# US 8,785,484 B2 · Dosing regimen for a selective S1P1 receptor agonist

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- Number: US 8,785,484 B2
- Document ID: US8785484B2
- Status: Granted
- Kind: B2
- Application number: 12/922,777
- Filed: 2009-03-12
- Published: 2011-01-27
- Granted: 2014-07-22
- Earliest claimed: 2008-03-17
- Assignees: Actelion Pharmaceuticals Ltd.
- Applicants: Patrick Brossard; Jasper Dingemanse; Oliver Nayler; Michael Scherz; Beat Steiner
- Inventors: Patrick Brossard; Jasper Dingemanse; Oliver Nayler; Michael Scherz; Beat Steiner
- Web page: https://patentgrep.com/patent/US8785484B2

## CPC

- A61K 31/426: 1,3-Thiazoles
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/425: Thiazoles
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/06: Antiarrhythmics
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to a dosing regimen for a selective S1P1 receptor agonist, whereby the selective S1P1 receptor agonist is administered to a subject in such a way that during the initial treatment phase the selective S1P1 receptor agonist is administered at a dose which induces desensitization of the heart wherein said dose is below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of the selective S1P1 receptor agonist.

## Claims

### Claim 1

A method for 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, wherein, during the an initial treatment phase Compound 1, or a pharmaceutically acceptable salt thereof is administered at a dose which induces desensitization of the heart to acute heart rate reduction, said dose being below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of Compound 1, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according to claim 1, wherein the dose in the initial treatment phase is between 2- to 5-fold lower than the target dose.

### Claim 3 (depends on 1)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according to claim 1, wherein the dose in the initial treatment phase is between 5- to 16-fold lower than the target dose.

### Claim 4 (depends on 1)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according to claim 1, wherein the dose below the target dose is administered to the subject during the initial 2 to 4 days of the treatment.

### Claim 5 (depends on 1)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according claim 1, wherein the dose below the target dose is administered at a dosing frequency of once or twice daily.

### Claim 6 (depends on 3)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according claim 3, wherein the dose below the target dose is administered at a dosing frequency of once or twice daily.

### Claim 7 (depends on 1)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according claim 1, wherein the target dose is 20 mg of Compound 1 administered p.o. once daily.

### Claim 8 (depends on 3)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according claim 3, wherein the target dose is 20 mg of Compound 1 administered p.o. once daily.

### Claim 9 (depends on 5)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according claim 5, wherein the target dose is 20 mg of Compound 1 administered p.o. once daily.

### Claim 10 (depends on 6)

The method for administering Compound 1, or a pharmaceutically acceptable salt thereof, according claim 6, wherein the target dose is 20 mg of Compound 1 administered p.o. once daily.