New use

Abstract

According to the invention there is provided a kit of parts comprising: (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier; and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, which components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other, as well as the use of such a kit of parts in the treatment of a condition in which inhibition of thrombin is required or desired.

1 . A kit of parts comprising: 
 (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier; and    (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier,    which components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other.    
     
     
         2 . A kit of parts as claimed in  claim 1 , wherein the prodrug of component (b) is a prodrug of the thrombin inhibitor of component (a).  
     
     
         3 . A kit of parts as claimed in  claim 1 , wherein components (a) and (b) are suitable for sequential, separate and/or simultaneous use in the treatment of a condition in which inhibition of thrombin is required or desired.  
     
     
         4 . A kit of parts as claimed in  claim 3 , wherein the condition is deep venous thrombosis.  
     
     
         5 . A kit of parts as claimed in  claim 1 , wherein the thrombin inhibitor is melagatran.  
     
     
         6 . A kit of parts as claimed in  claim 5 , wherein the prodrug is of the formula  
         R 1 O 2 C—CH 2 —(R)Cgl-Aze-Pab-OH, wherein R 1  represents linear or branched C 1-6  alkyl and the OH group replaces one of the amidino hydrogens in Pab.    
     
     
         7 . A kit of parts as claimed in  claim 6 , wherein R 1  represents methyl, ethyl or propyl.  
     
     
         8 . A kit of parts as claimed in  claim 1 , wherein the formulation comprising thrombin inhibitor, or derivative thereof, is a parenteral formulation and that comprising the prodrug, or derivative thereof, is an oral formulation.  
     
     
         9 . A method of making a kit of parts as defined in  claim 1 , which method comprises bringing a component (a) according to  claim 1 , into association with a component (b) according to  claim 1 , thus rendering the two components suitable for administration in conjunction with each other.  
     
     
         10 . A kit of parts comprising: 
 (1) one of components (a) and (b) as defined in  claim 1;  together with    (2) instructions to use that component in conjunction with the other of the two components.    
     
     
         11 . A pharmaceutical formulation including a low molecular weight thrombin inhibitor (or a pharmaceutically acceptable derivative thereof) and a prodrug of a low molecular weight thrombin (or a pharmaceutically acceptable derivative of that prodrug), in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.  
     
     
         12 . A method of treatment of a condition in which inhibition of thrombin is required or desired, which comprises administration of: 
 (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier; in conjunction with    (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, to a patient suffering from, or susceptible to, such a condition.    
     
     
         13 . A method as claimed in  claim 12  in which component (a) is administered prior to commencement of administration of component (b).  
     
     
         14 . A method of treatment of a condition in which inhibition of thrombin is required or desired, which comprises administration of a formulation as defined in  claim 11  to a patient suffering from, or susceptible to, such a condition.  
     
     
         15 . A method as claimed in any one of  claims 12  to  14 , wherein the condition is deep venous thrombosis.  
     
     
         16 . A method as claimed in  claim 15 , wherein the thrombosis results from surgery.  
     
     
         17 . A method as claimed in  claim 16 , wherein the surgery is gastrointestinal surgery or orthopaedic surgery.  
     
     
         18 . A method as claimed in  claim 16 , wherein component (a) is administered parenterally prior to and/or after surgery and component (b) is administered orally following that surgery.  
     
     
         19 . The use of a thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in the manufacture of a medicament for the treatment or prophylaxis of a condition in which inhibition of thrombin is required or desired, which treatment or prophylaxis comprises administration of: 
 (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier; in conjunction with    (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, to a patient suffering from, or susceptible to, such a condition.