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

• US 6,306,844 B1
• Filed: 07/14/2000
• Issued: 10/23/2001
• Est. Priority Date: 03/17/1997
• Status: Expired due to Term

• Current Assignee: Wisconsin Alumni Research Foundation (University of Wisconsin System)
• Original Assignee: Wisconsin Alumni Research Foundation (University of Wisconsin System)
• Inventors: Smith, Connie M., DeLuca, Hector F.
• Primary Examiner(s): Moezie, Minna
• Assistant Examiner(s): HUI, SAN MING R
• Application Number:
  US09/616,778
• Time in Patent Office: 466 Days
• Field of Search: 514/167, 552/653
• US Class Current: 514/167
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• 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 17/06 Antipsoriatics
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/02 specific for leukemia
• CPC Class Codes: B22D 17/20 Accessories: Details
• CPC Class Codes: B22D 17/2236 Equipment for loosening or ejecting castings from dies for plastics B29C45/40
• CPC Class Codes: B22D 17/24 Accessories for locating and holding cores or inserts
• CPC Class Codes: C07C 401/00 Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation

Abstract

This invention provides pharmaceutical uses for 2α-methyl-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 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 monocyte 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.

Claims

1. A method of treating metabolic bone disease 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 D₃ having the formula;

2. The method of claim 1 where the disease is renal osteodystrophy.

3. The method of claim 1 wherein 2α

-methyl-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered orally.

4. The method of claim 1 wherein 2α

-methyl-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered parenterally.

5. The method of claim 1 wherein 2α

-methyl-19-nor-20(S)-1α

,25-dihydroxyvitamin D₃ is administered transdermally.

6. The method of claim 1 wherein 2α

-methyl-19-nor-20(S)-1α

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

g to 10 μ

g per day.