Selective progesterone receptor modulator (sprm) regimen

Abstract

The invention is directed to a pharmaceutical composition comprising a progesterone receptor antagonist namely (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethy)estra-4,9-dien-3-one for the treatment and/or prophylaxis of Uterine Fibroids (myomas, uterine leiomyoma) that is administered to a patient diagnosed with Uterine Fibroids following a specific regimen. Additionally, the invention is directed to a method for treating Uterine Fibroids (myomas, uterine leiomyoma) and/or for reducing Uterine Fibroids (myomas, uterine leiomyoma) size and symptoms related to Uterine Fibroids following a specific regimen as well as treatment of Heavy Menstrual Bleeding (HMB).

1 . A pharmaceutical composition comprising (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula 
       
         
           
           
               
               
           
         
         or salts, solvates or solvates of the salts, including all crystal modifications thereof for the treatment and/or prophylaxis of Uterine Fibroids wherein Compound 1 is administered daily during a period of four (4) weeks to one (1) year, preferably, twelve (12) weeks up to twenty-four (24) weeks. 
       
     
     
         2 . The pharmaceutical composition according to  claim 1  wherein the administration period of (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) is followed by a break period wherein administration of Compound 1 is discontinued until one (1) or two (2) bleeding episodes occur and administration and break periods are repeated at least one (1) time. 
     
     
         3 . The pharmaceutical composition according to  claim 1  wherein Compound 1 is administered during a period of twelve (12) weeks, sixteen (16) weeks, twenty (20) weeks or twenty-four (24) weeks. 
     
     
         4 . A method for treating Uterine Fibroids by administrating to a patient a pharmaceutical composition comprising (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula 
       
         
           
           
               
               
           
         
         or salts, solvates or solvates of the salts, including all crystal modifications thereof wherein Compound 1 is administered daily during a period of four (4) weeks to one (1) year, preferably, twelve (12) weeks up to twenty-four (24) weeks followed by a break wherein administration of Compound 1 is discontinued until one (1) or two (2) bleeding episodes occur; optionally administration and break are repeated at least one (1) time. 
       
     
     
         5 . A method for reducing Uterine Fibroids size and/or reducing symptoms related to Uterine Fibroids by administrating to a patient a pharmaceutical composition comprising (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula 
       
         
           
           
               
               
           
         
         or salts, solvates or solvates of the salts, including all crystal modifications thereof wherein Compound 1 is administered daily during a period of four (4) weeks to one (1) year, preferably, twelve (12) weeks up to twenty-four (24) weeks followed by a break wherein administration of Compound 1 is discontinued until one (1) or two (2) bleeding episodes occur; optionally administration and break are repeated at least one (1) time. 
       
     
     
         6 . A method for treating Heavy Menstrual Bleeding (HMB) by administrating to a patient a pharmaceutical composition comprising (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula 
       
         
           
           
               
               
           
         
         or salts, solvates or solvates of the salts, including all crystal modifications thereof wherein Compound 1 is administered daily during a period of four (4) weeks to one (1) year, preferably, twelve (12) weeks up to twenty-four (24) weeks followed by a break wherein administration of Compound 1 is discontinued until one (1) or two (2) bleeding episodes occur; optionally administration and break are repeated at least one (1) time. 
       
     
     
         7 . The method according to  claim 3  wherein Compound 1 is administered during a period of twelve (12) weeks, sixteen (16) weeks, twenty (20) weeks or twenty-four (24) weeks. 
     
     
         8 . A Compound 1 defined as (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one of formula 
       
         
           
           
               
               
           
         
         or salts, solvates or solvates of the salts, including all crystal modifications thereof for the use in a method for treating and/or prophylaxis of Uterine Fibroids wherein 
         a) Compound 1 is administered daily during a period of four (4) weeks to one (1) year, preferably, ten (10) weeks up to twenty six (26) weeks. 
       
     
     
         9 . The compound according to  claim 8  where step a) is followed by
 b) a break period wherein administration of Compound 1 is discontinued and encompass one (1) or two (2) bleeding episodes and 
 c) step a) and/or b) are/is repeated at least one (1) time. 
 
     
     
         10 . The compound according to  claim 8  where amenorrhea is reached during step a). 
     
     
         11 . The compound according to  claim 8  where ovulation inhibition is reached during step a).