Treatment of metabolic syndrome with an sGC stimulator
Inventors
Hanrahan, John P. • Profy, Albert Thomas • Wakefield, James D.
Assignees
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Publication Number
US-11389449-B2
Publication Date
2022-07-19
Expiration Date
Abstract
The present invention provides a method of treating a subject with metabolic syndrome by administering a stimulator of soluble guanylate cyclase (sGC) (Compound I) either alone or in combination therapy with a blood glucose lowering (antihyperglycemic or antidiabetes) medication, a blood pressure lowering (anti-hypertensive) medication, an anti-hyperlipidemic medication, or combinations thereof. It also relates to a method of reducing the level of a clinical marker selected from the group comprising of fasting blood glucose levels, fasting blood insulin levels, hemoglobin A1C (HbA1C) levels, blood cholesterol levels (total or LDL), blood ApoB levels, HOMA-IR levels, blood triglyceride levels, blood concentration of ADMA, blood levels of alanine transaminase, aspartate transaminase, and GGT, body weight and abdominal circumference, or any combination of these markers thereof, in a subject in need thereof by administering a stimulator of sGC (Compound I) either alone or in combination therapy with a blood glucose lowering (antihyperglycemic or antidiabetes) medication, a blood pressure lowering (anti-hypertensive) medication, an anti-hyperlipidemic medication, or combinations thereof.
Core Innovation
The disclosed invention uses an sGC stimulator, referred to as Compound I, for treating metabolic syndrome in a human patient. The method includes administering Compound I as a single oral daily dose between 10 mg and 50 mg.
The described approach is also directed to reducing levels of metabolic markers in humans. The markers include fasting blood glucose, fasting blood insulin, HbA1C, blood cholesterol, apolipoprotein B (ApoB), blood triglyceride, and body weight, using the same oral daily dosing of Compound I between 10 mg and 50 mg.
Additionally, the disclosed invention is directed to increasing insulin sensitivity or improving endothelial function while reducing cardiovascular risk. These objectives are addressed by administering Compound I with a single oral daily dose between 10 mg and 50 mg.
Claims Coverage
The provided claims include three independent claims. Across them, the inventive coverage centers on treating metabolic syndrome, reducing selected metabolic markers, and increasing insulin sensitivity and/or improving endothelial function while reducing cardiovascular risk, each via administering Compound I as a single oral daily dose between 10 mg and 50 mg.
Treating metabolic syndrome with Compound I single oral daily dose
A method of treating a human patient with metabolic syndrome by administering Compound I as a single oral daily dose between 10 mg and 50 mg.
Reducing a metabolic marker level with Compound I single oral daily dose
A method of reducing the level of a metabolic marker selected from fasting blood glucose, fasting blood insulin, HbA1C, blood cholesterol, apolipoprotein B (ApoB), blood triglyceride, and body weight by administering Compound I as a single oral daily dose between 10 mg and 50 mg.
Increasing insulin sensitivity and/or improving endothelial function with Compound I single oral daily dose
A method of increasing insulin sensitivity or improving endothelial function and reducing cardiovascular risk by administering Compound I as a single oral daily dose between 10 mg and 50 mg.
Overall, the claim set consistently ties the therapeutic and physiological objectives to Compound I administered orally once per day within 10 mg to 50 mg.
Stated Advantages
Reduces levels of metabolic markers selected from fasting blood glucose, fasting blood insulin, HbA1C, blood cholesterol, ApoB, blood triglyceride, and body weight.
Increases insulin sensitivity.
Improves endothelial function.
Reduces cardiovascular risk.
Improves liver function.
Documented Applications
Use of Compound I to treat metabolic syndrome in humans, including alone or in combination with combination therapies directed to lowering blood glucose, lowering blood pressure, and/or anti-hyperlipidemic drugs.
Clinical/metabolic marker assessment in humans including fasting glucose/insulin, HbA1C, cholesterol/LDL, ApoB, triglycerides, HOMA-IR, ADMA, liver enzymes ALT/AST/GGT, and body weight/abdominal circumference, with functional aims of improving insulin sensitivity, endothelial function, and liver function and reducing cardiovascular risk.
Phase 2a clinical regimen embodiments assessing fasting glucose, insulin, lipids, ApoB, ADMA, liver enzymes, and HOMA-IR over a short period with placebo-referenced reductions reported.
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