| Primary information |
|---|
| ID | 1663 |
| ThPP ID | Th1155 |
| Therapeutic Peptide/Protein Name | Urokinase |
| Sequence | KPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSV view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 31126.5 |
| Chemical Formula | C1376H2145N383O406S18 |
| Isoelectric Point | 8.66 |
| Hydrophobicity | -0.466 |
| Melting Point (℃) | 76 |
| Half Life | 12 minutes |
| Description | Low molecular weight form of human urokinase, that consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. Recombinant urokinase plasminogen activator |
| Indication/Disease | Urokinase can be used for the treatment of pulminary embolism, coronary artery thrombosis, IV catheter clearance, and venous and arterial blood clots. |
| Pharmacodynamics | Urokinase is used for the treatment of pulmonary embolisms. The low molecular weight form of human urokinase consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. Urokinase is an enzyme (protein) produced by the kidney, and found in the urine. There are two forms of urokinase which differ in molecular weight but have similar clinical effects. Urokinase is the low molecular weight form. Urokinase acts on the endogenous fibrinolytic system. It converts plasminogen to the enzyme plasmin. Plasmin degrades fibrin clots as well as fibrinogen and some other plasma proteins. |
| Mechanism of Action | Urokinase acts on the endogenous fibrinolytic system. It cleaves the Arg-Val bond in plasminogen to produce active plasmin. Plasmin degrades fibrin clots as well as fibrinogen and other plasma proteins. |
| Toxicity | Urokinase administered by intravenous infusion is rapidly cleared by the liver. Small fractions of the administered dose are excreted in bile and urine |
| Metabolism | Proteolysis |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | N.A. |
| Patents Number | US4258030 |
| Date of Issue | 07/03/81 |
| Date of Expiry | N.A. |
| Drug Interaction | Drotrecogin alfa, Gingko biloba, Ginseng increases risk of bleeding. |
| Target | Plasminogen,Urokinase plasminogen activator surface receptor, Urokinase-type plasminogen activator, Tissue-type plasminogen activator, Plasminogen activator inhibitor 1, 2, Plasma serine protease inhibitor, Low-density lipoprotein receptor-related protein 2, Suppressor of tumorigenicity 14 protein, Nidogen-1 |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Kinlytic |
| Company | N.A. |
| Brand Discription | Kinlytic (urokinase for injection) is a thrombolytic agent obtained from human neonatal kidney cells grown in tissue culture. The principal active ingredient of Kinlytic is the low molecular weight form of urokinase, and consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. |
| Prescribed for | For the lysis of acute massive pulmonary emboli, defined as obstruction of blood flow to a lobe or multiple segments; For the lysis of pulmonary emboli accompanied by unstable hemodynamics, i.e., failure to maintain blood pressure without supportive measures. |
| Chemical Name | N.A. |
| Formulation | Each mL contains 50,000 international units of urokinase activity, 0.5% mannitol, 5% Albumin (Human), and 1% sodium chloride (pH range 6.0 to 7.5). |
| Physcial Appearance | Kinlytic (urokinase injection) is supplied as a sterile lyophilized white powder |
| Route of Administration | Intravenous infusion |
| Recommended Dosage | The loading dose of 4,400 international units per kilogram of Kinlyticâ„¢ (urokinase injection) is given at a rate of 90 mL per hour over a period of 10 minutes. |
| Contraindication | The use of Kinlytic (urokinase injection) is contraindicated in patients with a history of hypersensitivity to the product. It is also containdicated in stages like active internal bleeding, cardiopulmonary resustication, intracranial surgery. |
| Side Effects | hypoxia, cyanosis, dyspnea, tachycardia, hypotension, hypertension, acidosis, fever and/or chills/rigors, back pain, vomiting, and nausea. |
| Useful Link | http://www.drugs.com/mtm/urokinase.html; http://www.rxlist.com/kinlytic-drug.htm |
| PubMed ID | 26876783, 25231010, 24140055, 23482705, 22817872, 20420509, 18030361, 15112999, 25460592 |
| 3-D Structure | Th1155 (View) or (Download) |