Repositioning Candidate Details
| Candidate ID: | R0005 |
| Source ID: | DB00015 |
| Source Type: | approved; investigational |
| Compound Type: | biotech |
| Compound Name: | Reteplase |
| Synonyms: | Human t-PA (residues 1-3 and 176-527); Reteplase; Reteplase, recombinant; Reteplase,recombinant |
| Molecular Formula: | -- |
| SMILES: | -- |
| DrugBank 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). |
| CAS Number: | 133652-38-7 |
| Molecular Weight: | |
| DrugBank Indication: | For lysis of acute pulmonary emboli, intracoronary emboli, and management of myocardial infarction. |
| DrugBank Pharmacology: | Reteplase 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. |
| DrugBank MoA: | Reteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then 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. |
| Targets: | Plasminogen activator; Fibrinogen alpha chain; Plasminogen activator inhibitor 1 |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I08 | 114 | Cardiovascular system disease | A disease of anatomical entity which occurs in the blood, heart, blood vessels or the lymphatic system that passes nutrients (such as amino acids and electrolytes), gases, hormones, blood cells or lymph to and from cells in the body to help fight diseases and help stabilize body temperature and pH to maintain homeostasis. http://en.wikipedia.org/wiki/Circulatory_system | disease of anatomical entity | Details |