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Treatment for high cholesterol

A high-cholesterol, cholesterol-high technology, applied in medical preparations containing active ingredients, pharmaceutical formulations, organic chemistry, etc., can solve the problem of not being able to reduce total cholesterol LDL-C and so on

Inactive Publication Date: 2015-03-18
FIBROGEN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Additionally, for some patients, currently available agents do not provide sufficient levels of lowering of total cholesterol and / or LDL-C

Method used

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  • Treatment for high cholesterol
  • Treatment for high cholesterol
  • Treatment for high cholesterol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0234] Example 1: Effect of Compound A on Cholesterol Levels in Treated Anemic CKD or ESRD Patients

[0235] Study 1 was a phase 2 randomized open-label dose-adjusted efficacy and safety study of Compound A in anemic non-dialysis chronic kidney disease (CKD) patients. The primary objective of the study was to evaluate the efficacy and safety of the compound in correcting anemia (ie increasing hemoglobin levels) in non-dialysis CKD patients. The study included 6 dosing groups of approximately 24 individuals each. Subjects in Study 1 received Compound A at a dose range of 1.0 mg / kg-2.5 mg / kg at a frequency of once, twice or three times per week. Groups A and B received a weight-adjusted dose of approximately 1 mg / kg three times a week for 16 weeks; once the anemia was corrected, the dose in group B was reduced to twice a week. Groups C and D received a fixed dose of 50 mg or 100 mg, three times a week, for 24 weeks. Group E received a weight-adjusted dose of approximately 1 m...

Embodiment 2

[0261] Example 2: Reduction of Circulating LDL-C in Healthy Individuals

[0262] Plasma (sodium heparin anticoagulant) samples were collected from subjects receiving placebo (n=6) or 0.75 mg / Kg (n=6) or 1.88 mg / Kg (n=6) compound orally twice weekly. Compound A was taken on the first day after an overnight fast. Subjects were fasted overnight prior to subsequent dosing days. Overnight fasting is not required on non-dosing days. Samples were stored frozen at -70°C for up to 6 years and subjected to up to 2 thaw / freeze cycles before testing. Results are shown separately for samples taken during fasting: Day 1 (0, 1, 2 hours after dosing), Day 2 (24 hours), Day 3 (72 hours), Day 7 (168 hours), Day 10 (240 hours) and Day 17 (408 hours).

[0263] Samples were analyzed using a validation test in a Roche modular system. Total cholesterol was determined using the CHOD-PAP reagent from Roche cat no. 11875540216. HDL cholesterol was determined using reagents from Polymedco Cat# 940...

Embodiment 3

[0267] Embodiment 3: Effect of a single dose of compound A on rat blood lipid panel

[0268] The effect of a single oral dose of Compound A on changes from baseline in cholesterol, HDL, LDL levels and LDL / HDL ratio was evaluated in Sprague-Dawley rats. Compound A was administered at a dose of 60 mg / kg to rats (6 rats / dosing group), followed by overnight fasting. Blood samples were collected at baseline (pre-dose) and approximately 24 hours post-dose to determine levels of cholesterol, HDL, LDL and LDL / HDL ratio.

[0269] The data generated in this study showed that administration of a single oral dose of 60 mg / kg of Compound A to fasted Sprague-Dawley rats resulted in an increase in total cholesterol, LDL and LDL / HDL ratio after a single dose 24 hours significantly decreased from baseline. After 24 hours, total cholesterol decreased by 26±9 mg / dL, HDL decreased by 21±7 mg / dL, LDL decreased by 11±3 mg / dL, and LDL / HDL ratio decreased by 0.14±0.08. The mean percent reduction ±...

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Abstract

The present invention provides a method for treatment of high cholesterol by reducing low density lipoprotein cholesterol (LDL-C) and / or very low density Opoproiein cholesterol (VLDL-C) in subjects In need thereof by administering a compound that inhibits HIF hydroxylase activity. The method is useful, for reducing LDL cholesterol levels and total cholesterol levels even In subjects already undergoing treatment with other cholesterol-lowering medications, for example statins, fibrates, nicotinic acids and bile acid-binding resins, and in patients having chronic kidney disease or end stage renal disease, inter alia.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Application 61 / 609,007, filed March 9, 2012, and U.S. Provisional Application 61 / 650,043, filed May 22, 2012, the entire contents of which are incorporated by reference Incorporated into this article. field of invention [0003] The present invention relates to methods of treatment for reducing circulating levels of total cholesterol, in particular for reducing circulating levels of LDL-C and / or VLDL-C, and / or increasing the ratio of HDL-C / LDL-C. Background of the invention [0004] Over the past 25 years, substantial evidence from numerous clinical trials has demonstrated that pharmaceutical agents that lower blood levels of total cholesterol, particularly low-density lipoprotein-cholesterol (LDL-C), also reduce the risk of coronary heart disease (CHD). The totality of clinical data to date supports the notion that lowering circulating l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/00
CPCA61K31/472A61K31/437C07D217/26C07D471/04A61K45/06A61K2300/00
Inventor 林跃托马斯·B·内夫余健鸿
Owner FIBROGEN INC
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