Methods and compositions comprising at least one α3 βA4 nAChR antagonist or pharmaceutically acceptable salt thereof
AssigneeAGI Therapeutics Public Limited Company
InventorJohn Devane
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Abstract
The present invention is directed to methods and formulations for treating, modifying, and/or managing gastrointestinal secretion, and intestinal conditions that cause the same. Methods of using at least one α3 β4 nAChR antagonist and formulations comprising at least one α3 β4 nAChR antagonist, or pharmaceutically acceptable salt thereof, are included.
Claims12
A pharmaceutical composition comprising a therapeutically-effective amount of N-2,3,3-tetramethylbicyclo-[2.2.1]heptan-2-amine or pharmaceutically-acceptable salt thereof and at least one pharmaceutically-acceptable excipient in a modified-release formulation in a dosage form chosen from oral, intra-nasal, and transdermal forms;
- wherein:
- N-2,3,3-tetramethylbicyclo-[2.2.1]heptan-2-amine exhibits an IC50 value for the α3 β4 sub-type of nAChR ranging from 1.0=10-6 to 1×10-9 M or exhibits a potency for the α3 β4 nAChR sub-type at least two-times greater in comparison to at least one other nAChR sub-type;
- the composition produces a peak:trough plasma level ratio of greater than zero to less than about 4:1;
- the therapeutically-effective amount ranges from about 2 mg to about 12 mg per day;
- the composition minimizes at least one side effect chosen from effects on heart rate, blood pressure, vision, and bladder function associated with a conventional formulation of the at least one an α3 β4 nAChR antagonist or pharmaceutically-acceptable salt thereof;
- and
- N-2,3,3-tetramethylbicyclo-[2.2.1]heptan-2-amine or the pharmaceutically-acceptable salt thereof is the sole active pharmaceutical compound in the composition.
Dependencies are inferred from the claim text.