Use of 2alpha-methyl-19-nor-20(S)-1alpha,25-dihydroxyvitamin D3 to increase bone strength

Abstract

This invention provides pharmaceutical uses for 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3 . This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment of diseases where bone formation is desired, particularly osteoporosis. This compound also exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocle thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. This compound also increases both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.

We claim:  
     
         1 . A method of treating metabolic bone disease where it is desired to maintain or increase bone mass comprising administering to a patient with said disease an effective amount of 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  having the formula:  
       
         
           
           
               
               
           
         
       
     
     
         2 . The method of  claim 1  where the disease is senile osteoporosis.  
     
     
         3 . The method of  claim 1  where the disease is postmenopausal osteoporosis.  
     
     
         4 . The method of  claim 1  where the disease is steroid-induced osteoporosis.  
     
     
         5 . The method of  claim 1  where the disease is a low bone turnover osteoporosis.  
     
     
         6 . The method of  claim 1  where the disease is osteomalacia.  
     
     
         7 . The method of  claim 1  where the disease is renal osteodystrophy.  
     
     
         8 . The method of  claim 1  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered orally.  
     
     
         9 . The method of  claim 1  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered parenterally.  
     
     
         10 . The method of  claim 1  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered transdermally.  
     
     
         11 . The method of  claim 1  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered in a dosage of from 0.1 μg to 10 μg per day.  
     
     
         12 . A method of treating psoriasis comprising administering to a patient with psoriasis an effective amount of 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  having the formula:  
       
         
           
           
               
               
           
         
       
     
     
         13 . The method of  claim 12  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered orally.  
     
     
         14 . The method of  claim 12  2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered parenterally.  
     
     
         15 . The method of  claim 12  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered transdermally.  
     
     
         16 . The method of  claim 12  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered topically.  
     
     
         17 . The method of  claim 12  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered in a dosage of from about 0.01 μg/day to about 10 μg/day.  
     
     
         18 . A method of treating leukemia, colon cancer, breast cancer or prostate cancer comprising administering to a patient with said disease an effective amount of 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  having the formula:  
       
         
           
           
               
               
           
         
       
     
     
         19 . The method of  claim 18  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered orally.  
     
     
         20 . The method of  claim 18  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered parenterally.  
     
     
         21 . The method of  claim 18  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered transdermally.  
     
     
         22 . The method of  claim 12  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered in a dosage of from about 0.01 μg/day to about 10 μg/day.  
     
     
         23 . A method of increasing the strength of a bone comprising administering to a patient in need of such treatment an effective amount of 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  having the formula:  
       
         
           
           
               
               
           
         
       
     
     
         24 . The method of  claim 23  wherein the bone strength is cortical strength.  
     
     
         25 . The method of  claim 23  wherein the bone strength is trabecular strength.  
     
     
         26 . The method of  claim 23  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered orally.  
     
     
         27 . The method of  claim 23  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered parenterally.  
     
     
         28 . The method of  claim 23  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered transdermally.  
     
     
         29 . The method of  claim 23  wherein 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D 3  is administered in a dosage of from 0.1 μg to 10 μg per day.