Radioactive arsenic-containing compounds and their uses in the treatment of tumors

Abstract

This invention provides a process for producing a radioactive arsenic-containing compound, comprising the steps of: (i) subjecting an arsenic-containing compound to a neutron irradiation treatment, said arsenic-containing compound being selected from a group consisting of As 2 O 3 , As 2 S 3 , AS 2 S 2 , and a combination thereof, such that the arsenic element contained in the arsenic-containing compound is converted to a radioactive arsenic isotope; and (ii) recovering the resultant product from step (i). This invention also provides a pharmaceutical composition comprising a therapeutically effective amount of the radioactive arsenic-containing compound and a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the treatment of tumors/cancers such as hematological malignancies and solid tumors.

We claim:  
     
         1 . A pharmaceutical composition, comprising: 
 (a) a therapeutically effective amount of a radioactive arsenic-containing compound, said radioactive arsenic-containing compound being prepared by a process comprising the steps of: 
 (i) subjecting an arsenic-containing compound selected from a group consisting of As 2 O 3 , As 2 S 3 , AS 2 S 2 , and a combination thereof to a neutron irradiation treatment such that the arsenic element contained in said arsenic-containing compound is converted to a radioactive arsenic isotope; and  
 (ii) recovering the resultant product from step (i); and  
   (b) a pharmaceutically acceptable carrier.    
     
     
         2 . The pharmaceutical composition according to  claim 1 , wherein said radioactive arsenic-containing compound can emit γ particles and β particles.  
     
     
         3 . The pharmaceutical composition according to  claim 1 , wherein said radioactive arsenic-containing compound contains an  76 As isotope.  
     
     
         4 . The pharmaceutical composition according to  claim 1 , wherein said radioactive arsenic-containing compound is As 2 O 3  having subjected to the neutron irradiation treatment.  
     
     
         5 . The pharmaceutical composition according to  claim 1 , which is formulated into an injection formulation.  
     
     
         6 . A process for preparing a radioactive arsenic-containing compound, comprising the steps of: 
 (i) subjecting anarsenic-containing compound selected from a group consisting of As 2 O 3 , AS 2 S 3 , As 2 S 2 , and a combination thereof to a neutron irradiation treatment such that the arsenic element contained in said arsenic-containing compound is converted to a radioactive arsenic isotope; and    (ii) recovering the resultant product from step (i).    
     
     
         7 . The process according to  claim 6 , wherein the resultant product recovered in step (ii) can emit γ particles and β particles.  
     
     
         8 . The process according to  claim 6 , wherein the resultant product recovered by step (ii) contains an  76 As isotope.  
     
     
         9 . The process according to  claim 6 , wherein said arsenic-containing compound used in step (i) is As 2 O 3 .  
     
     
         10 . A pharmaceutical composition for treating a tumor or cancer, comprising 
 (a) a therapeutically effective amount of a radioactive arsenic-containing compound prepared by the process of  claim 6;  and    (b) a pharmaceutically acceptable carrier.    
     
     
         11 . The pharmaceutical composition of  claim 10 , wherein the tumor or cancer is selected from a group consisting of hematological malignancies and solid tumors.  
     
     
         12 . The pharmaceutical composition according to claim  11 , wherein the solid tumors are selected from a group consisting of breast cancer, rectal cancer, liver tumor, ovarian cancer and prostate cancer.  
     
     
         13 . The pharmaceutical composition according to  claim 12 , wherein the liver tumor is selected from a group consisting of hepatocellular carcinoma, cholangiocarcinoma, liver cell carcinoma, fibrolamellar variant of hepatocellular carcinoma, intrahepatic bile duct carcinoma, mixed hepatocellular cholangicocarinomoa, undifferentiated hepatocellular carcinoma, hepatoma with tumor invasion to common bile duct, hepatoblastoma, childhood hepatic tumor and primary hepatocellular carcinoma.  
     
     
         14 . The pharmaceutical composition according to  claim 10 , which is formulated into an injection formulation.  
     
     
         15 . The pharmaceutical composition according to  claim 10 , wherein said radioactive arsenic-containing compound can emit γ particles and β particles.  
     
     
         16 . The pharmaceutical composition according to  claim 10 , wherein said radioactive arsenic-containing compound is As 2 O 3  having subjected to the neutron irradiation treatment.  
     
     
         17 . The pharmaceutical composition according to  claim 10 , wherein said radioactive arsenic-containing compound contains an  76 As isotope.