Pharmaceutical formulations of amyloid inhibiting compounds
First Claim
Patent Images
1. An oral formulation comprising an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable vehicle, wherein, when the formulation is administered in a dose of 50 mg of the active agent, a mean plasma concentration profile having a mean AUC∞
- of about 1396 ng▪
h/mL±
20%, and a mean Cmax of about 310 ng/mL±
20% is achieved, and wherein the formulation is effective to inhibit or prevent amyloid deposition and/or treat or prevent an amyloid-related disease.
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Abstract
Therapeutic formulations and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Therapeutic formulations and methods for preventing or treating amyloidosis and/or amyloid-related disease are also described.
53 Citations
16 Claims
-
1. An oral formulation comprising an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable vehicle,
wherein, when the formulation is administered in a dose of 50 mg of the active agent, a mean plasma concentration profile having a mean AUC∞ - of about 1396 ng▪
h/mL±
20%, and a mean Cmax of about 310 ng/mL±
20% is achieved, andwherein the formulation is effective to inhibit or prevent amyloid deposition and/or treat or prevent an amyloid-related disease. - View Dependent Claims (4, 5, 6, 7, 15)
- of about 1396 ng▪
-
2. An oral formulation comprising an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable vehicle,
wherein, when the formulation is administered in a dose of 100 mg of the active agent, a mean plasma concentration profile having a mean AUC∞ - of about 2569 ng▪
h/mL±
20%, and a mean Cmax of about 618 ng/mL±
20% is achieved, andwherein the formulation is effective to inhibit or prevent amyloid deposition and/or treat or prevent an amyloid-related disease.
- of about 2569 ng▪
-
3. An oral formulation comprising an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable vehicle,
wherein, when the formulation is administered in a dose of 150 mg of the active agent, a mean plasma concentration profile having a mean AUC∞ - of about 3418 ng▪
h/mL±
20%, and a mean Cmax of about 624 ng/mL±
20% is achieved, andwherein the formulation is effective to inhibit or prevent amyloid deposition and/or treat or prevent an amyloid-related disease.
- of about 3418 ng▪
- 8. A method of lessening gastrointestinal side effects in a human patient which occur from orally administering an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof, comprising administering said agent according to a schedule wherein an initial dose is administered and the dose is increased over time to a higher dose which inhibits or prevents amyloid deposition and/or treats or prevents an amyloid-related disease.
-
12. A method for lowering the level of Aβ
-
42 in the cerebrospinal fluid of a patient which comprises orally administering to the patient an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof, in a formulation which, when administered in a dose of 100 mg of the active agent, achieves a mean plasma concentration profile having a mean AUC0-t of about 2467 ng▪
h/mL±
20% and, a mean Cmax of about 618 ng/mL±
20%.
-
42 in the cerebrospinal fluid of a patient which comprises orally administering to the patient an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof, in a formulation which, when administered in a dose of 100 mg of the active agent, achieves a mean plasma concentration profile having a mean AUC0-t of about 2467 ng▪
-
13. A method for treating and/or preventing Alzheimer'"'"'s disease in a patient which comprises orally administering to the patient an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof, in a formulation which, when administered in a dose of 100 mg of the active agent, achieves a mean plasma concentration profile having a mean AUC0-t of about 2467 ng▪
- h/mL±
20% and, a mean Cmax of about 618 ng/mL±
20%.
- h/mL±
-
14. A method for stabilizing cognitive function or decreasing the rate of decline in cognitive function, as assessed by Clinical Dementia Rating (CDR) scale, Mini-mental State Examination (MMSE), or Alzheimer'"'"'s Disease Assessment Scale-Cognitive Subscale (ADAS-Cog), in a patient which comprises orally administering to the patient an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof, in a formulation which, when administered in a dose of 100 mg of the active agent, achieves a mean plasma concentration profile having a mean AUC0-t of about 2467 ng▪
- h/mL±
20% and, a mean Cmax of about 618 ng/mL±
20%.
- h/mL±
-
16. An oral formulation for lessening gastrointestinal side effects in a human patient which occur from administration of an active agent which is 3-amino-1-propanesulfonic acid or a pharmaceutically acceptable salt thereof in an immediate release dosage form, comprising an effective amount of said agent to treat amyloidosis, inhibit or prevent amyloid deposition and/or treat or prevent an amyloid deposition-related disease and a pharmaceutically accetpable vehicle, wherein the formulation results in lesser side effects in comparison to those of said immediate release dosage form, and wherein the formulation, when administered in a dose of 100 mg of the active agent, achieves a mean plasma concentration profile having a mean AUC0-t of about 2467 ng▪
- h/mL±
20% and, a mean Cmax of about 618 ng/mL±
20%.
- h/mL±
Specification