Urokinase

  • CAS Number: 9039-53-6

Urokinase or urokinase-type plasminogen activator ( uPA short ) is an enzyme from the group of peptidases ( proteases also ), which is used for the treatment of myocardial infarction, pulmonary embolism and other thrombotic vascular occlusions, as well as for the therapy and prophylaxis of thrombotic catheter locks.

Urokinase was first discovered in human urine and described as a protease. Physiologically, it circulates in the bloodstream and is plasminogen to plasmin which is a serine proteinase which dissolves various proteins in the plasma and, in particular fibrin clot. This process is known as fibrinolysis, and the activity of urokinase as a drug based on this mechanism. Urokinase is inhibited by the plasminogen activator inhibitors PAI-1 and PAI -2.

It was found that the expression of urokinase and PAI -1 is significantly elevated in various cancers and may serve as a prognostic marker.

Its effect can be reversed by administration of tranexamic acid.

Urokinase receptor

When urokinase to its cellular receptor, by glycosylphosphatidylinositol anchor ( GPI anchor ) attached to the cell membrane urokinase receptor ( uPAR ) is attached is greatly increased its proteolytic activity. In addition, the cell by the binding of urokinase to the uPAR mitotic signaling pathways activated and increased cellular migration. These processes are independent of the proteolytic activity of urokinase.

Indications

Urokinase is approved in Germany for use in

  • Peripheral arterial thrombosis
  • Acute and subacute thrombosis, deep venous
  • Acute pulmonary embolism diagnosis secured, especially in unstable hemodynamic conditions
  • Arteriovenous shunt thrombosiertem
  • For the prevention of infectious and thrombotic complications of central venous catheters
  • Restoration of patency of central venous catheters thrombotic closed, including hemodialysis.

Trade names

Urokinase is in Germany, Austria and Switzerland under the name of urokinase HS Medac in six dosage strengths (10,000 / 50,000 / 100,000 / 250,000 / 500,000 / 1,000,000 IU) available.

Human Genome Organisation CAS registry number Anatomical Therapeutic Chemical Classification System DrugBank MEROPS Organism Plasminogen activator inhibitor-1
794832
de