Dosage regimen of an s1p receptor modulator

Abstract

S1P receptor modulators are administered following a dosage regimen providing a positive benefit-risk profile.

Description

[0001]The present invention relates to a dosage regimen of an S1P receptor modulator or agonist in the course of the treatment of patients suffering from an inflammatory or autoimmune disease or disorder, for example multiple sclerosis (MS).[0002]Multiple sclerosis is the chief cause of neurological disability in young adults and the most common demyelinating disorder of the central nervous system. Available therapies such as interferon-β and glatiramer acetate have modest efficacy and marginal effects on the progression of disability. These biological agents are administered parenterally and are associated, e.g., with injection site reactions and pyretic symptoms, such as flu-like symptoms. Therefore, there is a strong medical need for a safe and effective oral treatment of multiple sclerosis.[0003]Of those people with multiple sclerosis who receive treatment, a significant number continue to experience disease activity clinically or experience side effects that include flu-like sy...

AI Technical Summary

Benefits of technology

[0006]Oral fingolimod is the first compound in the new class of therapeutics called sphingosine 1-phosphate receptor modulators. Fingolimod is believed to reduce the number of lymphocytes circulating in the blood stream by reversibly trapping a proportion of them in the lymph nodes. Consequently, the number of activated lymphocytes reaching the brain is decreased, resulting in reduced inflammatory destruction. This is a new mechanism of action for MS.

[0010]Therefore there is a need to reduce or manage the possible adverse events which may be generated by administration of such a S1P receptor modulator, while administering a dosage which is adequate to treat or prevent the disease for which the compound is administered during the required period of treatment.

Problems solved by technology

Available therapies such as interferon-β and glatiramer acetate have modest efficacy and marginal effects on the progression of disability.

As a result, a substantial population of patients are untreated, including many with active disease.

These MS patients have either tried an existing therapy but discontinued due to intolerance, adverse effects, or perceived lack of efficacy or have not started any therapy because of their concern with adverse effects, fear of self-injection, fear of needles, or belief that currently available options are not effective enough to warrant trial.

Thus, there is a significant unmet need for effective new therapies in MS, which limit or reduce the possible adverse events or side effects.

Administration of a S1P receptor modulator, such as fingolimod may induce adverse events, such as a transient reduction of the heart rate and cardiac conduction at treatment initiation.

Patients may have to stay in hospitals which complicate the treatment and increase the costs of treatment.

Occurrence of adverse events during a drug treatment may induce patient hospitalization or prolongation of existing hospitalization.

Such possible events may also cause the patients to interrupt their treatment, change the recommended dosing regimen on their own or take the medication on an irregular basis, without any medical support or recommendation for doing that.

Images