Use of flibanserin in the treatment of obesity

Inventors

Ceci, AngeloSchindler, Marcus

Assignees

Sprout Pharmaceuticals Inc

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Publication Number

US-8785458-B2

Patent

Publication Date

2014-07-22

Expiration Date


Abstract

The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.

Core Innovation

The document discloses the use of flibanserin for treatment and/or prevention of obesity and related diseases. It includes flibanserin in free base form and as pharmacologically acceptable acid addition salts, including flibanserin hydrochloride, and optionally hydrates and solvates. The disclosed embodiments address promoting weight loss, inhibiting or reducing appetite, and preventing body weight gain by administering a therapeutically effective amount of flibanserin or a pharmacologically acceptable acid addition salt thereof.

The document provides a biological and target context for flibanserin based on binding/affinity at the 5-HT1A and 5-HT2 receptor family. It further defines obesity using body mass index (BMI) thresholds and identifies obesity subtypes and obesity-associated disorders, including metabolic syndrome (syndromeX), diabetes (type II), dyslipidaemia, hypertension, osteoarthritis/arthritis, diabetic retinopathy, and diabetic neuropathy, and includes insulin resistance and artherosclerosis in the listed associated conditions.

The document also describes combination concepts involving flibanserin together with a second active ingredient. It outlines that the second active ingredient may be selected from many anti-obesity and comorbidity agents, including named pharmacological categories and specific examples such as orlistat, sibutramine, phenetermine, and topiramate, and further includes extensive additional drug lists spanning antidiabetic/insulin-related agents, lipid-lowering agents, analgesic/anti-inflammatory and cardiovascular agents. The document additionally includes rat pharmacology data showing reduced body-weight gain with flibanserin doses compared with controls.

Claims Coverage

The partial content provides three independent claims directed to promoting weight loss, inhibiting body weight gain, and inhibiting or reducing appetite. Across these independent claims, the core inventive element is administering flibanserin, including free base and pharmacologically acceptable acid addition salts, for the respective obesity and weight-management objective, with dependent claims expanding scope via combination administration using a second active ingredient selected from enumerated alternatives.

Promoting weight loss by administering flibanserin

Administering to an individual in need a therapeutically effective amount of flibanserin, or a pharmacologically acceptable acid addition salt thereof, to promote, increase or facilitate weight loss.

Inhibiting body weight gain by administering flibanserin

Administering to an individual in need a therapeutically effective amount of flibanserin, or a pharmacologically acceptable acid addition salt thereof, to inhibit body weight gain.

Inhibiting or reducing appetite by administering flibanserin

Administering to an individual in need a therapeutically effective amount of flibanserin, or a pharmacologically acceptable acid addition salt thereof, to inhibit or reduce appetite.

The claim set in the provided partial content centers on flibanserin administration for weight-loss-related outcomes, with combination possibilities introduced in dependent claims by administering a second active ingredient selected from extensive enumerated alternatives.

Stated Advantages

Promotes, increases or facilitates weight loss.

Inhibits or reduces appetite.

Inhibits body weight gain.

Prevents body weight gain.

Reduced body-weight gain observed in rat pharmacology data with flibanserin doses versus controls.

Documented Applications

Treatment and/or prevention of obesity and related diseases, including promoting weight loss and preventing body weight gain.

Treatment and/or prevention of appetite-related aspects of obesity by inhibiting or reducing appetite.

Management of obesity-associated disorders including metabolic syndrome (syndromeX), diabetes (type II), dyslipidaemia, hypertension, osteoarthritis/arthritis, diabetic retinopathy, diabetic neuropathy, insulin resistance, and artherosclerosis.

Combination therapy use cases for obesity and comorbidities by administering flibanserin together with a second active ingredient selected from listed anti-obesity and comorbidity agents.

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