Dosing regimen for a selective S1P1 receptor agonist

Patent metadata

Field	Value
Publication number	US-11771683-B2
Application number	US-202017090756-A
Country	US
Kind code	B2
Filing date	Nov 5, 2020
Priority date	Dec 11, 2014
Publication date	Oct 3, 2023
Grant date	Oct 3, 2023

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.

First claim

The invention claimed is:

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.

Assignees

• Actelion Pharmaceuticals Ltd

Inventors

• Dingemanse Jasper
• Hoch Matthias
• Krause Andreas

Classifications

• A61K31/426 Primary

  1,3-Thiazoles · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K31/22 Primary

  of acyclic acids, e.g. pravastatin · CPC title

• A61K31/225

  Polycarboxylic acids · CPC title

• A61K31/4015

  having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide · CPC title