catheter Occlusion |
| Chemical Name | NA |
| Formulation | Each vial of Cathflo Activase contains 2.2 mg of Alteplase (which includes a 10% overfill), 77 mg of Larginine, 0.2 mg of polysorbate 80, and phosphoric acid for pH adjustment. Each reconstituted vial will deliver 2 mg of Cathflo Activase, at a pH of approximately 7.3. |
| Physical Appearance | sterile, white to pale yellow, lyophilized powder |
| Route of Administration | Injection for intracatheter instillation for restoration of function to central venous access devices following reconstitution with Sterile Water for Injection, USP. |
| Recommended Dosage | Cathflo® Activase® (Alteplase) is for instillation into the dysfunctional catheter at a concentration of 1 mg/mL. Patients weighing ≥30 kg: 2 mg in 2 mL Patients weighing <30 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg in 2 mL |
| Contraindication | Cathflo Activase should not be administered to patients with known hypersensitivity to Alteplase or any component of the formulation |
| Side Effects | hives, difficulty breathing, swelling of your face, lips, tongue, or throat, any bleeding that will not stop, sudden headache, weakness, dizziness, bleeding gums, nosebleeds, easy bruising, bleeding from a wound, incision, catheter, or needle injection, bloody or tarry stools, coughing up blood, vomit that looks like coffee grounds, red or pink urine, heavy menstrual periods, abnormal vaginal bleeding, sudden numbness or weakness (especially on one side of the body), slurred speech, problems with vision or balance, chest pain or pressure, pain spreading to the jaw or shoulder, nausea, sweating, general ill feeling, sudden severe back pain, muscle weakness, numbness or loss of feeling in your arms or legs, swelling, rapid weight gain, little or nor urination, severe stomach pain, vomiting, darkening or purple discoloration of your fingers or toes, very slow heartbeats, shortness of breath, lightheadedness, sudden severe back pain, severe headache, blurred vision, pounding in your neck or ears, and anxiety |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10058 |
| Therapeutic ID | Th1009 |
| Protein Name | Alteplase |
| Sequence | >Th1009_Alteplase SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP |
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting point | 60 |
| Half-life | NA |
| Description | Glycosylated, human tissue plasminogen activator of 527 residues purified from CHO cells. |
| Indication/Disease | To manage acute myocardial infarction, acute ischemic stroke and for lysis of acute pulmonary emboli |
| Pharmacodynamics | Alteplase 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 Action | Alteplase 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. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| NA | |
| Clearance | NA |
| Categories | Agents causing angioedema, Amino Acids, Peptides, and Proteins, Anticoagulants, Blood and Blood Forming Organs, Blood Proteins, Cardiovascular Agents, Endopeptidases, Enzymes, Enzymes and Coenzymes, Fibrin Modulating Agents, Fibrinolytic Agents, Hematologic Agents, Hydrolases, Ophthalmologicals, Peptide Hydrolases, Plasminogen Activators, Proteins, Sensory Organs, Serine Endopeptidases, Serine Proteases, Tissue Plasminogen Activator, Tissue Plasminogen Activator, antagonists & inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | NA |
| Brand Name | NA |
| Company | NA |
| Brand Description | NA |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | History of bleeding problems, or severe uncontrolled high blood pressure. |
| Side Effects | Sudden arm or leg pain; sudden dizziness, fainting, severe headache, or vomiting; unusual or easy bleeding or bruising. |
| Useful Link 1 | NA |
| Useful Link 2 | NA |
| Remarks | NA |