A database of FDA approved therapeutic peptides and proteins
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1055 details |
| Primary information | |
|---|---|
| ThPP ID | Th1009 |
| Therapeutic Peptide/Protein Name | Alteplase |
| Sequence | SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting Point (℃) | 60 |
| Half Life | N.A. |
| 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 | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Thrombolytic Agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| 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 |
| Information of corresponding available drug in the market | |
| Brand Name | Activase |
| Company | Genentech Inc |
| Brand Discription | Activase 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 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 | N.A. |
| Formulation | N.A. |
| Physcial Appearnce | 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 | http://www.drugs.com/cdi/activase.html |
| PubMed ID | 15650539 |
| 3-D Structure | Th1009 (View) or (Download) |