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Ppary agonist for treatment of bone disorders

A bone growth and bone loss technology, applied in bone diseases, drug combinations, active ingredients of heterocyclic compounds, etc., can solve problems such as unpredictable efficacy of INT131

Inactive Publication Date: 2019-06-04
INTEKRIN THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the effect of other PPARγ agonists on patients cannot predict the efficacy of INT131

Method used

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  • Ppary agonist for treatment of bone disorders
  • Ppary agonist for treatment of bone disorders
  • Ppary agonist for treatment of bone disorders

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Experimental program
Comparison scheme
Effect test

specific Embodiment approach

[0030] New uses for known compounds that modulate PPARγ have now been discovered. In particular, PPARγ agonists, particularly INT131, have been found to be effective in the treatment of osteoporosis.

[0031] Accordingly, in one embodiment, the present invention relates to a method for treating osteoporosis or its symptoms in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of INT131 or a pharmaceutically acceptable salt, prodrug thereof or the pharmaceutical composition of the isomer.

[0032] In the study of 10mg / kg INT131 administered to obese mice, it is suggested that INT131 may be an ideal drug that does not affect the bone mass of patients with type 2 diabetes. Lee et al., The Selective PPARγ Modulator INT131 Normalizes Insulin Signaling Defects and Improves Bone Mass in Diet-Induced Obese Mice, Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E552-60. However, INT131 has not been shown to be useful for treating os...

Embodiment 1

[0050] NT131 is a potent adiponectin upregulator in patients with reduced adiponectin levels

[0051] method

[0052] A randomized, double-blind, placebo-controlled 24-week study was conducted in which adiponectin levels were measured. The study had a 2-week run-in period, a 24-week double-blind treatment period and a 2-week follow-up period. 367 patients with type 2 diabetes mellitus (TD2), a disease in which patients have reduced adiponectin levels, were randomly assigned to receive 0.5, 1, 2, or 3 mg of INT131 besylate, 45 mg of pioglitazone, or placebo daily for 24 days. week. To measure adiponectin levels, blood was drawn at weeks 0, 2, 6, 12 and 24.

[0053] The results of this study showed that INT131 at doses of 1, 2 and 3 mg resulted in HbA compared with placebo 1c level was statistically significantly lower. Furthermore, the study showed that INT131 at doses of 2 mg and 3 mg reduced HbA 1c Levels at least consistent with 45 mg of pioglitazone, an FDA-approved T...

Embodiment 2

[0065] INT131 is a potent upregulator of adiponectin in healthy subjects

[0066] method

[0067]A study was conducted to determine the effect of INT131 on serum adiponectin levels. 30 healthy subjects were randomly selected to receive placebo, 0.1mg INT131, 1mg INT131 or 4mg INT131 daily for 14 days. To measure adiponectin levels, blood was drawn on days 1, 4, 8 and 14.

[0068] result

[0069] From day 1 to day 14, administration of placebo and 0.1 mg INT131 did not significantly change serum adiponectin levels, and further administration of 0.1 mg INT131 resulted in no significant change in adiponectin levels compared to placebo. see figure 1 . However, administration of 1 mg or 4 mg INT131 resulted in significant changes in serum adiponectin levels relative to placebo and from day 1 to day 14. Thus, administration of INT131 was able to upregulate adiponectin in healthy individuals.

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Abstract

Methods of treatment of bone disorders, including osteoporosis or its symptoms, with PPARY agonists, and in particular, the compound of formula (I) known as INT131 : (I).

Description

field of invention [0001] The present invention relates to methods of treating bone disorders including bone loss and osteoporosis. Background technique [0002] Osteoporosis is a disease that leads to weakened bones and an increased risk of fractures. According to reports, women over the age of 50 in the United States have about a 50 percent chance of breaking a bone during their lifetime. Osteoporosis is thought to cause about 1.5 million fractures each year in the United States, including about 700,000 spine fractures and about 300,000 hip fractures. According to the Mayo Clinic, about 25 percent of people over the age of 50 who fracture a hip die within a year of the accident. After the first fracture, the risk of fracture is doubled in people with osteoporosis. Osteoporotic individuals have an approximately four-fold increased risk of second vertebral fracture after a first vertebral fracture. [0003] Osteoporosis is a common cause of fractures in the elderly. Ost...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61P19/10A61P19/08
CPCA61K31/47A61P19/00A61P19/10
Inventor D·兰费尔
Owner INTEKRIN THERAPEUTICS