Escalating dosing regimen for effecting weight loss and treating obesity
Inventors
Najarian, Thomas • Tam, Peter Y. • Wilson, Leland F.
Assignees
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Publication Number
US-8580299-B2
Publication Date
2013-11-12
Expiration Date
Abstract
The present invention is drawn to novel topiramate compositions as well as methods for effecting weight loss, e.g., in the treatment of obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention features an escalating dosing regimen adapted for the administration of topiramate and optionally a sympathomimetic agent such as phentermine or bupropion, in the treatment of obesity and related conditions.
Core Innovation
The invention relates to a method for effecting weight loss in a subject having a body mass index of at least 30 kg/m2 and a condition associated with obesity. The method administers an escalating unit dosage form over an initial period and then continues daily dosing for an extended duration while treating the condition associated with obesity.
The unit dosage form includes controlled-release topiramate and immediate-release phentermine as part of the escalating regimen. The controlled-release topiramate reaches maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration and exhibits a lower Cmax than non-controlled release topiramate without decreasing total drug exposure defined by the area under the concentration-time curve (AUC).
The disclosed purpose is enabling a reduction in side effects without compromising the efficacy of the treatment while effecting weight loss. In the described regimen, a first dosage form is administered daily for 2 weeks and then a second dosage form is administered daily for at least 2 years, thereby effecting weight loss and treating the obesity-associated condition.
Claims Coverage
The partial content provides one independent claim covering an escalating long-term weight-loss method in obese subjects using controlled-release topiramate combined with immediate-release phentermine, with specific pharmacokinetic performance targets to reduce side effects without decreasing AUC.
Escalating unit dosage form with controlled-release topiramate and immediate-release phentermine
Administering an escalating unit dosage form that includes a first dosage form daily for 2 weeks comprising controlled-release topiramate and immediate-release phentermine, followed by a second dosage form daily for at least 2 years comprising controlled-release topiramate and immediate-release phentermine.
Pharmacokinetic profile enabling reduced side effects without decreasing AUC
Configuring the controlled-release topiramate such that it reaches maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration and exhibits a lower Cmax, than non-controlled release topiramate, without decreasing total drug exposure defined by the area under the concentration-time curve (AUC), enabling a reduction in side effects without compromising the efficacy of the treatment.
Weight loss treatment in obese subjects with obesity-associated condition
Using the method in a subject having a body mass index of at least 30 kg/m2 and a condition associated with obesity, wherein the method effecting weight loss also treats the condition associated with obesity during daily dosing.
Across the independent claim, the inventive concept is a daily escalating regimen that pairs controlled-release topiramate with immediate-release phentermine and is characterized by a reduced Cmax at delayed Tmax while maintaining AUC, to enable reduced side effects without compromising efficacy for long-term weight loss in obese subjects with an obesity-associated condition.
Stated Advantages
Reduction in side effects without compromising the efficacy of the treatment.
Documented Applications
Treating a condition associated with obesity in a subject having a body mass index of at least 30 kg/m2 by effecting weight loss.
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