Therapeutic regimens
View Patent ↗This invention relates to clinically useful therapeutic regimens comprising the administration of (R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol.
1. A unit dosage form suitable for once daily administration to a human subject in need thereof comprising 0.9 mg to 1.1 mg, 2.2 mg to 2.8 mg, 4.4 mg to 5.6 mg, or 9 mg to 11 mg of the compound of formula I as its dihydrochloride salt
2. The unit dosage form according to claim 1 , further comprising one or more pharmaceutically acceptable excipients.
3. The unit dosage form according to claim 2 , wherein the unit dosage form is a tablet or capsule suitable for oral administration.
4. A unit dosage form comprising 0.9 mg to 1.1 mg, 2.2 mg to 2.8 mg, 4.4 mg to 5.6 mg, or 9 mg to 11 mg of the compound of formula I or a salt thereof
wherein following oral administration the unit dosage form, is more than 50% dissolved in the stomach prior to being released into the small intestines.
5. The unit dosage form according to claim 4 , wherein the unit dosage form is not coated with an acid resistant coating.
6. A method of treating vasomotor disturbances in a peri-menopausal or postmenopausal woman in need thereof comprising administering to the woman a composition comprising a compound of formula I or a salt thereof
at a daily total dosage of the compound of formula I or a salt thereof at a range from 0.9 mg to 1.1 mg, 2.2 mg to 2.8 mg, 4.4 mg to 5.6 mg, or 9 mg to 11 mg.
7. The method according to claim 6 , wherein the composition is administered orally, once-daily.
8. The method according to claim 7 , wherein the composition is a tablet or capsule suitable for oral administration.
9. The method according to claim 8 , wherein the composition is more than 50% dissolved in the stomach prior to being released into the small intestines.
10. The method according to claim 9 , wherein the composition is not coated with an acid resistant coating.
11. A method of treating vasomotor disturbances in a peri-menopausal or postmenopausal woman in need thereof comprising administering to the woman a compound of formula I or a salt thereof
wherein the administration results in a steady state Cmax of from 0.40 ng/mL to 1.43 ng/mL.
12. The method of claim 11 , wherein a steady state trough level of the compound of formula I ranging from 0.11 ng/mL to 0.79 ng/mL or ranging from 0.12 ng/mL to 0.86 ng/mL is achieved.
13. The method of claim 11 , wherein the compound of formula I is in the form of a dihydrochloride salt.
14. The method of claim 13 , wherein the compound of formula I or a salt thereof is orally administered once-daily.
15. The method of claim 14 , wherein the compound is in a unit dosage form.
16. The method of claim 15 , wherein the compound is administered as a capsule or tablet.
17. The method of claim 16 , wherein the capsule or tablet is more than 50% dissolved in the stomach prior to being released into the small intestines.
18. The method according to claim 17 , wherein the unit dosage form is not coated with an acid resistant coating.
19. A method of treating vasomotor disturbances in a peri-menopausal or postmenopausal woman in need thereof comprising administering to the woman a compound of formula I or a salt thereof
wherein the administration results in a steady state Cmax of from 0.22 ng/mL to 1.61 ng/mL.
20. The method of claim 19 , wherein the compound of formula 1 is in its dihydrochloride salt form.
21. The method of claim 19 , wherein a steady state trough level of the compound of formula I ranging from 0.11 ng/mL to 0.79 ng/mL or ranging from 0.12 ng/mL to 0.86 ng/mL is achieved.
22. The method of claim 19 , wherein the compound of formula I is in the form of a dihydrochloride salt.
23. The method of claim 22 , wherein the compound of formula I or a salt thereof is orally administered once-daily.
24. The method of claim 23 , wherein the compound is in a unit dosage form.
25. The method of claim 24 , wherein the unit dosage formulation is a capsule or tablet.
26. The method of claim 25 , wherein the capsule or tablet is more than 50% dissolved in the stomach prior to being released into the small intestines.
27. The method according to claim 26 , wherein the unit dosage form is not coated with an acid resistant coating.
28. The unit dosage form according to claim 1 , wherein the unit dosage form comprises 1 mg, 2.5 mg, 5 mg, or 10 mg of the compound of Formula I or a salt thereof.
29. The unit dosage form according to claim 4 , further comprising one or more pharmaceutically acceptable excipients.
30. The unit dosage form according to claim 29 , wherein the unit dosage form is a tablet or capsule suitable for oral administration.
31. The unit dosage form according to claim 4 , wherein the unit dosage form comprises 1 mg, 2.5 mg, 5 mg, or 10 mg of the compound of Formula I or a salt thereof.
32. The unit dosage form according to claim 4 , wherein the unit dosage form comprises an acid addition salt of the compound of Formula I.
33. The unit dosage form according to claim 32 , wherein the unit dosage form comprises a dihydrochloride salt of the compound of Formula I.
34. The method according to claim 6 , wherein the daily total dosage of the compound of Formula I or a salt thereof is 1 mg, 2.5 mg, 5 mg, or 10 mg.
35. The method according to claim 6 , wherein the composition comprises an acid addition salt of the compound of Formula I.
36. The method according to claim 35 , wherein the composition comprises a dihydrochloride salt of the compound of Formula I.