AMISELIMOD FOR PREVENTING, TREATING OR AMELIORATING ULCERATIVE COLITIS
Described herein are methods for treating, ameliorating, and/or preventing ulcerative colitis (UC) as well as other inflammatory gastrointestinal disorders using amiselimod. The method of treatment includes dosing amiselimod at a larger initial dose as compared to the eventual maintenance dose.
1 . A method of treating or ameliorating ulcerative colitis in a subject in need thereof, the method comprising:
administering to the subject a first dose of amiselimod, or a pharmaceutically acceptable salt or enantiomer thereof, during a first administration period; and
administering to the subject a second dose of amiselimod, or a pharmaceutically acceptable salt or enantiomer thereof, during a second administration period,
wherein the first dose is larger than the second dose.
2 . The method of claim 1 , wherein administering the first dose to the subject does not induce a negative chronotropic effect in heart rate in the subject.
3 . The method of claim 1 , wherein the first dose is about 1.5 to about 2.5 times larger than the second dose.
4 . The method of claim 1 , wherein the first dose is about 2 times larger than the second dose.
5 . The method of claim 1 , wherein at least one of the first dose and the second dose is a daily dose.
6 . The method of claim 1 , wherein the first dose and the second dose are each independently about 0.05 mg to about 10 mg.
7 . The method of claim 1 , wherein the first dose and second dose are each independently about 0.1 mg to about 1 mg.
8 . The method of claim 1 , wherein the first dose is about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, or about 1.0 mg.
9 . The method of claim 1 , wherein the first dose is about 0.8 mg or about 0.4 mg.
10 . The method of claim 1 , wherein the first administration is period is 1 to 21 days.
11 . The method of claim 1 , wherein the first administration period is 1 to 14 days.
12 . The method of claim 1 , wherein the first administration period is at least 11 days.
13 . The method of claim 1 , wherein the second administration period is at least 1 year.
14 . The method of claim 1 , further comprising administering to the subject at least one additional therapeutic agent that treats or ameliorates ulcerative colitis.
15 . A method of reducing inflammation in a subject's gastrointestinal (GI) tract, the method comprising:
administering to the subject a first dose of amiselimod, or a pharmaceutically acceptable salt or enantiomer thereof, during a first administration period; and
administering to the subject a second dose of amiselimod, or a pharmaceutically acceptable salt or enantiomer thereof, during a second administration period,
wherein the first dose is larger than the second dose.
16 . The method of claim 15 , wherein administering the first dose to the subject does not induce a negative chronotropic effect in heart rate in the subject.
17 . The method of claim 15 , wherein the first dose is about 1.5 to about 2.5 times larger than the second dose.
18 . The method of claim 15 , wherein the first dose is about 2 times larger than the second dose.
19 . The method of claim 15 , wherein at least one of the first dose and the second dose is a daily dose.
20 . The method of claim 15 , wherein the first dose and the second dose are each independently about 0.05 mg to about 10 mg.
21 . The method of claim 15 , wherein the first dose is about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, or about 1.0 mg.
22 . The method of claim 15 , wherein the first dose is about 0.8 mg or about 0.4 mg.
23 . The method of claim 15 , wherein the first administration is period is 1 to 14 days.
24 . The method of claim 15 , wherein the second administration period is at least 1 year.
25 . The method of claim 15 , further comprising administering to the subject at least one additional therapeutic agent that treats or ameliorates ulcerative colitis.
26 . A method of treating mild to moderate ulcerative colitis in a subject in need thereof, the method comprising:
administering to the subject a first dose of amiselimod, or a pharmaceutically acceptable salt or enantiomer thereof, during a first administration period; and
administering to the subject a second dose of amiselimod, or a pharmaceutically acceptable salt or enantiomer thereof, during a second administration period,
wherein the first dose is larger than the second dose.
27 . The method of claim 26 , wherein administering the first dose to the subject does not induce a negative chronotropic effect in heart rate in the subject.
28 . The method of claim 26 , wherein the first dose is about 1.5 to about 2.5 times larger than the second dose.
29 . The method of claim 26 , wherein the first dose is about 2 times larger than the second dose.
30 . The method of claim 26 , wherein at least one of the first dose and the second dose is a daily dose.
31 . The method of claim 26 , wherein the first dose and the second dose are each independently about 0.05 mg to about 10 mg.
32 . The method of claim 26 , wherein the first dose and second dose are each independently about 0.1 mg to about 1 mg.
33 . The method of claim 26 , wherein the first dose is about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, or about 1.0 mg.
34 . The method of claim 26 , wherein the first dose is about 0.8 mg or about 0.4 mg.
35 . The method of claim 26 , wherein the first administration is period is 1 to 21 days.
36 . The method of claim 26 , wherein the first administration period is 1 to 14 days.
37 . The method of claim 26 , wherein the first administration period is at least 11 days.
38 . The method of claim 26 , wherein the second administration period is at least 1 year.
39 . The method of claim 26 , further comprising administering to the subject at least one additional therapeutic agent that treats or ameliorates ulcerative colitis.
40 . The method of claim 26 , wherein the first dose is administered once a day (QD), twice a day (BID), three times a day (TID), or four times a day (QID), optionally wherein the first dose is administered once a day (QD).
41 . (canceled)
42 . The method of claim 26 , wherein the second dose is administered once a day (QD), twice a day (BID), three times a day (TID), or four times a day (QID), optionally wherein the second dose is administered once a day (QD).
43 . (canceled)
44 . The method of claim 40 , wherein at least one of the following applies:
(a) the second dose is administered QD, BID, TID, or QID every other day during the second administration period;
(b) the second dose is administered QD, BID, TID, or QID every two days during the second administration period;
(c) the second dose is administered QD, BID, TID, or QID every three days during the second administration period;
(d) the second dose is administered QD, BID, TID, or QID every four days during the second administration period;
(e) the second dose is administered QD, BID, TID, or QID every five days during the second administration period;
(f) the second dose is administered QD, BID, TID, or QID every six days during the second administration period;
(g) the second dose is administered QD, BID, TID, or QID every seven days during the second administration period.
45 - 50 . (canceled)