IP Library Granted Patent US 11,771,683
Granted Patent B2
US 11,771,683 · App. 17/090,756 · Granted Oct 3, 2023

Dosing regimen for a selective S1P

Inventors: Jasper Dingemanse (Allschwil, CH); Matthias Hoch (Harston, GB); Andreas Krause (Allschwil, CH)
Assignee: Actelion Pharmaceuticals Ltd
A61K31/426A61K9/0053
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Quick Facts
Patent No.
US 11,771,683
App. No.
17/090,756
Granted
Oct 3, 2023
Kind
B2
Abstract

The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.

Claims (15)

1. A method of administering (R)-5[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one (Compound 1), or a pharmaceutically acceptable salt thereof, to a subject in need thereof, for use in the treatment of a disease or disorder “selected from the group consisting of rejection of transplanted organs selected from kidney, liver, heart and lung; autoimmune syndromes selected from rheumatoid arthritis, psoriasis, psoriatic arthritis, Crohn's disease, and Hashimoto's thyroiditis; and atopic dermatitis” 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 the maintenance dose of 20 mg of Compound 1 to be administered orally once daily.

2. The method of 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 to be administered 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. The method of 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. The method of in claim 1 , comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, is to be administered to a human subject 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. The method of claim 1 , wherein the disease or disorder is the rejection of a transplanted kidney.

6. A method as in claim 1 , wherein the disease or disorder is the rejection of a transplanted liver.

7. A method as in claim 1 , wherein the disease or disorder is the rejection of a transplanted heart.

8. A method as in claim 1 , wherein the disease or disorder is the rejection of a transplanted lung.

9. A method as in claim 1 , wherein the disease or disorder is rheumatoid arthritis.

10. A method as in claim 1 , wherein the disease or disorder is psoriasis.

11. A method as in claim 1 , wherein the disease or disorder is psoriatic arthritis.

12. A method as in claim 1 , wherein the disease or disorder is Crohn's disease.

13. A method as in claim 1 , wherein the disease or disorder is ulcerative colitis.

14. A method as in claim 1 , wherein the disease or disorder is Hashimoto's thyroiditis.

15. A method as in claim 1 , wherein the disease or disorder is atopic dermatitis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 29, 2024
From: ACTELION PHARMACEUTICALS LTD
To: VANDA PHARMACEUTICALS INC.
Reel/Frame 066276/0577 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 18, 2020
From: DINGEMANSE, JASPER; HOCH, MATTHIAS; KRAUSE, ANDREAS
To: ACTELION PHARMACEUTICALS LTD
Reel/Frame 054690/0208 →
Continuity (3)
Division 16261327 · Jan 29, 2019
Division 15534929
Related Publication 20210052555A1 · Feb 25, 2021