Use of 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3 for the prophylaxis of bone diseases

• US 7,214,671 B2
• Filed: 02/19/2004
• Issued: 05/08/2007
• Est. Priority Date: 02/19/2004
• Status: Active Grant

• Current Assignee: Wisconsin Alumni Research Foundation (University of Wisconsin System)
• Original Assignee: Wisconsin Alumni Research Foundation (University of Wisconsin System)
• Inventors: Plum, Lori A., DeLuca, Hector F., Clagette-Dame, Margaret
• Primary Examiner(s): QAZI, SABIHA NAIM
• Application Number:
  US10/782,337
• Publication Number:
  US 20050187201A1
• Time in Patent Office: 1,174 Days
• Field of Search: 514/167, 552/653, 552/167
• US Class Current: 514/167
• CPC Class Codes: A61K 31/59 Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
• CPC Class Codes: A61K 31/593 9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
• CPC Class Codes: A61P 19/10 for osteoporosis

Abstract

This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D₃. 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 and prophylaxis of diseases where bone formation is desired, particularly osteoporosis. 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, as well as use by normal subjects when high bone mass is desired.

Claims

1. A method for prophylaxis of osteoporosis comprising administering to a subject an effective amount of 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ having the formula;

2. The method of claim 1 wherein 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered orally.

3. The method of claim 1 wherein 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered parenterally.

4. The method of claim 1 wherein 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered transdermally.

5. The method of claim 1 wherein said osteoporosis is low bone turnover osteoporosis.

6. The method of claim 1 wherein said osteoporosis is steroid induced osteoporosis.

7. The method of claim 1 wherein said osteoporosis is senile osteoporosis.

8. The method of claim 1 wherein said osteoporosis is postmenopausal osteoporosis.

9. The method of claim 1 wherein 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered to a human in a dosage of from about 0.01 μ

g to about 100 μ

g per day.

10. The method of claim 1 wherein 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered to a human in a dosage of from about 0.1 μ

g to about 10 μ

g per day.

11. The method of claim 1 wherein 2-methylene-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered to an animal in a dosage of from about 0.000 1 μ

g to about 700 μ

g per day.