Pharmaceutical composition for treating ulcerative colitis
Inventors
Kageyama, Shunsuke • GODA, Yoshiki • Sugiura, Toshihiko
Assignees
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Publication Number
US-10183022-B2
Publication Date
2019-01-22
Expiration Date
Abstract
Provided is a pharmaceutical composition for treating ulcerative colitis, comprising a compound represented by a formula (1) or a pharmaceutically acceptable salt thereof, wherein the compound or the pharmaceutically acceptable salt is administered in an amount of 600 mg or more per day to an ulcerative colitis patient.
Core Innovation
A pharmaceutical composition and treatment method are described for ulcerative colitis that use, as an active ingredient, a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. The method administers the compound to an ulcerative colitis patient at a daily amount of 1500 mg or more per day, with preferred oral administration and dosing in multiple daily administrations.
The described approach is targeted to ulcerative colitis patients, including active-stage patients, in whom treatment with 5-aminosalicylic acid and/or a corticosteroid is insufficient in effect or is not tolerated. Patient criteria discussed include assessments using Mayo score and subscores such as stool frequency, bloody stool, mucosal finding, and physician’s global assessment, including thresholds consistent with active-stage disease ranges.
An 8-week randomized comparison is presented to support the treatment. The comparison evaluates Example 1 versus a placebo, including a regimen corresponding to 960 mg compound (1) 3 times/day, and reports improvements in response and remission outcomes, including mucosal remission and histopathological assessment using Riley score. Safety outcomes are described as showing no severe drug-related adverse events.
Claims Coverage
The independent claim is directed to a method for treating ulcerative colitis by administering a compound represented by formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient at a daily dose of at least 1500 mg per day. The claim family includes four inventive features refining dose amount, patient and therapy context, preparation form, and dosing frequency.
Daily dose of 1500 mg or more per day
Administering a compound represented by formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient in an amount of 1500 mg or more per day to an ulcerative colitis patient.
Active-stage patient with insufficient effect or intolerance to prior therapies
Treating an ulcerative colitis patient in an active stage whose treatment with a 5-aminosalicylic acid preparation and/or a corticosteroid preparation is insufficient or is not tolerated.
Oral preparation administration
Formulating the compound represented by formula (1) or a pharmaceutically acceptable salt in the form of an oral preparation for administration.
Administration 1 to 5 times per day
Administering the compound represented by formula (1) or a pharmaceutically acceptable salt 1 to 5 times per day.
The key coverage centers on treating ulcerative colitis with a compound represented by formula (1) or a pharmaceutically acceptable salt at a daily dose of at least 1500 mg, with refinements addressing active-stage patients with insufficient effect or intolerance to 5-aminosalicylic acid and/or corticosteroid therapy, oral preparation use, and multi-dose administration frequency.
Stated Advantages
Improved response and remission outcomes in the 8-week randomized comparison versus placebo.
Improved mucosal remission outcomes versus placebo.
Histopathological improvement as indicated by Riley score reduction.
No severe drug-related adverse events are reported.
Documented Applications
Use in a method for treating ulcerative colitis patients, including active-stage patients receiving 5-aminosalicylic acid and/or corticosteroids with insufficient effect or intolerance.
Clinical evaluation over an 8-week period using an Example 1 versus placebo randomized comparison, including response, remission, mucosal remission, and histopathology outcomes.
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