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Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders

a technology which is applied in the field of co-therapy comprising the administration of canagliflozin and phentermine for the treatment of obesity and obesity related disorders, can solve the problems of increased risk of cardiovascular disease, so as to reduce the risk of cardiovascular disease and improve the effect of cardiovascular diseas

Inactive Publication Date: 2017-03-16
JANSSEN PHARMA NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a composition that includes canagliflozin, phentermine, and a carrier, for the treatment of obesity and related disorders. The composition is designed to target specific disorders associated with renal or fatty liver disorders, such as hyperfiltrative diabetic nephropathy and compensatory hyperfiltration. The technical effect of this composition is to provide an effective treatment for obesity and related disorders while addressing the specific needs of renal or fatty liver disorder patients.

Problems solved by technology

Obesity is more common among women and in the poor; the prevalence in children is also rising at a worrisome rate.
Obesity has major adverse effects on health.
There is also a higher probability of high blood pressure, sexual dysfunction, headaches, depression and sleep apnea.
People with diabetes either don't produce insulin, produce too little insulin or do not respond to insulin, resulting in the build up of glucose in the blood.
Damage to the nephrons represents an important form of kidney disease.
This damage may leave kidneys unable to remove wastes.
When the kidneys do not properly filter large molecules (such as albumin) from the urine, albumin is excreted in urine and is typically a sign of kidney damage or excessive salt intake.
Symptoms of sleep apnea include excessive daytime sleepiness (EDS) and impaired alertness.
In other words, common effects of sleep apnea include daytime fatigue, a slower reaction time, and vision problems.
OSA may increase risk for driving accidents and work-related accidents.
If OSA is not treated, one has an increased risk of other health problems such as diabetes.
Even death could occur from untreated OSA due to lack of oxygen to the body.
Another symptom of sleep apnea is waking up in sleep paralysis.
In severe cases, the fear of sleep due to sleep paralysis can lead to insomnia.
These effects become very hard to deal with, thus the development of depression may transpire.
There is also increasing evidence that sleep apnea may also lead to liver function impairment, particularly fatty liver diseases.
Brain tumors may hinder the brain's ability to regulate normal breathing.
During sleep, when throat and tongue muscles are more relaxed, this soft tissue can cause the airway to become blocked.

Method used

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  • Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders
  • Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders

Examples

Experimental program
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Effect test

example 1

Trial

Co-Therapy with 300 mg Canagliflozin and 15 mg Phentermine

[0281]The safety and efficacy of combination treatment with 300 mg canagliflozin and 15 mg phentermine was investigated in a 26 week, randomized, double-blind, placebo-controlled, parallel group, multi-center study. (Complete study protocol filed and available as STUDY 28431754-OBE2002 on www.clinicaltrials.gov).

Trial Design:

[0282]The study began with a 4-week single blind placebo run-in period. After completing the run-in period 335 overweight or obese non-diabetic adult subjects who had a BMI≧230 kg / m2 and 2 at screening; or BMI≧227 kg / m2 and 2 at screening in the presence of a comorbidity / comorbidities of hypertension and / or dyslipidemia were randomly assigned in a 1:1:1:1 ratio to treatment with (A) canagliflozin 300 mg and phentermine 15 mg, (B) canagliflozin 300 mg, (C) phentermine 15 mg, or (D) placebo with the stratification factor run-in weight loss of ≦2 kg or >2 kg. All subjects were provided with diet and exe...

formulation example 1

[0293]As a specific embodiment of an oral composition, 300 mg of canagliflozin and 15 mg of phentermine are formulated with sufficient finely divided lactose to provide a total amount of 580 to 590 mg to fill a size O hard gel capsule.

formulation example 2

[0294]As a specific embodiment of an oral composition, 300 mg of canagliflozin and 15 mg of phentermine are formulated with lactose and microcrystalline cellulose to provide a tablet of total weight in the amount of about 600 mg to about 620 mg.

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Abstract

The present invention is directed to the use of co-therapy comprising administration of canagliflozin and phentermine for the treatment of obesity and obesity related disorders. More particularly, the present invention is directed to co-therapy for treating obesity, for promoting weight loss and / or for suppressing appetite; for treating, delaying, slowing the progression of and / or preventing metabolic disorders (including for example Type 2 diabetes mellitus); for treating, delaying, slowing the progression of and / or preventing renal or fatty liver disorders (including for example NASH, NAFLD, etc.); for treating, delaying, slowing the progression of and / or preventing sleep disorders (including for example sleep apnea); for providing cardiovascular protection; for treating, delaying, slowing the progression of and / or preventing cardiovascular events (including major adverse cardiac events (MACE) such as myocardial infarction, unstable angina, cardiovascular death, revascularization, fatal or non-fatal cerebrovascular accident, peripheral arteriopathy, aortic events, hospitalization due to congestive heart failure, etc.); and / or for extending or prolonging life span.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. Provisional Patent Application No. 62 / 218,842, filed Sep. 15, 2015, and U.S. Provisional Patent Application No. 62 / 306,110, filed Mar. 10, 2016, the disclosures of which are hereby incorporated by reference in their entireties.FIELD OF THE INVENTION[0002]The present invention is directed to the use of co-therapy comprising administration of canagliflozin and phentermine for the treatment of obesity and obesity related disorders. More particularly, the present invention is directed to co-therapy for treating obesity, for promoting weight loss and / or for suppressing appetite; for treating, delaying, slowing the progression of and / or preventing metabolic disorders (including for example Type 2 diabetes mellitus); for treating, delaying, slowing the progression of and / or preventing renal or fatty liver disorders (including for example NASH, NAFLD, etc.); for treating, delaying, slowing the progression ...

Claims

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Application Information

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IPC IPC(8): A61K31/7042A61K31/135
CPCA61K31/135A61K31/7042A61K31/137A61P1/16A61P13/00A61P3/00A61P3/04A61P43/00A61P9/00A61P9/12A61K2300/00
Inventor ROSENTHAL, NORMAN R.ROTHENBERG, PAULPOLIDORI, DAVID C.WAYS, DOUGLAS K.STEIN, PETER P.
Owner JANSSEN PHARMA NV
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