Composition for inhibition of cathepsin K
The present invention relates to the a method of inhibiting bone resorption in a mammal in need thereof with an oral pharmaceutical composition comprising a cathepsin K inhibitor, or a pharmaceutically acceptable salt thereof, or a mixture thereof, according to a continuous schedule having a dosage interval of once weekly, biweekly, twice monthly or once monthly.
1. A method of inhibiting bone resorption in a human in need thereof consisting of administering to the human 50 mg of N 1 -(1-cyanocyclopropyl)-4-fluoro-N 2 -{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof, as an oral unit dose according to a once weekly dosing regimen.
2. The method according to claim 1 where the oral unit dose is a tablet.
3. The method according to claim 1 for treating osteoporosis.
4. A method of treating osteoporosis in a human in need thereof consisting of administering to the human 50 mg of N 1 -(1-cyanocyclopropyl)-4-fluoro-N 2 -{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide as an oral unit dose according to a once weekly dosing regimen.
5. A method of treating osteoporosis in a human in need thereof consisting of administering to the human 50 mg of N 1 -(1-cyanocyclopropyl)-4-fluoro-N 2 -{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide and 5,600 IU of Vitamin D3 as an oral unit dose according to a once weekly dosing regimen.
6. The method according to claim 3 for treating osteoporosis in a postmenopausal woman.
7. The method according to claim 4 where the oral unit dose is a tablet.
8. The method according to claim 4 for treating osteoporosis in a postmenopausal woman.
9. The method according to claim 1 consisting of administering to the human 50 mg of N 1 -(1-cyanocyclopropyl)-4-fluoro-N 2 -{(1S) -2,2,2-trifluoro-1-[4′-(methylsulfonyl) -1,1′-biphenyl-4-yl]lethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof and Vitamin D, as an oral unit dose according to a once weekly dosing regimen.
10. The method according to claim 9 for treating osteoporosis.
11. The method according to claim 10 for treating osteoporosis in a postmenopausal woman.
12. A method of inhibiting bone resorption in a human in need thereof consisting of administering to the human 50 mg of N 1 -(1-cyanocyclopropyl)-4-fluoro-N 2 -{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]lethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof and Vitamin D, as an oral unit dose according to a once weekly dosing regimen.
13. The method according to claim 12 consisting of administering to the human 50 mg of N 1 -(1-cyanocyclopropyl)-4-fluoro-N 2 -{(1S) -2,2,2-trifluoro-1-[4′-(methylsulfonyl) -1,1′-biphenyl-4-yl]lethyl}-L-leucinamide or a pharmaceutically acceptable salt thereof and Vitamin D, as an oral unit dose according to a once weekly dosing regimen.
14. The method according to claim 13 wherein the Vitamin D is Vitamin D3.
15. The method according to claim 14 wherein the amount of Vitamin D3 is from about 100 to 60,000 IU.
16. The method according to claim 15 wherein the amount of Vitamin D3 is 2,400 IU, 5,600 IU, 7,000 IU, 8,400 IU, 11,200 IU, 14,000 IU, 15,400 IU, 16,800 IU or 19,600 IU.
17. The method according to claim 16 wherein the amount of Vitamin D3 is 5,600 IU.
18. The method according to claim 16 wherein the amount of Vitamin D3 is 8,400 IU.
19. The method according to claim 16 wherein the amount of Vitamin D3 is 11,200 IU.
20. The method according to claim 13 for treating osteoporosis.
21. The method according to claim 20 for treating osteoporosis in a postmenopausal woman.