Formulations and Treatment Methods

Abstract

The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

1 . A pharmaceutical formulation comprising one or more excipients and a compound having the structure  
     
       
         
         
             
             
         
       
       wherein,  
       R 1  is —OH, an ether or an ester; and  
       R 4  is optionally substituted C 2-8  alkynyl.  
     
   
   
       2 . The pharmaceutical formulation of  claim 1  wherein R 1  is —OH and R 4  is —CCH.  
   
   
       3 . The pharmaceutical formulation of  claim 1  wherein R 1  is —OH and R 4  is —CCCH 3 .  
   
   
       4 . A method to treat prostate cancer or breast cancer in a subject comprising administering to the subject an effective amount of a compound having the structure  
     
       
         
         
             
             
         
       
       wherein,  
       R 1  is —OH, an ether or an ester; and  
       R 4  is optionally substituted C 2-8  alkynyl.  
     
   
   
       5 . The method of  claim 4  wherein R 1  is —OH and R 4  is —CCH.  
   
   
       6 . The method of  claim 5  wherein the subject has prostate cancer.  
   
   
       7 . The method of  claim 4  wherein R 1  is —OH and R 4  is —CCCH 3 .  
   
   
       8 . The method of  claim 7  wherein the subject has prostate cancer.