| Generic name |
Reteplase
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| Brand Names/Synonyms |
Tissue-type plasminogen activator precursor;tPA;t- PA;t-plasminogen activator;Alteplase;Reteplase; Retavase (Centocor); Retavase (Roche) |
| Indication |
For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction |
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Description |
Human tissue plasminogen activator, purified, glycosylated, 355 residues purified from CHO cells. Retavase is considered a "third-generation" thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase - kringle-1, finger, and epidermal growth factor (EGF). |
| Pharmacology |
Retavase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction. |
| Mechanism Of Action |
Retavase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots. |
Reteplase News
(When available) |
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| Dosage Forms |
LIQUID;POWDER FOR SOLUTION |
| Drug_Category |
Thrombolytic Agents |
| Absorption |
Not Available |
| Interactions |
Not Available |
| Toxicity |
Not Available |
| Organisms Affected |
Humans and other mammals |
| Chemical IUPAC Name |
Human tissue plasminogen activator fragment |
| Chemical Formula |
C1736H2671N499O522S22 |
| Molecular Weight |
39589.6 |
| Smiles String |
Not Available |
| Melting Point |
60 oC (Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)) |
| Water Solubility |
Not Available |
| State |
Transparent, slightly viscous, aqueous liquid |
| LogP/Hphobicity |
-0.435 |
| Isoelectric Point |
6.86 |
| Biotransformation |
Not Available |
| Half Life |
Not Available |
| Protein Binding [%] |
Not Available |
| RxList Link |
RXlist |
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| Drug Reference |
http://www.rxlist.com/cgi/generic2/reteplase.htm |
| Drug Type |
Approved Drug |
| Accession No |
BIOD00013 |
| CAS Registry Number |
133652-38-7 |
| KEGG Compound ID |
Not Available |
| PubChem ID |
Not Available |
| PharmGKB ID |
Not Available |
| SwissProt ID |
TPA_HUMAN (P00750) |
| GenBank ID |
L00153 |
| Drug ID Number [DIN] |
2233013
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