Claims for Patent: 10,220,023

Summary for Patent: 10,220,023

Title:	Dosing regimen for a selective S1P.sub.1 receptor agonist
Abstract:	The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylim- ino)-3-o-tolyl-thiazolidin-4-one.
Inventor(s):	Dingemanse; Jasper (Allschwil, CH), Hoch; Matthias (Harston, GB), Krause; Andreas (Allschwil, CH)
Assignee:	ACTELION PHARMACEUTICALS LTD (Allschwil, CH)
Application Number:	15/534,929
Patent Claims:	1. A method of administering (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylim- ino)-3-o-tolyl-thiazolidin-4-one (Compound 1), or a pharmaceutically acceptable salt thereof, to a human subject in need thereof, for use in the treatment of a disease or disorder associated with an activated immune system, comprising the following steps: during initiation of treatment, or upon re-initiation of treatment after drug discontinuation, administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by (a) administering the maintenance dose of 10 mg of Compound 1 orally once daily from day 12 onwards; or (b) administering 10 mg of Compound 1 orally once daily for 2, 3 or 4 days, followed by administering the maintenance dose of 20 mg of Compound 1 orally once daily, wherein the disease is multiple sclerosis. 2. A method as in claim 1, comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by administering 10 mg of Compound 1 orally once daily for 2, 3 or 4 days; followed by administering the maintenance dose of 20 mg of Compound 1 orally once daily. 3. A method as in claim 1, comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by administering 10 mg of Compound 1 orally once daily on days 12, 13, and 14; followed by administering the maintenance dose of 20 mg of Compound 1 orally once daily from day 15 onwards. 4. A method as in claim 1, comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by administering the maintenance dose of 10 mg of Compound 1 orally once daily from day 12 onwards. 5. A method as in claim 1, wherein the human subject is suffering from relapsing multiple sclerosis. 6. A method as in claim 1, wherein the human subject is suffering from relapsing-remitting multiple sclerosis. 7. The method as in claim 2, wherein the human subject is suffering from relapsing multiple sclerosis. 8. The method as in claim 2, wherein the human subject is suffering from relapsing-remitting multiple sclerosis. 9. The method as in claim 3, wherein the human subject is suffering from relapsing multiple sclerosis. 10. The method as in claim 3, wherein the human subject is suffering from relapsing-remitting multiple sclerosis. 11. The method as in claim 4, wherein the human subject is suffering from relapsing multiple sclerosis. 12. The method as in claim 4, wherein the human subject is suffering from relapsing-remitting multiple sclerosis.